Autoimmune Diseases
Conditions
Keywords
Crossover, Sequential, GSK2982772, Safety, Pharmacokinetics, Healthy subjects
Brief summary
This study is designed to evaluate the safety, tolerability and PK of GSK2982772, in repeat oral doses in healthy subjects. This study is being conducted to support administration of higher dose levels of GSK2982772 than initially studied in the First Time in Human (FTiH) study. This study will also assess the impact of food during the repeat doses of GSK2982772. This will be a two part study; Part A and Part B. Part A (cohort 1) - single ascending dose, randomized, placebo-controlled, 3-way crossover. Part B (cohorts 2, 3, 4 and 5) - repeat dose, randomized, placebo-controlled, sequential-group. Subjects will be randomized in 3:1 ratio to receive GSK2982772 or placebo in crossover manner on Day 1 of each of the three periods in Part A. Subjects will be randomized in 3:1 ratio to receive GSK2982772 or placebo in sequential groups for 14 days in cohort 2 of Part B and in 9:5 ratio to receive GSK2982772 or placebo in sequential groups for 14 days in cohorts 3, 4 and 5 of Part B. Approximately 66 subjects will be included in this study. The study duration, including screening and follow-up, will not be expected to exceed 13 weeks for Part A and 8 weeks for Part B.
Interventions
GSK2982772 will be available as size 00, white, opaque capsule containing white to almost white Solid (120 mg maximum fill per capsule). It will be administered orally with water to receive total dose of 120 mg, 240 mg or 360 mg per randomization.
DRUGPlacebo capsule
Placebo will be available as size 00, white, opaque capsule containing white to almost white Solid. It will be administered orally with water.
Sponsors
GlaxoSmithKline
Study design
Allocation
RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
TREATMENT
Masking
DOUBLE (Subject, Investigator)
Masking description
This will be a double-blind study. Subjects and investigator will be masked.
Intervention model description
This study will consist of two parts; Part A and Part B. Part A will be a 3-way crossover design and Part B will be a sequential-group design.
Eligibility
Sex/Gender
ALL
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Subject must be 18 to 65 years of age inclusive, at the time of signing the informed consent. * Healthy as determined by the Investigator or medically qualified designee based on a medical evaluation including medical history, physical examination, neurological examination, laboratory tests and cardiac monitoring. A subject with a clinical abnormality or laboratory parameter(s) which is/are not specifically listed in the inclusion or
Exclusion criteria
, outside the reference range for the population being studied may be included only if the Investigator in consultation with the Medical Monitor (if required) agree and document that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures. * Body weight \>=50 kilograms (kg) and body mass index (BMI) within the range 19 - 30 kg per square meter (kg/m\^2) (inclusive). * A male subject with a female partner of reproductive potential must agree to use contraception during the treatment period and for at least 90 days after the last dose of study treatment and refrain from donating sperm during this period. A female subject is eligible to participate if she is not pregnant, not breastfeeding, and at least one of the following conditions applies: not a woman of childbearing potential (WOCBP) or a WOCBP who agrees to follow the contraceptive guidance for a minimum of 28 days prior to the treatment period and for at least 30 days after the last administration of study drug. A WOCBP using a hormonal method of highly effective contraception must also agree to partner use of a male condom during the treatment period and for at least 30 days after the last administration of study drug. * Capable of giving signed informed consent.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Number of Participants With AEs and SAEs: Part B | Up to Day 28 | An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment were categorized as SAE. |
| Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | Up to Day 14 | An AE is any untoward medical occurrence in a clinical study subjects, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment will be categorized as SAE. |
| Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Up to Week 9 | Blood samples were collected from participants for the analysis of following clinical chemistry parameters: alanine amino transferase (ALT), albumin, alkaline phosphatase, aspartate amino transferase (AST), calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times Upper Limit of Normal (ULN) units per liter (U/L) for ALT, \<30 grams per liter (g/L) for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 millimoles per liter (mmol/L) for calcium, \>44.2 micromoles per liter (µmol/L) for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category. |
| Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Up to Week 4 | Blood samples were collected from participants for the analysis of following clinical chemistry parameters: ALT, albumin, alkaline phosphatase, AST, calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times ULN U/L for ALT, \<30 g/L for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 mmol/L for calcium, \>44.2 µmol/L for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category. |
| Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Up to Week 9 | Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and white blood cell (WBC) counts. PCI ranges were \>0.54 or \< 0.075 proportion of red blood cells (RBC) in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category. |
| Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Up to Week 4 | Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and WBC counts. PCI ranges were \>0.54 or \< 0.075 proportion of RBC in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category. |
| Number of Participants With Worst Case Urinalysis Results: Part A | Up to Week 9 | Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented. |
| Number of Participants With Worst Case Urinalysis Results: Part B | Up to Week 4 | Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented. |
| Number of Participants With Abnormal Vital Signs: Part A | Up to Week 9 | Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 millimeters of mercury \[mmHg\]), diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported. |
| Number of Participants With Abnormal Vital Signs: Part B | Up to Week 4 | Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 mmHg, diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported. |
| Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Up to Day 4 | 12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. |
| Number of Participants With Abnormal ECG Findings: Part B | Up to Week 4 | 12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| AUC (14-24) Following TID Dosing of GSK2982772 in Part B | 14 hours, 14 hours 20 minutes, 14 hours 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (7-14) Following TID Dosing of GSK2982772 in Part A | 7 hours, 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (14-24) Following TID Dosing of GSK2982772 in Part A | 14 hours, 14 hours 20 and 40 minutes, 15 and 15 hours 30 minutes, 16, 19, 22 and 24 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (0-12) Following BID Dosing of GSK2982772 in Part A | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (12-24) Following BID Dosing of GSK2982772 in Part A | 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (14-24) Following TID Dosing of GSK2982772 in Part B | 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (7-14) Following TID Dosing of GSK2982772 in Part A | 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (14-24) Following TID Dosing of GSK2982772 in Part A | 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (0-12) Following BID Dosing of GSK2982772 in Part A | Pre-dose, 20 and 40 minutes, 1hour, 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (12-24) Following BID Dosing of GSK2982772 in Part A | 12 hours, 12 hours 20 and 40 minutes, 13 hours, 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (0-7) Following TID Dosing of GSK2982772 Part B | Pre-dose, 20 and 40 minutes, 1 hour, 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (7-14) Following TID Dosing of GSK2982772 in Part B | 7hours and 7 hours 20 and 40 minutes, 8hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (14-24) Following TID Dosing of GSK2982772 in Part B | 14hours, 14 hours 20 and 40 minutes, 15 hours and 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A | 7 hours post-dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A | 14 hours post-dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C24 Following TID Dosing of GSK2982772 in Part A | 24 hours post-dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C12 Following BID Dosing of GSK2982772 in Part A | 12 hours post-dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C24 Following BID Dosing of GSK2982772 in Part A | 24 hours post-dose on Day 1 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A | Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C7 Following TID Dosing of GSK2982772 in Part B | 7 hours post-dose on Days 1 and 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C14 Following TID Dosing of GSK2982772 in Part B | 14 hours post-dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| C24 Following TID Dosing of GSK2982772 in Part B | 24 hours post-dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Pre-dose on Day 1 and 24 hours post first dose on Day 14 | Blood samples were collected into EDTA tubes and processed to plasma for 4 beta-hydroxycholesterol and cholesterol. Ratio of 4 beta-hydroxycholesterol to cholesterol is presented |
| C0 Following TID Dosing of GSK2982772 in Part B | Pre-dose on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC(0-24) Following BID Dosing of GSK2982772: Part A | Pre-dose, 20min, 40min, 1hr, 1hr 30min, 2hr, 3hr, 4hr, 6hr, 8hr, 10hr, 12hr, 12hr 20min, 12hr 40min, 13hr, 13hr 30min, 14hr, 15hr, 16hr, 19hr, 22hr, 24hr post dose on Day 1. | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC[0-24] Following TID Dosing of GSK2982772: Part B | Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day14 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (0-7) Following TID Dosing of GSK2982772 : Part A | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Day 1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (0-7) Following TID Dosing of GSK2982772 in Part B | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| Cmax (7-14) Following TID Dosing of GSK2982772 in Part B | 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (7-14) Following TID Dosing of GSK2982772 : Part A | 7 hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (14-24) Following TID Dosing of GSK2982772 : Part A | 14 hours, 14 hours 20 and 40 minutes, 15 hours ,15 hours 30 minutes, 16, 19, 22 and 24 hours on Day 1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (0-12) Following BID Dosing of GSK2982772 in Part A | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours,12 hours on Day 1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (12-24) Following BID Dosing of GSK2982772 in Part A | 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours on Day 1 | Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC(0-7) Following TID Dosing of GSK2982772 in Part B | Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 1 and 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
| AUC (7-14) Following TID Dosing of GSK2982772 in Part B | 7 and 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14 | Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis. |
Countries
United Kingdom
Participant flow
Recruitment details
This study consisted of two parts; part A was single ascending dose, 3-way crossover and part B was repeat dose, sequential assignment which investigated the safety, tolerability, and pharmacokinetics of GSK2982772, in healthy participants.
Pre-assignment details
A total of 62 participants (15 in Part A and 47 in Part B) were enrolled in the study. Participants were not enrolled into the GSK2982772 360 milligram (mg) twice daily (BID) arm of Part B as one participant in the 360 mg BID dose level in Part A exceeded the maximum concentration (Cmax) stopping criteria.
Participants by arm
| Arm | Count |
|---|---|
| Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID Participants received oral capsule of 120 mg GSK2982772 three times a day in treatment period 1 followed by 240 mg TID in treatment period 2 followed by 360 mg BID in treatment period 3. The treatment periods were separated by a washout period of at least 7 days. | 5 |
| Part A:GSK2982772 120 mg TID/240 mg TID/Placebo Participants received oral capsule of 120 mg GSK2982772 TID in treatment period 1 followed by 240 mg TID in treatment period 2 followed by matching Placebo in treatment period 3. The treatment periods were separated by a washout period of at least 7 days. | 4 |
| Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID Participants received oral capsule of 120 mg GSK2982772 TID in treatment period 1 followed by matching Placebo in treatment period 2 followed by 360 mg GSK2982772 BID in treatment period 3. The treatment periods were separated by a washout period of at least 7 days. | 3 |
| Part A:Placebo/GSK2982772 240 mg TID/360 mg BID Participants received oral capsule of matching Placebo in treatment period 1 followed by 240 mg GSK2982772 TID in treatment period 2 followed by 360 mg GSK2982772 BID in treatment period 3. The treatment periods were separated by a washout period of at least 7 days. | 3 |
| Part B:Placebo Participants received matching oral placebo capsule to GSK2928772 for 14 days. | 14 |
| Part B:GSK2982772 120 mg TID Participants received GSK2982772 oral capsule at a dose of 120 mg TID for 14 days | 20 |
| Part B:GSK2982772 240 mg TID Participants received GSK2982772 oral capsule at a dose of 240 mg TID for 14 days. | 13 |
| Part B:GSK2982772 360 mg TID Participants received GSK2982772 oral capsule at a dose of 360 mg TID for 14 days. | 0 |
| Total | 62 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 | FG003 | FG004 | FG005 | FG006 | FG007 |
|---|---|---|---|---|---|---|---|---|---|
| Part A Period 1 (1Day) + Washout (7days) | Adverse Event | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
| Part A Period 2 (1Day) + Washout (7days) | Adverse Event | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Part A Period 2 (1Day) + Washout (7days) | Physician Decision | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Part B (14 Days) | Adverse Event | 0 | 0 | 0 | 0 | 1 | 2 | 4 | 0 |
| Part B (14 Days) | Physician Decision | 0 | 0 | 0 | 0 | 2 | 8 | 1 | 0 |
Baseline characteristics
| Characteristic | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Total | Part B:GSK2982772 360 mg TID |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | 36.2 Years STANDARD_DEVIATION 9.04 | 42.5 Years STANDARD_DEVIATION 9.95 | 59.0 Years STANDARD_DEVIATION 3.61 | 49.0 Years STANDARD_DEVIATION 10 | 39.1 Years STANDARD_DEVIATION 9.66 | 43.3 Years STANDARD_DEVIATION 10.87 | 38.6 Years STANDARD_DEVIATION 11.03 | 45.25 Years STANDARD_DEVIATION 9.16 | — |
| Race/Ethnicity, Customized Asian - East Asian Heritage | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 1 Participants | 0 Participants | 0 Participants | 1 Participants | — |
| Race/Ethnicity, Customized Asian - Japanese Heritage | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 1 Participants | 0 Participants | 0 Participants | 1 Participants | — |
| Race/Ethnicity, Customized Black or African American | 0 Participants | 1 Participants | 1 Participants | 0 Participants | 0 Participants | 1 Participants | 3 Participants | 6 Participants | — |
| Race/Ethnicity, Customized White - White/Caucasian/European Herit | 5 Participants | 3 Participants | 2 Participants | 3 Participants | 12 Participants | 19 Participants | 10 Participants | 54 Participants | — |
| Sex: Female, Male Female | 2 Participants | 2 Participants | 1 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 5 Participants | 0 Participants |
| Sex: Female, Male Male | 3 Participants | 2 Participants | 2 Participants | 3 Participants | 14 Participants | 20 Participants | 13 Participants | 57 Participants | 0 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk | EG005 affected / at risk | EG006 affected / at risk | EG007 affected / at risk |
|---|---|---|---|---|---|---|---|---|
| deaths Total, all-cause mortality | 0 / 9 | 0 / 9 | 0 / 9 | 0 / 9 | 0 / 14 | 0 / 20 | 0 / 13 | 0 / 0 |
| other Total, other adverse events | 3 / 9 | 6 / 9 | 4 / 9 | 7 / 9 | 9 / 14 | 17 / 20 | 12 / 13 | 0 / 0 |
| serious Total, serious adverse events | 0 / 9 | 0 / 9 | 0 / 9 | 0 / 9 | 1 / 14 | 0 / 20 | 0 / 13 | 0 / 0 |
Outcome results
Primary
Number of Participants With Abnormal ECG Findings: Part B
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
Time frame: Up to Week 4
Population: Safety population. GSK2982772 360 mg BID of Part B was not started as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, not clinically significant | 3 Participants |
| Part A:Placebo | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, clinically significant | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, not clinically significant | 4 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, clinically significant | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, not clinically significant | 3 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal ECG Findings: Part B | Abnormal, clinically significant | 0 Participants |
Primary
Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
Time frame: Up to Day 4
Population: Safety population
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, not clinically significant | 1 Participants |
| Part A:Placebo | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, clinically significant | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, clinically significant | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, not clinically significant | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, clinically significant | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, not clinically significant | 2 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, not clinically significant | 4 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A | Abnormal, clinically significant | 0 Participants |
Primary
Number of Participants With Abnormal Vital Signs: Part A
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 millimeters of mercury \[mmHg\]), diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
Time frame: Up to Week 9
Population: Safety population
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Part A:Placebo | Number of Participants With Abnormal Vital Signs: Part A | 6 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal Vital Signs: Part A | 8 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal Vital Signs: Part A | 7 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Abnormal Vital Signs: Part A | 8 Participants |
Primary
Number of Participants With Abnormal Vital Signs: Part B
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 mmHg, diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
Time frame: Up to Week 4
Population: Safety population. GSK2982772 360 mg BID of Part B was not started as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Part A:Placebo | Number of Participants With Abnormal Vital Signs: Part B | 11 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Abnormal Vital Signs: Part B | 20 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Abnormal Vital Signs: Part B | 12 Participants |
Primary
Number of Participants With AEs and SAEs: Part B
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment were categorized as SAE.
Time frame: Up to Day 28
Population: Safety population. GSK2982772 360 mg BID was not started in Part B as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With AEs and SAEs: Part B | AEs | 9 Participants |
| Part A:Placebo | Number of Participants With AEs and SAEs: Part B | SAEs | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With AEs and SAEs: Part B | AEs | 17 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With AEs and SAEs: Part B | SAEs | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With AEs and SAEs: Part B | AEs | 12 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With AEs and SAEs: Part B | SAEs | 0 Participants |
Primary
Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: alanine amino transferase (ALT), albumin, alkaline phosphatase, aspartate amino transferase (AST), calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times Upper Limit of Normal (ULN) units per liter (U/L) for ALT, \<30 grams per liter (g/L) for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 millimoles per liter (mmol/L) for calcium, \>44.2 micromoles per liter (µmol/L) for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 9
Population: Safety population
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Creatinine, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Glucose, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Albumin, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Potassium, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Total Bilirubin, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | AST, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Sodium, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | ALT, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Calcium, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A | Alkaline phosphatase, No change | 9 Participants |
Primary
Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: ALT, albumin, alkaline phosphatase, AST, calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times ULN U/L for ALT, \<30 g/L for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 mmol/L for calcium, \>44.2 µmol/L for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 4
Population: Safety population. GSK2982772 360 mg BID of Part B was not started as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, No change | 14 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, High | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, No change | 19 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, No change | 19 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, High | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, No change | 20 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Total Bilirubin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | ALT, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Albumin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Alkaline phosphatase, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | AST, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Calcium, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Creatinine, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Glucose, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, No change | 12 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Potassium, High | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B | Sodium, Low | 0 Participants |
Primary
Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and white blood cell (WBC) counts. PCI ranges were \>0.54 or \< 0.075 proportion of red blood cells (RBC) in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 9
Population: Safety population.
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet count, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC count, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, No change | 8 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, No change | 9 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, Low | 1 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC count, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet count, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, No change | 9 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet count, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, No change | 9 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC count, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC count, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hematocrit, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | WBC, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Hemoglobin, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, No change | 9 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet count, Low | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Platelet, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, High | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A | Lymphocytes, Low | 0 Participants |
Primary
Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and WBC counts. PCI ranges were \>0.54 or \< 0.075 proportion of RBC in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 4
Population: Safety population. GSK2982772 360 mg BID of Part B was not started as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC count, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, High | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet count, Low | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, No change | 14 Participants |
| Part A:Placebo | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet count, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, Low | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, No change | 19 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC count, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, Low | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, No change | 20 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, High | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, No change | 12 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, No change | 10 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet count, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, Low | 3 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Total Neutrophils, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hemoglobin, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, Low | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, Low | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Platelet, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC, No change | 13 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Lymphocytes, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | Hematocrit, High | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B | WBC count, Low | 0 Participants |
Primary
Number of Participants With Worst Case Urinalysis Results: Part A
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
Time frame: Up to Week 9
Population: Safety population. Only those participants with available data at specified time points were analyzed.
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Any increase | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 1-9/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 1-9/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, No change | 3 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Any increase | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Any increase | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, No change | 3 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, No change | 3 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Any increase | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, No change | 3 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Any increase | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:Placebo | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, No change | 3 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, No change | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, No change | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, No change | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 1-9/HPF | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, No change | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, No change | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Any increase | 1 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 1-9/HPF | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, Any increase | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Granular casts, No change | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, No change | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, No change | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Any increase | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Cellular casts, Any increase | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, No change | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Any increase | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, Any increase | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | Hyaline casts, No change | 1 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Participants With Worst Case Urinalysis Results: Part A | RBC, Increase 1-9/HPF | 1 Participants |
Primary
Number of Participants With Worst Case Urinalysis Results: Part B
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
Time frame: Up to Week 4
Population: Safety population. GSK2982772 360 mg BID of Part B was not started as one participant in GSK2982772 360 mg BID of Part A exceeded the Cmax stopping criteria. Only those participants with data available at specified timepoints were analyzed.
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, No change | 7 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, No change | 5 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Any increase | 2 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Any increase | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Increase 1-9/HPF | 2 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, No change | 5 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Any increase | 2 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, No change | 7 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Increase 1-9/HPF | 2 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, No change | 7 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, No change | 2 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, No change | 2 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Increase to 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Cellular casts, Increase to 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Increase 1-9/HPF | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Hyaline casts, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, No change | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Any increase | 1 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | RBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, No change | 2 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Any increase | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Increase 1-9/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | WBC, Increase 10-50/HPF | 0 Participants |
| Part A:GSK2982772 240 mg TID | Number of Participants With Worst Case Urinalysis Results: Part B | Granular casts, No change | 2 Participants |
Primary
Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A
An AE is any untoward medical occurrence in a clinical study subjects, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment will be categorized as SAE.
Time frame: Up to Day 14
Population: Safety population. Safety population consists of all randomized participants who take at least 1 dose of study treatment.
| Arm | Measure | Group | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|---|
| Part A:Placebo | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | AEs | 3 Participants |
| Part A:Placebo | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | SAEs | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | SAEs | 0 Participants |
| Part A:GSK2982772 120 mg TID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | AEs | 6 Participants |
| Part A:GSK2982772 240 mg TID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | AEs | 4 Participants |
| Part A:GSK2982772 240 mg TID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | SAEs | 0 Participants |
| Part A:GSK2982772 360 mg BID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | AEs | 7 Participants |
| Part A:GSK2982772 360 mg BID | Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A | SAEs | 0 Participants |
Secondary
Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day1
Population: Pharmacokinetic population. Pharmacokinetic population consists of participants in the safety population for whom a pharmacokinetic sample were obtained and analyzed.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A | 21.22 Hours*microgram per millilter | Geometric Coefficient of Variation 41.37 |
| Part A:GSK2982772 120 mg TID | Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A | 46.13 Hours*microgram per millilter | Geometric Coefficient of Variation 37.38 |
Secondary
AUC (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours,12 hours on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (0-12) Following BID Dosing of GSK2982772 in Part A | 21.80 Hours*microgram per millilter | Geometric Coefficient of Variation 24.41 |
Secondary
AUC(0-24) Following BID Dosing of GSK2982772: Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20min, 40min, 1hr, 1hr 30min, 2hr, 3hr, 4hr, 6hr, 8hr, 10hr, 12hr, 12hr 20min, 12hr 40min, 13hr, 13hr 30min, 14hr, 15hr, 16hr, 19hr, 22hr, 24hr post dose on Day 1.
Population: Pharmacokinetic population.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC(0-24) Following BID Dosing of GSK2982772: Part A | 54.02 Hours*microgram per millilter | Geometric Coefficient of Variation 36.02 |
Secondary
AUC[0-24] Following TID Dosing of GSK2982772: Part B
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day14
Population: Pharmacokinetic population. Only those participants with data available at the specified timepoints were analyzed.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC[0-24] Following TID Dosing of GSK2982772: Part B | 25.67 Hours*microgram per millilter | Geometric Coefficient of Variation 28.81 |
| Part A:GSK2982772 120 mg TID | AUC[0-24] Following TID Dosing of GSK2982772: Part B | 52.00 Hours*microgram per millilter | Geometric Coefficient of Variation 45.26 |
Secondary
AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B | AUC (0-7) following normal breakfast, Day 9 | 7.743 Hours*micrograms per milliliter | Geometric Coefficient of Variation 31.46 |
| Part A:Placebo | AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B | AUC (0-7) following high fat breakfast, Day 11 | 6.874 Hours*micrograms per milliliter | Geometric Coefficient of Variation 24.64 |
| Part A:GSK2982772 120 mg TID | AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B | AUC (0-7) following normal breakfast, Day 9 | 14.691 Hours*micrograms per milliliter | Geometric Coefficient of Variation 37.63 |
| Part A:GSK2982772 120 mg TID | AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B | AUC (0-7) following high fat breakfast, Day 11 | 15.987 Hours*micrograms per milliliter | Geometric Coefficient of Variation 42.86 |
Secondary
AUC(0-7) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 1 and 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles).
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | AUC(0-7) Following TID Dosing of GSK2982772 in Part B | AUC (0-7), Day 1, n=20, 13 | 6.550 Hour*microgram per millilter | Geometric Coefficient of Variation 37.67 |
| Part A:Placebo | AUC(0-7) Following TID Dosing of GSK2982772 in Part B | AUC (0-7), Day 14, n=10, 9 | 7.485 Hour*microgram per millilter | Geometric Coefficient of Variation 25.53 |
| Part A:GSK2982772 120 mg TID | AUC(0-7) Following TID Dosing of GSK2982772 in Part B | AUC (0-7), Day 1, n=20, 13 | 11.895 Hour*microgram per millilter | Geometric Coefficient of Variation 33.98 |
| Part A:GSK2982772 120 mg TID | AUC(0-7) Following TID Dosing of GSK2982772 in Part B | AUC (0-7), Day 14, n=10, 9 | 14.835 Hour*microgram per millilter | Geometric Coefficient of Variation 45.3 |
Secondary
AUC (0-7) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (0-7) Following TID Dosing of GSK2982772 : Part A | 6.053 Hours*microgram per millilter | Geometric Coefficient of Variation 33.87 |
| Part A:GSK2982772 120 mg TID | AUC (0-7) Following TID Dosing of GSK2982772 : Part A | 11.686 Hours*microgram per millilter | Geometric Coefficient of Variation 33.5 |
Secondary
AUC (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (12-24) Following BID Dosing of GSK2982772 in Part A | 31.69 Hours*microgram per millilter | Geometric Coefficient of Variation 48.02 |
Secondary
AUC (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 minutes, 14 hours 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (14-24) Following TID Dosing of GSK2982772 in Part B | 8.988 Hours*microgram per millilter | Geometric Coefficient of Variation 33.57 |
| Part A:GSK2982772 120 mg TID | AUC (14-24) Following TID Dosing of GSK2982772 in Part B | 19.816 Hours*microgram per millilter | Geometric Coefficient of Variation 55.6 |
Secondary
AUC (14-24) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours ,15 hours 30 minutes, 16, 19, 22 and 24 hours on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (14-24) Following TID Dosing of GSK2982772 : Part A | 7.213 Hours*microgram per millilter | Geometric Coefficient of Variation 48.85 |
| Part A:GSK2982772 120 mg TID | AUC (14-24) Following TID Dosing of GSK2982772 : Part A | 16.300 Hours*microgram per millilter | Geometric Coefficient of Variation 39.72 |
Secondary
AUC (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 and 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (7-14) Following TID Dosing of GSK2982772 in Part B | 9.095 Hours*microgram per millilter | Geometric Coefficient of Variation 30.57 |
| Part A:GSK2982772 120 mg TID | AUC (7-14) Following TID Dosing of GSK2982772 in Part B | 17.372 Hours*microgram per millilter | Geometric Coefficient of Variation 34.96 |
Secondary
AUC (7-14) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | AUC (7-14) Following TID Dosing of GSK2982772 : Part A | 7.829 Hours*microgram per millilter | Geometric Coefficient of Variation 44.25 |
| Part A:GSK2982772 120 mg TID | AUC (7-14) Following TID Dosing of GSK2982772 : Part A | 17.823 Hours*microgram per millilter | Geometric Coefficient of Variation 42.11 |
Secondary
C0 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C0 Following TID Dosing of GSK2982772 in Part B | 0.29926 Microgram per milliliter | Geometric Coefficient of Variation 56.63 |
| Part A:GSK2982772 120 mg TID | C0 Following TID Dosing of GSK2982772 in Part B | 0.57528 Microgram per milliliter | Geometric Coefficient of Variation 136.34 |
Secondary
C12 Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours post-dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C12 Following BID Dosing of GSK2982772 in Part A | 0.3490 Microgram per millilter | Geometric Coefficient of Variation 98.83 |
Secondary
C14 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours post-dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C14 Following TID Dosing of GSK2982772 in Part B | 0.3830 Microgram per milliliter | Geometric Coefficient of Variation 53.04 |
| Part A:GSK2982772 120 mg TID | C14 Following TID Dosing of GSK2982772 in Part B | 0.6912 Microgram per milliliter | Geometric Coefficient of Variation 106.01 |
Secondary
C24 Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C24 Following BID Dosing of GSK2982772 in Part A | 0.36965 Microgram per millililter | Geometric Coefficient of Variation 101.7 |
Secondary
C24 Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C24 Following TID Dosing of GSK2982772 in Part A | 0.34518 Microgram per milliliter | Geometric Coefficient of Variation 82.34 |
| Part A:GSK2982772 120 mg TID | C24 Following TID Dosing of GSK2982772 in Part A | 0.59880 Microgram per milliliter | Geometric Coefficient of Variation 158.88 |
Secondary
C24 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | C24 Following TID Dosing of GSK2982772 in Part B | 0.22712 Microgram per milliliter | Geometric Coefficient of Variation 60.78 |
| Part A:GSK2982772 120 mg TID | C24 Following TID Dosing of GSK2982772 in Part B | 0.33342 Microgram per milliliter | Geometric Coefficient of Variation 180.82 |
Secondary
C7 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours post-dose on Days 1 and 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles).
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | C7 Following TID Dosing of GSK2982772 in Part B | C7, Day 1, n=20, 13 | 0.3345 Microgram per milliliter | Geometric Coefficient of Variation 50.78 |
| Part A:Placebo | C7 Following TID Dosing of GSK2982772 in Part B | C7, Day 14, n=10, 9 | 0.3718 Microgram per milliliter | Geometric Coefficient of Variation 43.85 |
| Part A:GSK2982772 120 mg TID | C7 Following TID Dosing of GSK2982772 in Part B | C7, Day 1, n=20, 13 | 0.6105 Microgram per milliliter | Geometric Coefficient of Variation 57.01 |
| Part A:GSK2982772 120 mg TID | C7 Following TID Dosing of GSK2982772 in Part B | C7, Day 14, n=10, 9 | 0.6885 Microgram per milliliter | Geometric Coefficient of Variation 75.98 |
Secondary
Cmax (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (0-12) Following BID Dosing of GSK2982772 in Part A | 4.967 Microgram per milliliter | Geometric Coefficient of Variation 30.75 |
Secondary
Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Cmax(0-7), following Normal Breakfast, Day 9 | 2.0918 Microgram per milliliter | Geometric Coefficient of Variation 21.74 |
| Part A:Placebo | Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Cmax(0-7), following High Fat Breakfast, Day 11 | 1.8098 Microgram per milliliter | Geometric Coefficient of Variation 29.77 |
| Part A:GSK2982772 120 mg TID | Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Cmax(0-7), following Normal Breakfast, Day 9 | 3.9440 Microgram per milliliter | Geometric Coefficient of Variation 33.82 |
| Part A:GSK2982772 120 mg TID | Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Cmax(0-7), following High Fat Breakfast, Day 11 | 4.1171 Microgram per milliliter | Geometric Coefficient of Variation 58.36 |
Secondary
Cmax (0-7) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles).
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | Cmax (0-7) Following TID Dosing of GSK2982772 in Part B | Cmax (0-7), Day 1, n=20, 13 | 2.0883 Microgram per milliliter | Geometric Coefficient of Variation 37.87 |
| Part A:Placebo | Cmax (0-7) Following TID Dosing of GSK2982772 in Part B | Cmax (0-7), Day 14, n=10, 9 | 2.2239 Microgram per milliliter | Geometric Coefficient of Variation 30.03 |
| Part A:GSK2982772 120 mg TID | Cmax (0-7) Following TID Dosing of GSK2982772 in Part B | Cmax (0-7), Day 1, n=20, 13 | 3.2333 Microgram per milliliter | Geometric Coefficient of Variation 37.04 |
| Part A:GSK2982772 120 mg TID | Cmax (0-7) Following TID Dosing of GSK2982772 in Part B | Cmax (0-7), Day 14, n=10, 9 | 4.3784 Microgram per milliliter | Geometric Coefficient of Variation 45.62 |
Secondary
Cmax (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (12-24) Following BID Dosing of GSK2982772 in Part A | 6.965 Microgram per milliliter | Geometric Coefficient of Variation 61.7 |
Secondary
Cmax (14-24) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 and 15 hours 30 minutes, 16, 19, 22 and 24 hours post dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (14-24) Following TID Dosing of GSK2982772 in Part A | 1.4156 Microgram per milliliter | Geometric Coefficient of Variation 47.03 |
| Part A:GSK2982772 120 mg TID | Cmax (14-24) Following TID Dosing of GSK2982772 in Part A | 3.4812 Microgram per milliliter | Geometric Coefficient of Variation 28.46 |
Secondary
Cmax (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14
Population: Pharmacokinetic population.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (14-24) Following TID Dosing of GSK2982772 in Part B | 1.9205 Microgram per millilter | Geometric Coefficient of Variation 30.82 |
| Part A:GSK2982772 120 mg TID | Cmax (14-24) Following TID Dosing of GSK2982772 in Part B | 4.1607 Microgram per millilter | Geometric Coefficient of Variation 38.79 |
Secondary
Cmax (7-14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours, 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (7-14) Following TID Dosing of GSK2982772 in Part A | 2.148 Microgram per milliliter | Geometric Coefficient of Variation 36.24 |
| Part A:GSK2982772 120 mg TID | Cmax (7-14) Following TID Dosing of GSK2982772 in Part A | 5.007 Microgram per milliliter | Geometric Coefficient of Variation 33.09 |
Secondary
Cmax (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14
Population: Pharmacokinetic population.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Cmax (7-14) Following TID Dosing of GSK2982772 in Part B | 2.505 Microgram per milliliter | Geometric Coefficient of Variation 26.7 |
| Part A:GSK2982772 120 mg TID | Cmax (7-14) Following TID Dosing of GSK2982772 in Part B | 5.435 Microgram per milliliter | Geometric Coefficient of Variation 32.59 |
Secondary
Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A | 1.7672 Microgram per milliliter | Geometric Coefficient of Variation 41.78 |
| Part A:GSK2982772 120 mg TID | Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A | 3.3125 Microgram per milliliter | Geometric Coefficient of Variation 25.88 |
Secondary
Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours post-dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A | 0.4318 Microgram per milliliter | Geometric Coefficient of Variation 86.28 |
| Part A:GSK2982772 120 mg TID | Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A | 0.7487 Microgram per milliliter | Geometric Coefficient of Variation 76.95 |
Secondary
Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours post-dose on Day 1
Population: Pharmacokinetic population
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Part A:Placebo | Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A | 0.3614 Microgram per milliliter | Geometric Coefficient of Variation 84.67 |
| Part A:GSK2982772 120 mg TID | Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A | 0.7723 Microgram per milliliter | Geometric Coefficient of Variation 89.3 |
Secondary
Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B
Blood samples were collected into EDTA tubes and processed to plasma for 4 beta-hydroxycholesterol and cholesterol. Ratio of 4 beta-hydroxycholesterol to cholesterol is presented
Time frame: Pre-dose on Day 1 and 24 hours post first dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Part A:Placebo | Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Day 14, 24 hour; n=1, 10, 9 | 0.000016 Ratio | — |
| Part A:GSK2982772 120 mg TID | Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Day 1, Pre-dose; n=0, 19, 12 | 0.000019 Ratio | Standard Deviation 0.0000064 |
| Part A:GSK2982772 120 mg TID | Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Day 14, 24 hour; n=1, 10, 9 | 0.000021 Ratio | Standard Deviation 0.0000089 |
| Part A:GSK2982772 240 mg TID | Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Day 1, Pre-dose; n=0, 19, 12 | 0.000023 Ratio | Standard Deviation 0.0000099 |
| Part A:GSK2982772 240 mg TID | Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B | Day 14, 24 hour; n=1, 10, 9 | 0.000024 Ratio | Standard Deviation 0.0000065 |
Secondary
Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1
Population: Pharmacokinetic population.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A | 3.008 Hours |
| Part A:GSK2982772 120 mg TID | Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A | 2.043 Hours |
Secondary
Tmax (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1hour, 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1
Population: Pharmacokinetic population.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (0-12) Following BID Dosing of GSK2982772 in Part A | 3.000 Hours |
Secondary
Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Part A:Placebo | Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Tmax(0-7), Day 9 | 3.000 Hours |
| Part A:Placebo | Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Tmax (0-7), Day 11 | 4.000 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Tmax(0-7), Day 9 | 3.000 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B | Tmax (0-7), Day 11 | 3.000 Hours |
Secondary
Tmax (0-7) Following TID Dosing of GSK2982772 Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 hour, 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed (represented by n= X in the category titles).
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Part A:Placebo | Tmax (0-7) Following TID Dosing of GSK2982772 Part B | Tmax (0-7), Day 1, n=20, 13 | 2.000 Hours |
| Part A:Placebo | Tmax (0-7) Following TID Dosing of GSK2982772 Part B | Tmax (0-7), Day 14, n=10, 9 | 1.750 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (0-7) Following TID Dosing of GSK2982772 Part B | Tmax (0-7), Day 1, n=20, 13 | 3.000 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (0-7) Following TID Dosing of GSK2982772 Part B | Tmax (0-7), Day 14, n=10, 9 | 2.003 Hours |
Secondary
Tmax (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 hours, 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1
Population: Pharmacokinetic population.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (12-24) Following BID Dosing of GSK2982772 in Part A | 14.01 Hours |
Secondary
Tmax (14-24) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 1
Population: Pharmacokinetic population.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (14-24) Following TID Dosing of GSK2982772 in Part A | 19.00 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (14-24) Following TID Dosing of GSK2982772 in Part A | 17.02 Hours |
Secondary
Tmax (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14hours, 14 hours 20 and 40 minutes, 15 hours and 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (14-24) Following TID Dosing of GSK2982772 in Part B | 17.02 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (14-24) Following TID Dosing of GSK2982772 in Part B | 18.92 Hours |
Secondary
Tmax (7-14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1
Population: Pharmacokinetic population.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (7-14) Following TID Dosing of GSK2982772 in Part A | 10.000 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (7-14) Following TID Dosing of GSK2982772 in Part A | 9.000 Hours |
Secondary
Tmax (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours and 7 hours 20 and 40 minutes, 8hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 14
Population: Pharmacokinetic population. Only those participants with data available at the specified data points were analyzed.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Part A:Placebo | Tmax (7-14) Following TID Dosing of GSK2982772 in Part B | 9.001 Hours |
| Part A:GSK2982772 120 mg TID | Tmax (7-14) Following TID Dosing of GSK2982772 in Part B | 10.008 Hours |