Healthy
Conditions
Keywords
Healthy,, Abiraterone Acetate,, Bioequivalence.
Brief summary
The purpose of this study is to determine the bioequivalence (equivalence of pharmacokinetic parameters) of 2 abiraterone acetate coated tablet formulations with respect to the current commercial abiraterone acetate uncoated tablet formulation under fasted (without eating or drinking) conditions in healthy male participants.
Detailed description
This is a Phase 1, randomized (study medication assigned to participants by chance), open-label (all people know the identity of the intervention), single-center, single-dose and 3-way Crossover (the same medications provided to all participants but in different sequence) pivotal study to determine the bioequivalence of 2 abiraterone acetate coated tablet formulations with respect to the current commercial abiraterone acetate uncoated tablet formulation. Approximately 102 healthy male participants will participate in this study. Participants will be randomly assigned to 1 of 6 treatment sequences. The study will consist of 3 parts: Screening Phase (within 21 days before the first study drug administration of the first period), an open-label treatment Phase consisting of 3 single-dose treatment periods (45 days) and follow-up Phase (5 to 7 days after the last study procedure). The total study duration for each participant will be from 45 days to a maximum of 61 days. Participants will receive a single oral 1000 milligram (mg) dose of abiraterone acetate under fasted conditions either as Treatment A (current commercial formulation, uncoated), Treatment B (current commercial formulation, coated) or Treatment C (new composition, coated). Bioequivalence will be primarily evaluated by pharmacokinetic parameters. Participants' safety will be monitored throughout the study.
Interventions
DRUGAbiraterone acetate (Treatment A)
Participants will receive a single oral 1000 mg dose of abiraterone acetate as Treatment A (current commercial formulation, 4\*250 mg uncoated tablets) under fasted conditions on Day 1 of period as specified in the protocol.
DRUGAbiraterone acetate (Treatment B)
Participants will receive a single oral 1000 mg dose of abiraterone acetate as Treatment B (current commercial formulation, 4\*250 mg coated tablets) under fasted conditions on Day 1 of period as specified in the protocol.
Sponsors
Janssen Research & Development, LLC
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* If sexually active, participants must always use a condom during the study and for 1 week after last intake of study drug. If sexually active with a pregnant woman or woman of child-bearing potential, participants must agree to abstain from intercourse during the study and for 1 week after last intake of study drug. Participants should not donate sperm during the study and for 1 week after receiving the last dose of study drug * Body mass index (BMI; weight \[kilogram(kg)\]/height\^2 \[meter square (m\^2)\]) between 18.5 and 30.0 kg/m\^2, (inclusive), and body weight not less than 50 kg * Blood pressure (after the participants is supine for 5 minutes) between 90 and 140 millimeter of mercury (mmHg) systolic, inclusive, and no higher than 90 mmHg diastolic at Screening * A 12-lead electrocardiogram (ECG) consistent with normal cardiac conduction and function at Screening as specified in the protocol * Non-smoker, no history of smoking or use of nicotine-containing substances within the previous 2 months, as determined by medical history or participant's verbal report
Exclusion criteria
* History of or current clinically significant medical illness including (but not limited to) cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease, infection, or any other illness that the investigator considers should exclude the participants or that could interfere with the interpretation of the study results * Clinically significant abnormal values for hematology or clinical chemistry at Screening * Presence of sexual dysfunction (abnormal libido, erectile dysfunction, etc.) or any medical condition that would affect sexual function * Use of any prescription or nonprescription medication (including vitamins and herbal supplements), except for acetaminophen, within 14 days before the first dose of the study drug is scheduled through study completion * History of, or a reason to believe a participants has a history of drug or alcohol abuse within the past 5 years
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Plasma Concentration (Cmax) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | The Cmax is the maximum observed plasma concentration of abiraterone acetate. |
| Area Under the Plasma Concentration-Time Curve From Time 0 to Time of the Last Quantifiable Concentration (AUC [0-last]) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | The AUC (0-last) is the area under the plasma abiraterone acetate concentration-time curve from time zero to time of the last quantifiable concentration. |
| Area Under the Plasma Concentration-Time Curve From Time 0 to Infinite Time (AUC [0-infinity]) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | The AUC (0-infinity) is the area under the plasma abiraterone acetate concentration-time curve from time 0 to infinite time, calculated as the sum of AUC (0-last) and C(last)/lambda(z), in which AUC(0-last) is area under the plasma abiraterone acetate concentration-time curve from time zero to time of the last quantifiable concentration, C(last) is the last observed quantifiable concentration and lambda(z) is elimination rate constant. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Rate Constant (Lambda [z]) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | Lambda (z) is the first-order rate constant associated with the terminal portion of the curve, determined as the negative slope of the terminal log-linear phase of the drug concentration-time curve. |
| Time to Reach the Maximum Plasma Concentration (Tmax) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | The Tmax is the time to reach the maximum observed plasma concentration of abiraterone acetate. |
| Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs) | Screening up to follow-up (5 to 7 days after last dose administration) | An adverse event (AE) is any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. A serious adverse event (SAE) is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. |
| Time to Last Quantifiable Plasma Concentration (T [last]) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | Time to last quantifiable plasma concentration of abiraterone acetate will be observed. |
| Percentage of Area Under the Plasma Concentration-Time Curve Extrapolated From Last Measurable Concentration to Infinite Time (%AUC, ext) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | Percentage of area under the plasma abiraterone acetate concentration-time curve extrapolated from last measurable concentration to infinite time (%AUC, ext) is calculated using formula: ((AUC \[0-infinity\] minus- AUC \[0-last)\]/AUC \[0-infinity\])\*100. |
| Elimination Half-Life (t 1/2, Lambda) of abiraterone acetate | Pre-dose; 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose on Day 1 of each period | Elimination half-life (t 1/2, Lambda) is associated with the terminal slope (lambda \[z\]) of the semi logarithmic drug concentration-time curve, calculated as 0.693/lambda(z). |
Countries
United States
Outcome results
None listed