Healthy Volunteers
Conditions
Brief summary
The aim of this study is to compare how much of the study drug gets into the blood stream when it is given as a single oral dose and as an intravenous infusion (given directly into a vein via a small needle). The study will also provide information on how well the study drug is tolerated when given as a capsule in combination with giving it intravenously, and information on any changes in heart function. The study will last about 10 days. Screening is required within 28 days before study drug is given.
Interventions
DRUGLY2835219
Administered orally
DRUG¹³C₈-LY2835219
Administered IV
Sponsors
Eli Lilly and Company
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Overtly healthy sterile males or surgically sterile females or postmenopausal females * Have a body mass index (BMI) of 18 to 32 kilogram per meter square (kg/m\^2) * Have given written informed consent approved by Lilly and the ethical review board (ERB) governing the site. * Participants who are reliable and willing to make themselves available for the duration of the study and are willing to follow study procedures
Exclusion criteria
* Have participated in a clinical trial involving investigational product within the last 90 days * Have an abnormality in the 12-lead electrocardiogram (ECG) that, in the opinion of the investigator, increases the risks associated with participating in the study * Have an abnormal blood pressure * Show evidence of human immunodeficiency virus (HIV), hepatitis B or hepatitis C * Have donated blood of more than 500 milliliters (mL) within the last month * Have consumed any sensitive CYP2B6 substrate drugs, any CYP3A4 inhibitor or any CYP3A inducer, herbal supplements, grapefruits or grapefruit containing products, Seville oranges or Seville orange containing products, star fruits or star fruit containing products within 2 weeks prior to dosing or intend to consume during the study * Regularly use known drugs of abuse and/or show positive findings on urinary drug screening
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-∞)] of LY2835219 and ¹³C₈-LY2835219 | Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose |
Secondary
| Measure | Time frame |
|---|---|
| PK: Maximum Observed Concentration (Cmax) of LY2835219 | Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose |
| PK: Time of Maximum Observed Drug Concentration (Tmax) of LY2835219 | Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose |
Countries
United Kingdom
Participant flow
Pre-assignment details
This is a single arm study. Participants first received 200 mg LY2835219 and then 0.4 mg ¹³C₈-LY2835219 given 6 hours later.
Participants by arm
| Arm | Count |
|---|---|
| All Participants 200 mg LY2835219 administered orally on day 1. 0.4 mg ¹³C₈-LY2835219 given intravenously (IV) for 15 minutes, starting approximately 6 hours after the oral dose on day 1. | 11 |
| Total | 11 |
Baseline characteristics
| Characteristic | All Participants |
|---|---|
| Age, Continuous | 56.00 years STANDARD_DEVIATION 8 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 11 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 1 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 10 Participants |
| Region of Enrollment United Kingdom | 11 Participants |
| Sex: Female, Male Female | 3 Participants |
| Sex: Female, Male Male | 8 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — |
| other Total, other adverse events | 3 / 11 | 5 / 11 |
| serious Total, serious adverse events | 0 / 11 | 0 / 11 |
Outcome results
Primary
Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-∞)] of LY2835219 and ¹³C₈-LY2835219
Time frame: Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK data
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg LY2835219 | Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-∞)] of LY2835219 and ¹³C₈-LY2835219 | 3730 nanogram*h/milliliter (ng∙h/mL) | Geometric Coefficient of Variation 31 |
| 200 mg LY2835219 + 0.4 mg ¹³C₈-LY2835219 | Pharmacokinetics (PK): Area Under the Concentration-Time Curve From Zero to Infinity [AUC(0-∞)] of LY2835219 and ¹³C₈-LY2835219 | 15.4 nanogram*h/milliliter (ng∙h/mL) | Geometric Coefficient of Variation 28 |
90% CI: [0.395, 0.508]
Secondary
PK: Maximum Observed Concentration (Cmax) of LY2835219
Time frame: Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg LY2835219 | PK: Maximum Observed Concentration (Cmax) of LY2835219 | 114 nanogram per milliliter (ng/mL) | Geometric Coefficient of Variation 32 |
Secondary
PK: Time of Maximum Observed Drug Concentration (Tmax) of LY2835219
Time frame: Predose, 2, 4, 6, 6.25, 6.5, 6.75, 7.25, 8.25,10, 12, 14, 24, 48, 72, 96,120, 144, 168,192 Hours Postdose
Population: All participants who received at least 1 dose of study drug and had evaluable PK data
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 200 mg LY2835219 | PK: Time of Maximum Observed Drug Concentration (Tmax) of LY2835219 | 6.63 hours |