Healthy Volunteers
Conditions
Brief summary
Evacetrapib (study drug) is an investigational drug being developed with the aim to help people at high risk of heart problems in the future. In this study we will be comparing how much of the study drug gets into the blood stream when it is given as a single dose (in tablet form) compared to an intravenous injection (given directly into a vein via a small needle). The study is expected to last at least 15 days for each participant, not including screening. Screening will occur up to 28 days before the study drug is given.
Interventions
DRUGEvacetrapib Tablet
Oral administration
DRUGEvacetrapib Intravenous
Intravenous administration
Sponsors
Eli Lilly and Company
Study design
Allocation
NA
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
* Are overtly healthy males or females, as determined by medical history and physical examination * Female participants are post menopausal women or women not of child bearing potential due to surgical sterilization (at least 6 weeks after surgical hysterectomy, bilateral oophorectomy, or tubal occlusion) confirmed by medical history, or menopause * Have a body mass index (BMI) of less than 32 kilograms per square meter (kg/m\^2) * Have given written informed consent approved by Eli Lilly and Company and the ethical review board (ERB) governing the site
Exclusion criteria
* Have known allergies to evacetrapib, related compounds or any components of the formulation, intolerance to alcohol containing products, or history of significant allergic disease as determined by the investigator * Have an abnormal blood pressure as determined by the investigator * Have a history or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the study medication; or of interfering with the interpretation of data * Regularly use known drugs of abuse and/or show positive findings on urinary drug screening * Show evidence of human immunodeficiency virus (HIV) infection and/or positive human HIV antibodies * Are women who are pregnant or are lactating * Have used or intend to use over-the-counter or prescription medications (including vitamins/mineral supplements/herbal medicine) 14 days prior to the first dose and during the study. The use of topical medicine, provided there is no evidence of chronic dosing with risk of systemic exposure, and occasional acetaminophen is acceptable * Have donated blood of more than 500 milliliter (mL) within the last 3 months * Are unwilling to comply with the dietary requirements/restrictions during the study: * Consume only the meals provided during the inpatient appointments, * Refrain from eating any food or drinking any beverages containing grapefruit, grapefruit juice, Seville oranges, Seville orange juice, star fruit, pomelo, or commercial apple juice or orange juice for at least 7 days prior to the first dose
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib | Day 1:Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.25, 4.5, 5, 5.5, 6, 6.5, 8, 10, 12, Day 2; 24, 36 Day 3; 48 Day 4; 72 Day 5; 96 Day 6; 120 Day 7; 144 and Day 8; 168 hours post-dose |
Countries
United Kingdom
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Evacetrapib Tablet + Evacetrapib Intravenous Single oral dose of 130 mg evacetrapib tablet + a single IV dose of 175 µg \[¹³C₈\] evacetrapib administered over a 4 hour infusion. | 8 |
| Total | 8 |
Baseline characteristics
| Characteristic | Evacetrapib Tablet + Evacetrapib Intravenous |
|---|---|
| Age, Continuous | 42.9 years STANDARD_DEVIATION 14.1 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 8 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 | 0 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 | 8 Participants |
| Region of Enrollment United Kingdom | 8 Participants |
| Sex: Female, Male Female | 1 Participants |
| Sex: Female, Male Male | 7 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 4 / 8 |
| serious Total, serious adverse events | 0 / 8 |
Outcome results
Primary
Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib
Time frame: Day 1:Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.25, 4.5, 5, 5.5, 6, 6.5, 8, 10, 12, Day 2; 24, 36 Day 3; 48 Day 4; 72 Day 5; 96 Day 6; 120 Day 7; 144 and Day 8; 168 hours post-dose
Population: All participants who received at least one dose of study drug and had evaluable PK data
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Evacetrapib: Tablet | Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib | 111 nanogramxhour/milliliter/mg (ngxh/ml/mg) | Geometric Coefficient of Variation 21 |
| Evacetrapib: Intravenous | Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib | 248 nanogramxhour/milliliter/mg (ngxh/ml/mg) | Geometric Coefficient of Variation 16 |