Healthy
Conditions
Brief summary
The purpose of this study is to measure how much of the new LY2409021 tablet formulations get into the blood stream and how long it takes the body to get rid of them, compared to the current LY2409021 capsule formulation. In addition, the safety and tolerability of both the new and current formulations will be evaluated. Information about any side effects that may occur will also be collected. The study has two parts. Each participant may enroll in one part only. The study will last up to 8 weeks for each participant. Screening is required prior to the start of the study.
Interventions
DRUGLY2409021
Administered orally
Sponsors
Eli Lilly and Company
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 85 Years
Healthy volunteers
Yes
Inclusion criteria
* Overtly healthy males or surgically sterile or postmenopausal females, as determined by medical history and physical examination * Have a body mass index (BMI) of 18.0 to 32.0 kilogram per square meter (kg/m\^2) * Have clinical laboratory test results within normal reference range for the population or investigator site, or results with acceptable deviations that are judged to be not clinically significant by the investigator
Exclusion criteria
* Have known allergies to LY2409021, related compounds or any components of the formulation, or history of significant atopy * 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 known or ongoing psychiatric disorders
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2409021 | Day 1: Predose, 0.5 Hours (H), 1 H, 4 H, 8 H, 12 H, 24 H, 48 H, 72 H, 96 H, 144 H, 192 H, 264 H, 336 H Postdose in Each Period |
| PK: Maximum Plasma Concentration (Cmax) of LY2409021 | Day 1: Predose, 0.5 H, 1 H, 4 H, 8 H, 12 H, 24 H, 48 H, 72 H, 96 H, 144 H, 192 H, 264 H, 336 H Postdose in Each Period |
Countries
United States
Participant flow
Recruitment details
This study was designed to have two parts. During Part A, decision was made to terminate the study. Participants in Part A were allowed to complete the study. Part B was not conducted.
Participants by arm
| Arm | Count |
|---|---|
| LY2409021 (Part A) 20 mg LY2409021 administered as capsules, T2, or T3 once, orally in each of 3 study periods. | 18 |
| Total | 18 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 | FG003 | FG004 | FG005 |
|---|---|---|---|---|---|---|---|
| Period 2 | Protocol Violation | 0 | 0 | 1 | 0 | 0 | 0 |
Baseline characteristics
| Characteristic | LY2409021 (Part A) |
|---|---|
| Age, Continuous | 44.4 years STANDARD_DEVIATION 13 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 6 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 12 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 | 3 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 | 15 Participants |
| Region of Enrollment United States | 18 Participants |
| Sex: Female, Male Female | 4 Participants |
| Sex: Female, Male Male | 14 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk |
|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — |
| other Total, other adverse events | 4 / 15 | 1 / 17 | 4 / 17 |
| serious Total, serious adverse events | 0 / 15 | 0 / 17 | 0 / 17 |
Outcome results
Primary
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2409021
Time frame: Day 1: Predose, 0.5 Hours (H), 1 H, 4 H, 8 H, 12 H, 24 H, 48 H, 72 H, 96 H, 144 H, 192 H, 264 H, 336 H Postdose in Each Period
Population: All participants who received the LY2409021 formulation and had evaluable AUC(0-inf) values. PK data for 1 participant who met study exclusion criteria was excluded from analyses. This participant only received the capsule formulation.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| LY2409021 Capsules (Part A) | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2409021 | 56400 nanograms x hours/milliliters (ng•h/mL | Geometric Coefficient of Variation 17 |
| LY2409021 T2 (Part A) | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2409021 | 55700 nanograms x hours/milliliters (ng•h/mL | Geometric Coefficient of Variation 24 |
| LY2409021 T3 (Part A) | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-inf]) of LY2409021 | 59100 nanograms x hours/milliliters (ng•h/mL | Geometric Coefficient of Variation 15 |
Primary
PK: Maximum Plasma Concentration (Cmax) of LY2409021
Time frame: Day 1: Predose, 0.5 H, 1 H, 4 H, 8 H, 12 H, 24 H, 48 H, 72 H, 96 H, 144 H, 192 H, 264 H, 336 H Postdose in Each Period
Population: All participants who received the LY2409021 formulation and had evaluable Cmax values. PK data for 1 participant who met study exclusion criteria was excluded from analyses. This participant only received the capsule formulation.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| LY2409021 Capsules (Part A) | PK: Maximum Plasma Concentration (Cmax) of LY2409021 | 724 ng/mL | Geometric Coefficient of Variation 18 |
| LY2409021 T2 (Part A) | PK: Maximum Plasma Concentration (Cmax) of LY2409021 | 718 ng/mL | Geometric Coefficient of Variation 30 |
| LY2409021 T3 (Part A) | PK: Maximum Plasma Concentration (Cmax) of LY2409021 | 760 ng/mL | Geometric Coefficient of Variation 20 |