Clinical trial NCT03375463: A Study of Tirzepatide (LY3298176) in Healthy Participants
Official title: Pharmacokinetics, Safety, and Tolerability of a Solution Formulation of LY3298176 in Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Eli Lilly and Company
Sponsor class: INDUSTRY
First posted: 2017-12-18
Enrollment: 52
Sex: ALL
Minimum age (years): 18
Maximum age (years): 70
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: BASIC_SCIENCE

Brief summary: This study has four parts. Each participant will enroll in one part.

Part A: The purpose of Part A is to compare study drug tirzepatide solution formulation to a powder formulation mixed with water and given subcutaneously (SC) (just under the skin). Part A will measure how much of the study drug gets into the blood stream and how long it takes the body to get rid of it.

Part B: The purpose of Part B is to evaluate the safety and tolerability of tirzepatide intravenous (IV) formulation when administered into a vein.

Part C: The purpose of Part C is to evaluate the safety and tolerability of tirzepatide following multiple SC weekly doses of a solution.

Part D: The purpose of Part D is to evaluate the safety and tolerability of tirzepatide following single IV bolus dose of lyophilized formulation.

This study will last approximately 70 days for each part (Part A, Part B or Part D) and 92 days for Part C. This does not include screening. Screening is required within 28 days prior to the start of the study.


Eligibility criteria: Inclusion Criteria:

* Overtly healthy males or females, as determined by medical history and physical examination
* Male participants: agree to use an effective method of contraception for the duration of the study and for 3 months following the last dose of investigational product
* Female participants: not of childbearing potential due to surgical sterilization (hysterectomy or bilateral oophorectomy or tubal ligation) or menopause. Women with an intact uterus are deemed postmenopausal if they are greater than or equal to (≥)45 years old and have not taken hormones or oral contraceptives within the last year and had cessation of menses for at least 1 year. Or, have had at least 6 months of amenorrhea with follicle-stimulating hormone levels consistent with a postmenopausal state
* Have a body mass index of 18.5 to 32.0 kilograms per meter squared (kg/m²) inclusive

Exclusion Criteria:

* Currently enrolled in a clinical trial involving an investigational product or any other type of medical research judged not to be scientifically or medically compatible with this study
* Received treatment with a drug that has not received regulatory approval for any indication within 30 days of screening
* Have a history of heart block, or a pulse rate (PR) interval greater than (\>)200 milliseconds (msec), or any abnormality in the 12-lead electrocardiogram (ECG) at screening that, in the opinion of the investigator, increases the risks associated with participating in the study
* Have a significant history of or current cardiovascular (myocardial infarction, congestive heart failure, cerebrovascular accident, venous thromboembolism, etc.), respiratory, hepatic, renal, gastrointestinal (GI), endocrine, hematological (including history of thrombocytopenia), or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs, or of constituting a risk when taking the study medication, or interfering with the interpretation of data

Primary outcomes:
measure: Pharmacokinetics (PK) Part A: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
timeFrame: Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480, 816-864 hours postdose
measure: PK Part A: Maximum Observed Drug Concentration (Cmax) of Tirzepatide
timeFrame: Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480 and 816-864 hours postdose
measure: PK Part B: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
timeFrame: Part B: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816h-864h and >=70 days post dose
Secondary outcomes:
measure: PK Part C: Area Under the Concentration Versus Time Curve [AUC (0-τ)] of Tirzepatide
timeFrame: Part C: Predose, 8 hours (h) (day (D)1), 24h (D2), 48h (D3),72h (D4), predose (D8), predose (D15), 8h (D15), 24h (D16), 48h (D17), 72h (D18), predose (D22), 8h (D22), 24h (D23), 48h (D24), 72h (D25), D57 and >= D96 postdose
measure: PK Part C: Maximum Observed Drug Concentration (Cmax) of Tirzepatide
timeFrame: Part C: Predose, 8 hours (h) (day (D)1), 24h (D2), 48h (D3),72h (D4), predose (D8), predose (D15), 8h (D15), 24h (D16), 48h (D17), 72h (D18), predose (D22), 8h (D22), 24h (D23), 48h (D24), 72h (D25), D57 and >= D96 postdose
measure: PK Part D: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide
timeFrame: Part D: Predose, 0.08 hours (h), 0.16h, 0.5h, 1h, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 72h, 96h, 120h, 144h, 168h, 336h, 816-864h and >= 70 days postdose
Other outcomes:
Locations:
city: Dallas
country: United States
facility: Covance
state: Texas
Study officials:
affiliation: Eli Lilly and Company
name: Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST)
role: STUDY_DIRECTOR
References: