A Study of Tirzepatide (LY3298176) in Healthy Participants

NCT03375463 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: 16671I8F-MC-GPGE
• Study Type: interventional
• Target: 52
• Locations: 1 country
• Sites: 1

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.

Conditions

Healthy

Outcome Measures

Primary Outcomes (3)

• Pharmacokinetics (PK) Part A: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

  Pharmacokinetics (PK) Part A: Area under the concentration versus time curve \[AUC (0-∞)\] of tirzepatide.

  Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480, 816-864 hours postdose

• PK Part A: Maximum Observed Drug Concentration (Cmax) of Tirzepatide

  PK Part A: Maximum observed plasma drug concentration (Cmax) of tirzepatide.

  Part A: Predose, 8, 12, 24, 48, 72, 96, 120, 144, 168, 336, 480 and 816-864 hours postdose

• PK Part B: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

  PK Part B: Area under the concentration versus time curve \[AUC (0-∞)\] of tirzepatide.

  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 (3)

• PK Part C: Area Under the Concentration Versus Time Curve [AUC (0-τ)] of Tirzepatide

  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

• PK Part C: Maximum Observed Drug Concentration (Cmax) of Tirzepatide

  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

• PK Part D: Area Under the Concentration Versus Time Curve [AUC (0-∞)] of Tirzepatide

  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

Study Arms (6)

5 mg Tirzepatide SC (Solution)-Part A

EXPERIMENTAL

Participants received 5 milligrams (mg) of tirzepatide subcutaneous (SC) solution formulation.

Drug: Tirzepatide

5 mg Tirzepatide SC (Lyophilized)-Part A

EXPERIMENTAL

Participants received 5 mg of tirzepatide SC lyophilized formulation.

Drug: Tirzepatide

0.5 mg LY3298176 IV-Part B

EXPERIMENTAL

Participants received Intravenous (IV) infusion of a single 0.5 mg dose of tirzepatide formulation.

Drug: Tirzepatide

5 mg/7.5 mg/ 10 mg Tirzepatide SC-Part C

EXPERIMENTAL

Participants received tirzepatide subcutaneous solution at 5 mg on Days 1 (week 1) and 8 (Week 2), 7.5 mg on Day 15 (Week 3) and 10 mg on Day 22 (Week 4).

Drug: Tirzepatide

Placebo SC-Part C

PLACEBO COMPARATOR

Participants received SC injection of placebo.

Drug: Placebo

0.5 mg LY3298176 Bolus IV-Part D

EXPERIMENTAL

Participants received IV bolus of 0.5 mg tirzepatide lyophilized formulation.

Drug: Tirzepatide

Interventions

Tirzepatide DRUG

Administered SC

Also known as: LY3298176

5 mg Tirzepatide SC (Lyophilized)-Part A; 5 mg Tirzepatide SC (Solution)-Part A; 5 mg/7.5 mg/ 10 mg Tirzepatide SC-Part C

Placebo DRUG

Administered SC

Placebo SC-Part C

Eligibility Criteria

• Age: 18 Years - 70 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Eli Lilly and Company: lead

Study Sites (1)

Covance

Dallas, Texas, 75247, United States

Location

MeSH Terms

Interventions

Tirzepatide

Intervention Hierarchy (Ancestors)

Glucagon-Like Peptide-1 Receptor; Glucagon-Like Peptide Receptors; Receptors, G-Protein-Coupled; Receptors, Cell Surface; Membrane Proteins; Proteins; Amino Acids, Peptides, and Proteins; Receptors, Gastrointestinal Hormone; Receptors, Peptide

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

ClinicalTrials.gov@lilly.com

800-545-5979

Study Officials

• 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)

  Eli Lilly and Company

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Part A, B and D are not blinded. Part C is blinded to Participant and Investigator
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 13, 2017
• First Posted: December 18, 2017
• Study Start: December 19, 2017
• Primary Completion: December 27, 2018
• Study Completion: December 27, 2018
• Last Updated: February 5, 2024
• Results First Posted: February 5, 2024

Record last verified: 2024-02

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)