Study of Tirzepatide in Healthy Participants

Disposition of [14C]-Tirzepatide Following Subcutaneous Administration in Healthy Male Subjects

The purpose of this study is to look at how much tirzepatide gets into the bloodstream and how long the body takes to get rid of it. This study will involve a single dose of 14C radiolabelled tirzepatide. This means that a radioactive tracer substance, C14, will be incorporated into the study drug to investigate the study drug and its breakdown products and to find out how much of these pass from blood into urine, feces and expired air.

Screening is required within 28 days prior to the start of the study. For each participant, the total duration of the clinical trial will be approximately 15 weeks, including screening.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: 14C Tirzepatide

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • West Yorkshire
    • Leeds, West Yorkshire, United Kingdom, LS2 9LH
      • Covance Clinical Research Ltd

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 30 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Overtly healthy males as determined by medical history, physical examination, and other screening procedures
• Have a body mass index (BMI) between 18.0 to 32.0 kilograms per meter squared (kg/m²), inclusive at screening
• Are willing to be available for the full duration of the study

Exclusion Criteria:

• Have known allergies to tirzepatide or related compounds
• Have a medical condition or medical history that makes participation in the study unsafe or which may interfere in the interpretation of the results of the study
• Have had exposure to significant radiation within 12 months prior to dosing (for example, multiple x-ray or computed tomography [CT] scans, barium meal, being employed in a job requiring radiation exposure monitoring)
• Have participated in any clinical trial involving a radiolabeled substance within the past 12 months

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 14C Tirzepatide; A single dose of [14C]-tirzepatide administered subcutaneously (SC).	Drug: 14C Tirzepatide; Administered SC.; Other Names: LY3298176

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Urinary Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered	Urinary Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered.	Pre-dose and up to 63 days post-dose
Fecal Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered	Fecal Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered.	Pre-dose and up to 63 days post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total Number of Metabolites	Total Number of Metabolites.	Pre-dose and up to 63 days post-dose
Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable)	Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable).	Pre-dose and up to 63 days post-dose
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Tirzepatide	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of tirzepatide.	Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose
PK: Maximum Concentration (Cmax) of Tirzepatide	PK: Maximum Concentration (Cmax) of tirzepatide.	Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity. Total radioactivity is reported as hours*nanogram equivalents per milliliter (h*ng Eq/mL).	Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose
PK: Maximum Concentration (Cmax) of Total Radioactivity	PK: Cmax of total radioactivity in plasma and whole blood. The Cmax of total radioactivity in plasma and whole blood are reported as nanogram equivalents per milliliter (ng Eq/mL).	Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

Collaborators and Investigators

• Sponsor: Eli Lilly and Company

Study record dates

Study Major Dates

• Study Start (Actual): July 28, 2020
• Primary Completion (Actual): October 2, 2020
• Study Completion (Actual): October 2, 2020

Study Registration Dates

• First Submitted: March 16, 2020
• First Submitted That Met QC Criteria: March 16, 2020
• First Posted (Actual): March 17, 2020

Study Record Updates

• Last Update Posted (Actual): March 24, 2023
• Last Update Submitted That Met QC Criteria: June 9, 2022
• Last Verified: June 1, 2022

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Hypoglycemic Agents; Physiological Effects of Drugs; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists; Incretins; Tirzepatide
• Other Study ID Numbers: 17378; I8F-MC-GPHX (Other Identifier: Eli Lilly and Company); 2019-003664-44 (EudraCT Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No