Disposition of [14C]-Tirzepatide Following Subcutaneous Administration
Research type
Research Study
Full title
Disposition of [14C]-Tirzepatide Following Subcutaneous Administration in Healthy Male Subjects
IRAS ID
274812
Contact name
Firas Almazedi
Contact email
Sponsor organisation
Eli Lilly and Company
Eudract number
2019-003664-44
Clinicaltrials.gov Identifier
20/NE/0003, REC Ref
Duration of Study in the UK
0 years, 3 months, 7 days
Research summary
Tirzepatide is being developed for the treatment of type 2 diabetes mellitus (T2DM) as an adjunct to diet and exercise. In addition, it is being developed as a therapy for the indications of chronic weight management and non-alcoholic steatohepatitis.
Study I8F-MC-GPHX (GPHX) is being conducted to determine the disposition of radioactivity and pharmacokinetics (PK) of tirzepatide (LY3298176) in healthy male subjects following a single subcutaneous(SC)injection of approximately 4.1 mg tirzepatide containing approximately 3.7 MBq [14C]-tirzepatide. The 3.7 MBq dose of the radiotracer will be administered to each subject to facilitate characterization of physiological disposition and metabolism of tirzepatide. The tirzepatide dose is therefore dependent upon the specific activity of the drug substance. At the target drug substance specific activity, the tirzepatide dose will be 4.1 mg. However, based on variability in the drug substance specific activity, the final tirzepatide dose will be approximately 4.1 mg and will be no higher than 5 mg.
No clinically significant safety or tolerability concerns have been identified in subjects to date for tirzepatide up to the highest single dose of 8 mg or multiple weekly doses, when escalated up to 15 mg.
A single subcutaneous (SC) dose of 4.1 mg was selected based on previous Phase 1 clinical study GPGA, where 5 mg doses of tirzepatide were well tolerated by healthy subjects and patients with T2DM.
Up to 8 subjects may be enrolled. It is planned that up to 6 subjects will be dosed initially and 2 additional subjects will be dosed if needed, in order that a minimum of 4 subjects complete the study. For purposes of this study, a subject completes the study when all scheduled procedures have been finished.
REC name
North East - York Research Ethics Committee
REC reference
20/NE/0003
Date of REC Opinion
3 Jul 2020
REC opinion
Further Information Favourable Opinion