NCT04311424

Study of Tirzepatide in Healthy Participants

Completed Phase 1 Results posted Last updated 24 March 2023

What this trial tests

Phase 1 trial testing 14C Tirzepatide in Healthy in 6 participants. Completed in 2 October 2020.

Timeline

28 July 2020

Primary endpoint
2 October 2020

2 October 2020

Quick facts

Lead sponsor	Eli Lilly and Company
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	na
Design	single group
Masking	none
Primary purpose	basic science
Enrollment	6
Start date	28 July 2020
Primary completion	2 October 2020
Estimated completion	2 October 2020
Sites	1 location across United Kingdom

Drugs / interventions tested

• 14C Tirzepatide — full drug profile →

Conditions studied

• Healthy — all drugs for Healthy →

Sponsor

Eli Lilly and Company — full company profile →

Who can join

Adults 30 to 55, male only, with Healthy. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Urinary Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered Primary · Pre-dose and up to 63 days post-dose

Urinary Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered.

Group	Value	95% CI
[14C]-Tirzepatide	49.56	± 2.58

Fecal Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered Primary · 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.

Group	Value	95% CI
[14C]-Tirzepatide	20.46	± 2.05

Total Number of Metabolites Secondary · Pre-dose and up to 63 days post-dose

Total Number of Metabolites.

Plasma

Group	Value	95% CI
[14C]-Tirzepatide	4

Urine

Group	Value	95% CI
[14C]-Tirzepatide	6

Feces

Group	Value	95% CI
[14C]-Tirzepatide	6

Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable) Secondary · Pre-dose and up to 63 days post-dose

Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable).

Group	Value	95% CI
[14C]-Tirzepatide	70.03	± 1.98

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Tirzepatide Secondary · 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 tirzepatide.

Group	Value	95% CI
[14C]-Tirzepatide	96100	± 13

PK: Maximum Concentration (Cmax) of Tirzepatide Secondary · 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.

Group	Value	95% CI
[14C]-Tirzepatide	453	± 29

Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity Secondary · 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. Total radioactivity is reported as hours\*nanogram equivalents per milliliter (h\*ng Eq/mL).

Plasma

Group	Value	95% CI
[14C]-Tirzepatide	87900	± 13

Whole blood

Group	Value	95% CI
[14C]-Tirzepatide	44000	± 11

PK: Maximum Concentration (Cmax) of Total Radioactivity Secondary · Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

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).

Plasma

Group	Value	95% CI
[14C]-Tirzepatide	327	± 16

Whole Blood

Group	Value	95% CI
[14C]-Tirzepatide	173	± 14

Adverse events — posted to ClinicalTrials.gov

Time frame: Up To Day 64. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

[14C]-Tirzepatide

Serious: 0/6 (0%)

Deaths: 0/6

Other adverse events (7 terms — click to expand)

Reaction	System	[14C]-Tirzepatide
Decreased appetite	Metabolism and nutrition disorders	—
Palpitations	Cardiac disorders	—
Nausea	Gastrointestinal disorders	—
Toothache	Gastrointestinal disorders	—
Vomiting	Gastrointestinal disorders	—
Feeling of body temperature change	General disorders	—
Presyncope	Nervous system disorders	—

Data from ClinicalTrials.gov NCT04311424 adverse events section.

Sponsor's own description

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.

Publications & conference data

No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.