Trial Outcomes & Findings for Study of Tirzepatide in Healthy Participants (NCT NCT04311424)

Results Overview

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

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Pre-dose and up to 63 days post-dose

Results posted on

2023-03-24

Participant Flow

Participant milestones

Participant milestones
Measure	[14C]-Tirzepatide Participants received single dose of approximately 4.1 milligrams (mg) tirzepatide containing approximately 100 microcurie (μCi) of \[14C\]- tirzepatide administered as a subcutaneous injection.
Overall Study STARTED	6
Overall Study COMPLETED	6
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Study of Tirzepatide in Healthy Participants

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Age, Continuous	41.0 years STANDARD_DEVIATION 10.4 • n=99 Participants
Sex: Female, Male Female	0 Participants n=99 Participants
Sex: Female, Male Male	6 Participants n=99 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants n=99 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	6 Participants n=99 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=99 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=99 Participants
Race (NIH/OMB) Asian	0 Participants n=99 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=99 Participants
Race (NIH/OMB) Black or African American	0 Participants n=99 Participants
Race (NIH/OMB) White	6 Participants n=99 Participants
Race (NIH/OMB) More than one race	0 Participants n=99 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=99 Participants
Region of Enrollment United Kingdom	6 Participants n=99 Participants

PRIMARY outcome

Timeframe: Pre-dose and up to 63 days post-dose

Population: All randomized participants who received at least one dose of study drug.

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

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Urinary Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered	49.56 Percentage of the total radioactive dose Standard Deviation 2.58

PRIMARY outcome

Timeframe: Pre-dose and up to 63 days post-dose

Population: All randomized participants who received at least one dose of study drug.

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

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Fecal Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered	20.46 Percentage of the total radioactive dose Standard Deviation 2.05

SECONDARY outcome

Timeframe: Pre-dose and up to 63 days post-dose

Population: All randomized participants who received at least one dose of study drug.

Total Number of Metabolites.

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Total Number of Metabolites Plasma	4 metabolites
Total Number of Metabolites Urine	6 metabolites
Total Number of Metabolites Feces	6 metabolites

SECONDARY outcome

Timeframe: Pre-dose and up to 63 days post-dose

Population: All randomized participants who received at least one dose of study drug.

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

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable)	70.03 Percentage of the total radioactive dose Standard Deviation 1.98

SECONDARY outcome

Timeframe: Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

Population: All randomized participants who received at least one dose of study drug and had evaluable PK data of tirzepatide.

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

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Tirzepatide	96100 nanogramhour per milliliter (ngh/mL) Geometric Coefficient of Variation 13

SECONDARY outcome

Timeframe: Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

Population: All randomized participants who received at least one dose of study drug and had evaluable PK data of tirzepatide.

PK: Maximum Concentration (Cmax) of tirzepatide.

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
PK: Maximum Concentration (Cmax) of Tirzepatide	453 ng/mL Geometric Coefficient of Variation 29

SECONDARY outcome

Timeframe: Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

Population: All randomized participants who received at least one dose and had evaluable PK data for 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).

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity Plasma	87900 h*ng Eq/mL Geometric Coefficient of Variation 13
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity Whole blood	44000 h*ng Eq/mL Geometric Coefficient of Variation 11

SECONDARY outcome

Timeframe: Pre-dose, Day 1, 2, 3, 4, 5, 6, 7, 10, 12, 14, 22, 29, 36, 43, 50, 57, and 64 post dose

Population: All randomized participants who received at least one dose and had evaluable PK data for 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).

Outcome measures

Outcome measures
Measure	[14C]-Tirzepatide n=6 Participants Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
PK: Maximum Concentration (Cmax) of Total Radioactivity Plasma	327 ng Eq/mL Geometric Coefficient of Variation 16
PK: Maximum Concentration (Cmax) of Total Radioactivity Whole Blood	173 ng Eq/mL Geometric Coefficient of Variation 14

Adverse Events

[14C]-Tirzepatide

Serious events: 0 serious events

Other events: 6 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	[14C]-Tirzepatide n=6 participants at risk Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection.
Cardiac disorders Palpitations	33.3% 2/6 • Number of events 2 • Up To Day 64 All randomized participants
Gastrointestinal disorders Nausea	16.7% 1/6 • Number of events 1 • Up To Day 64 All randomized participants
Gastrointestinal disorders Toothache	16.7% 1/6 • Number of events 1 • Up To Day 64 All randomized participants
Gastrointestinal disorders Vomiting	16.7% 1/6 • Number of events 1 • Up To Day 64 All randomized participants
General disorders Feeling of body temperature change	16.7% 1/6 • Number of events 1 • Up To Day 64 All randomized participants
Metabolism and nutrition disorders Decreased appetite	100.0% 6/6 • Number of events 6 • Up To Day 64 All randomized participants
Nervous system disorders Presyncope	16.7% 1/6 • Number of events 1 • Up To Day 64 All randomized participants

Additional Information

Chief Medical Officer

Eli Lilly and Company

Phone: 800-545-5979

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee
Publication restrictions are in place

Restriction type: GT60