Healthy
Conditions
Brief summary
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.
Interventions
DRUG14C Tirzepatide
Administered SC.
Sponsors
Eli Lilly and Company
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
30 Years to 55 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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 | Urinary 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 | Fecal Excretion of Tirzepatide Radioactivity Over Time Expressed As A Percentage of the Total Radioactive Dose Administered. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| 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 | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC\[0-∞\]) 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 | PK: Maximum Concentration (Cmax) of tirzepatide. |
| Total Number of Metabolites | Pre-dose and up to 63 days post-dose | Total Number of Metabolites. |
| PK: Maximum Concentration (Cmax) of Total Radioactivity | 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). |
| Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Total Radioactivity | 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). |
| Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable) | Pre-dose and up to 63 days post-dose | Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable). |
Countries
United Kingdom
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| [14C]-Tirzepatide Participants received single dose of approximately 4.1 mg tirzepatide containing approximately 100 μCi of \[14C\]- tirzepatide administered as a subcutaneous injection. | 6 |
| Total | 6 |
Baseline characteristics
| Characteristic | [14C]-Tirzepatide |
|---|---|
| Age, Continuous | 41.0 years STANDARD_DEVIATION 10.4 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 6 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 6 Participants |
| Region of Enrollment United Kingdom | 6 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 6 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | 0 / 6 |
| other Total, other adverse events | 6 / 6 |
| serious Total, serious adverse events | 0 / 6 |
Outcome results
Primary
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.
Time frame: Pre-dose and up to 63 days post-dose
Population: All randomized participants who received at least one dose of study drug.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C]-Tirzepatide | 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 |
Primary
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.
Time frame: Pre-dose and up to 63 days post-dose
Population: All randomized participants who received at least one dose of study drug.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C]-Tirzepatide | 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 |
Secondary
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.
Time frame: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| [14C]-Tirzepatide | Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve (AUC) From Zero To Infinity (AUC[0-∞]) of Tirzepatide | 96100 nanogram*hour per milliliter (ng*h/mL) | Geometric Coefficient of Variation 13 |
Secondary
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).
Time frame: 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.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| [14C]-Tirzepatide | 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 |
| [14C]-Tirzepatide | 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
PK: Maximum Concentration (Cmax) of Tirzepatide
PK: Maximum Concentration (Cmax) of tirzepatide.
Time frame: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| [14C]-Tirzepatide | PK: Maximum Concentration (Cmax) of Tirzepatide | 453 ng/mL | Geometric Coefficient of Variation 29 |
Secondary
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).
Time frame: 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.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| [14C]-Tirzepatide | PK: Maximum Concentration (Cmax) of Total Radioactivity | Plasma | 327 ng Eq/mL | Geometric Coefficient of Variation 16 |
| [14C]-Tirzepatide | PK: Maximum Concentration (Cmax) of Total Radioactivity | Whole Blood | 173 ng Eq/mL | Geometric Coefficient of Variation 14 |
Secondary
Total Number of Metabolites
Total Number of Metabolites.
Time frame: Pre-dose and up to 63 days post-dose
Population: All randomized participants who received at least one dose of study drug.
| Arm | Measure | Group | Value (NUMBER) |
|---|---|---|---|
| [14C]-Tirzepatide | Total Number of Metabolites | Plasma | 4 metabolites |
| [14C]-Tirzepatide | Total Number of Metabolites | Urine | 6 metabolites |
| [14C]-Tirzepatide | Total Number of Metabolites | Feces | 6 metabolites |
Secondary
Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable)
Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable).
Time frame: Pre-dose and up to 63 days post-dose
Population: All randomized participants who received at least one dose of study drug.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [14C]-Tirzepatide | Total Radioactivity Recovered in Urine, Feces, and Expired Air (if Applicable) | 70.03 Percentage of the total radioactive dose | Standard Deviation 1.98 |