Healthy
Conditions
Brief summary
The purpose of this study is to measure how much of the specially prepared study drug, LY3202626, containing radiolabeled carbon \[¹⁴C\] gets into the blood stream and how long it takes the body to get rid of it. Information about any side effects that may occur will also be collected. Participants will stay at a clinical research unit (CRU). The study will last about 28 days (check in to follow-up) for each participant. This study is for research purposes only and is not intended to treat any medical condition.
Interventions
DRUG[¹⁴C]-LY3202626
Administered as solution by mouth
Sponsors
Eli Lilly and Company
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Are overtly healthy males, as determined by physical examination, clinical laboratory tests, medical history and electrocardiogram (ECG) * Have a body mass index (BMI) of 18.5 to 32.0 kilograms per meter squared (kg/m²) inclusive at screening
Exclusion criteria
* Have participated in a \[¹⁴C\]-study within the last 6 months prior to admission for this study * Regularly use known drugs of abuse and/or show positive findings on urinary drug screening * Have consumed grapefruits or grapefruit-containing products, Seville oranges or Seville orange-containing products, star fruits or star fruit-containing products within 7 days prior to dosing or intend to consume during the study * Have a history of constipation or have had acute constipation within 3 weeks prior to admission * Are currently or have been smokers or users of tobacco or nicotine replacement products within the 3 months prior to admission and/or have positive cotinine at screening or check-in * Exposure to significant diagnostic, therapeutic, or employment-related radiation within 12 months prior to dosing (e.g., serial x-ray or computed tomography scans, barium meal, current employment in a job requiring radiation exposure monitoring)
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Fecal Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered | Predose, 6, 12, 24, 48, 72 Hours At 24 Hour Intervals Until Release Criteria Met | Fecal excretion of radioactivity over time expressed as a percentage of the total radioactive dose administered. |
| Urinary Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered | Predose, 6, 12, 24, 48, 72 Hours At 24 Hour Intervals Until Release Criteria Met | Urinary excretion of radioactivity over time was expressed as a percentage of the total radioactive dose administered |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to the Last Timepoint With a Measurable Concentration (AUC[0-tlast]) | Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met | Plasma radioactivity pharmacokinetics were measured by the area under the concentration-time curve from time zero to the last timepoint with a measurable concentration (AUC\[0-tlast\]). |
| Plasma Radioactivity Pharmacokinetics Maximum Observed Concentration (Cmax) | Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met | Plasma radioactivity pharmacokinetics were measured by the maximum observed concentration (Cmax). |
| Total Number of Metabolites in Excreta (Urine and Feces) That Represent at Least 10% of the Dose of Radioactivity | From Dosing Until Release Criteria Is Met | The total number of metabolites identified in excreta (urine and feces) that represent at least 10% of the dose of radioactivity |
| Total Number of Metabolites Representing at Least 10% of the Total Radioactivity in Plasma | Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24 Hours Postdose | Total number of metabolites were identified in at least 10% of the total radioactivity in plasma. |
| Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to Infinity (AUC[0-∞]) | Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met | Plasma radioactivity pharmacokinetics were measured by the area under the concentration-time curve from time zero to infinity (AUC\[0-∞\]). |
Countries
United States
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| [¹⁴C]-LY3202626 Single oral dose of LY3202626 containing (10 milligrams) 100 micro curies of radioactivity | 6 |
| Total | 6 |
Baseline characteristics
| Characteristic | [¹⁴C]-LY3202626 |
|---|---|
| Age, Continuous | 45.7 years STANDARD_DEVIATION 11.3 |
| Body Mass Index (BMI) | 27.90 Kilogram/Square Meter (kg/m²) STANDARD_DEVIATION 0.3 |
| 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 | 1 Participants |
| Race (NIH/OMB) Black or African American | 2 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 | 3 Participants |
| Region of Enrollment United States | 6 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 6 Participants |
| Weight | 86.40 Kilogram (kg) STANDARD_DEVIATION 6.3 |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 4 / 6 |
| serious Total, serious adverse events | 0 / 6 |
Outcome results
Primary
Fecal Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered
Fecal excretion of radioactivity over time expressed as a percentage of the total radioactive dose administered.
Time frame: Predose, 6, 12, 24, 48, 72 Hours At 24 Hour Intervals Until Release Criteria Met
Population: All participants who received the study drug and have evaluable pharmacokinetics (PK) data.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [¹⁴C]-LY3202626 | Fecal Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered | 31.3 percentage of the total radioactive dose | Standard Deviation 4.24 |
Primary
Urinary Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered
Urinary excretion of radioactivity over time was expressed as a percentage of the total radioactive dose administered
Time frame: Predose, 6, 12, 24, 48, 72 Hours At 24 Hour Intervals Until Release Criteria Met
Population: All participants who received the study drug and have evaluable PK data.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [¹⁴C]-LY3202626 | Urinary Excretion of Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered | 44.2 percentage of the total radioactive dose | Standard Deviation 3.7 |
Secondary
Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to Infinity (AUC[0-∞])
Plasma radioactivity pharmacokinetics were measured by the area under the concentration-time curve from time zero to infinity (AUC\[0-∞\]).
Time frame: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met
Population: All participants who received the study drug and have evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| [¹⁴C]-LY3202626 | Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to Infinity (AUC[0-∞]) | 1120 nanogram*hour/millilter (ng*h/mL) | Geometric Coefficient of Variation 27 |
Secondary
Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to the Last Timepoint With a Measurable Concentration (AUC[0-tlast])
Plasma radioactivity pharmacokinetics were measured by the area under the concentration-time curve from time zero to the last timepoint with a measurable concentration (AUC\[0-tlast\]).
Time frame: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met
Population: All participants who received the study drug and have evaluable PK data.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| [¹⁴C]-LY3202626 | Plasma Radioactivity Pharmacokinetics Area Under the Concentration-time Curve From Time Zero to the Last Timepoint With a Measurable Concentration (AUC[0-tlast]) | 814 ng*h/mL | Standard Deviation 31 |
Secondary
Plasma Radioactivity Pharmacokinetics Maximum Observed Concentration (Cmax)
Plasma radioactivity pharmacokinetics were measured by the maximum observed concentration (Cmax).
Time frame: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 Hours At 24 Hour Intervals Until Release Criteria Met
Population: All participants who received the study drug and have evaluable PK data.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| [¹⁴C]-LY3202626 | Plasma Radioactivity Pharmacokinetics Maximum Observed Concentration (Cmax) | 25.2 nanogram/millilter (ng/mL) | Geometric Coefficient of Variation 16 |
Secondary
Total Number of Metabolites in Excreta (Urine and Feces) That Represent at Least 10% of the Dose of Radioactivity
The total number of metabolites identified in excreta (urine and feces) that represent at least 10% of the dose of radioactivity
Time frame: From Dosing Until Release Criteria Is Met
Population: All participants who received the study drug and had evaluable PK data.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| [¹⁴C]-LY3202626 | Total Number of Metabolites in Excreta (Urine and Feces) That Represent at Least 10% of the Dose of Radioactivity | 2 metabolites |
Secondary
Total Number of Metabolites Representing at Least 10% of the Total Radioactivity in Plasma
Total number of metabolites were identified in at least 10% of the total radioactivity in plasma.
Time frame: Predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24 Hours Postdose
Population: All participants who received the study drug and have evaluable PK data.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| [¹⁴C]-LY3202626 | Total Number of Metabolites Representing at Least 10% of the Total Radioactivity in Plasma | 1 metabolites |