Phase 1
Completed N=12
A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants
Healthy
Source: ClinicalTrials.gov NCT05630287 ↗
Enrolled (actual)
12
Serious AEs
0.0%
Results posted
Apr 2025
Primary outcomePrimary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of Selpercatinib in Plasma (Part 1) — 24100 hour*nanogram per milliliter (h*ng/mL)
Summary
The main purpose of this study is to compare the amount of selpercatinib that gets into the blood stream and how long it takes the body to get rid of it and also to assess the pharmacokinetics (PK), metabolism, and routes and extent of elimination of selpercatinib in healthy male participants. The study will last up to 59 days (Part 1) or 46 days (Part 2) including screening and 7-day safety follow-up.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of Selpercatinib in Plasma (Part 1) |
24100 | — |
| PRIMARY PK: AUClast of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
21400; 11400 | — |
| PRIMARY PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma (Part 1) |
24200 | — |
| PRIMARY PK: AUC0-inf of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
26900; 16700 | — |
| PRIMARY PK: Area Under the Concentration-time Curve, From Time 0 to Hour 24 (AUC0-24) of Selpercatinib in Plasma (Part 1) |
17100 | — |
| PRIMARY PK: (AUC0-24) of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
21400; 12600 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma (Part 1) |
1890 | — |
| PRIMARY PK: Cmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
2240; 1260 | — |
| PRIMARY PK: Time to Reach Cmax (Tmax) of Selpercatinib in Plasma (Part 1) |
1.25 | — |
| PRIMARY PK: Tmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
1.50; 1.50 | — |
| PRIMARY PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma (Part 1) |
36.5 | — |
| PRIMARY PK: t½ of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity |
12.2; 10.5 | — |
| PRIMARY PK: Apparent Systemic Clearance (CL/F) of Selpercatinibin Plasma (Part 1) |
6.83 | — |
| PRIMARY PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of Selpercatinib in Plasma (Part 1) |
323 | — |
| PRIMARY PK: Plasma Selpercatinib/Total Radioactivity AUC0-24 Ratio (Part 1) |
0.799 | — |
| PRIMARY PK: Blood/Plasma Total Radioactivity AUC0-24 Ratio (Part 1) |
0.590 | — |
| PRIMARY PK: AUClast of Selpercatinib in Plasma (Part 2) |
20200 | — |
| PRIMARY PK: AUClast of [14C] Selpercatinib in Plasma (Part 2) |
1680 | — |
| PRIMARY PK: AUC0-inf of Selpercatinib in Plasma (Part 2) |
20300 | — |
| PRIMARY PK: AUC0-inf of [14C] Selpercatinib in Plasma (Part 2) |
1720 | — |
| PRIMARY PK: Cmax of Selpercatinib in Plasma (Part 2) |
1550 | — |
| PRIMARY PK: Cmax of [14C] Selpercatinib in Plasma (Part 2) |
201 | — |
| PRIMARY PK: Tmax of Selpercatinib in Plasma (Part 2) |
1.92 | — |
| PRIMARY PK: Tmax of [14C] Selpercatinib in Plasma (Part 2) |
0.167 | — |
| PRIMARY PK: t½ of Selpercatinib in Plasma (Part 2) |
31.5 | — |
| PRIMARY PK: t½ of [14C] Selpercatinib in Plasma (Part 2) |
16.9 | — |
| PRIMARY PK: CL/F of Selpercatinib in Plasma (Part 2) |
7.89 | — |
| PRIMARY PK: Systemic Clearance (CL) of [14C] Selpercatinib in Plasma (Part 2) |
5.70 | — |
| PRIMARY PK: Vz/F of Selpercatinib in Plasma (Part 2) |
307 | — |
| PRIMARY PK: Volume of Distribution During the Terminal Phase (Vz) of [14C] Selpercatinib in Plasma (Part 2) |
127 | — |
| PRIMARY PK: Volume of Distribution at Steady State (Vss) of [14C] Selpercatinib in Plasma (Part 2) |
85.0 | — |
| PRIMARY PK: Absolute Bioavailability (F) of Selpercatinib in Plasma (Part 2) |
0.732 | — |
Eligibility Criteria
Inclusion Criteria
- Body mass index (BMI) ≥ 18.0 and ≤ 32.0 kilograms per meter squared (kg/m²)
- Have normal blood pressure, pulse rate, electrocardiogram (ECG), and blood and urine laboratory test results that are acceptable for the study
- Participants will be surgically sterile for at least 90 days prior to Check in or, when sexually active with female partners of childbearing potential, will agree to use effective contraception methods or abstain from sexual intercourse from the time of first dose through 90 days after study drug administration
Exclusion Criteria
- Participation in any other radiolabeled investigational study drug trial within 12 months prior to Check-in
- Exposure to significant radiation (eg, serial x-ray or computed tomography scans, barium meal, current employment in a job requiring radiation exposure monitoring) within 12 months prior to Check-in
- Use or intention to use any medications/products known strong inducers or inhibitors of Cytochrome P450 3A4 enzymes, including St. John's wort, within 30 days prior to Check-in, unless deemed acceptable by the Investigator (or designee)
Data sourced from ClinicalTrials.gov (NCT05630287). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.