A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants

Lilly

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Selpercatinib; Drug: [14C]-Selpercatinib

Study type: Interventional

Funder types: Industry

Identifiers

NCT05630287

J2G-OX-JZJT (Other Identifier)

LOXO-RET-18016 (Other Identifier)

17768

Details and patient eligibility

About

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.

Enrollment: 12 patients

Sex: Male

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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)

Trial design

Primary purpose: Basic Science

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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12 participants in 2 patient groups

Carbon-14-labelled [14C]-Selpercatinib - Part 1

Experimental group

Description:

Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).

Treatment:

Drug: [14C]-Selpercatinib

Drug: [14C]-Selpercatinib

Selpercatinib and [14C]-Selpercatinib - Part 2

Experimental group

Description:

Participants received a single oral dose of 160 mg Selpercatinib followed by single dose of \<100 µg of \[14C\]-Selpercatinib (containing approximately 1 µCi) administered intravenously (IV).

Treatment:

Drug: [14C]-Selpercatinib

Drug: Selpercatinib

Drug: [14C]-Selpercatinib