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Completed

NCT Number: NCT05630287

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

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.

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Key information

Conditions

Healthy

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

LabCorp CRU, Inc.

Madison, Wisconsin, 53704, United States

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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)

Treatment and study plan

[14C]-Selpercatinib

Drug

Administered as an oral solution

Other names: LY3527723, LOXO-292

Selpercatinib

Drug

Administered orally

Other names: LY3527723, LOXO-292

Primary outcomes

  1. 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)

    Time frame: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUClast of Selpercatinib in plasma

  2. PK: AUClast of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUClast of [14C] Selpercatinib in plasma and whole blood

  3. PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma (Part 1)

    Time frame: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-inf of Selpercatinib in plasma

  4. PK: AUC0-inf of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-inf of [14C] Selpercatinib in plasma and whole blood

  5. PK: Area Under the Concentration-time Curve, From Time 0 to Hour 24 (AUC0-24) of Selpercatinib in Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

    PK: AUC0-24 of Selpercatinib in plasma

  6. PK: (AUC0-24) of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

    PK: AUC0-24 of [14C] Selpercatinib in plasma and whole blood

  7. PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Cmax of Selpercatinib in plasma

  8. PK: Cmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Cmax of [14C] Selpercatinib in plasma and whole blood

  9. PK: Time to Reach Cmax (Tmax) of Selpercatinib in Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Tmax of Selpercatinib in plasma

  10. PK: Tmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Tmax of [14C] Selpercatinib in plasma and whole blood

  11. PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: t½ of Selpercatinib in plasma

  12. PK: t½ of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: t½ of [14C] Selpercatinib in plasma and whole blood

  13. PK: Apparent Systemic Clearance (CL/F) of Selpercatinibin Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: CL/F of Selpercatinib in plasma

  14. PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of Selpercatinib in Plasma (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Vz/F of Selpercatinib in plasma

  15. PK: Plasma Selpercatinib/Total Radioactivity AUC0-24 Ratio (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose

    PK: AUC0-24 of Selpercatinib in plasma/AUC0-24 of total radioactivity in plasma

  16. PK: Blood/Plasma Total Radioactivity AUC0-24 Ratio (Part 1)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

    PK: AUC0-24 of total radioactivity in whole blood/AUC0-24 of total radioactivity in whole blood

  17. PK: AUClast of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUClast of Selpercatinib in plasma

  18. PK: AUClast of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUClast of [14C] Selpercatinib in plasma

  19. PK: AUC0-inf of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-inf of Selpercatinib in plasma

  20. PK: AUC0-inf of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: AUC0-inf of [14C] Selpercatinib in plasma

  21. PK: Cmax of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Cmax of Selpercatinib in plasma

  22. PK: Cmax of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Cmax of [14C] Selpercatinib in plasma

  23. PK: Tmax of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Tmax of Selpercatinib in plasma

  24. PK: Tmax of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Tmax of [14C] Selpercatinib in plasma

  25. PK: t½ of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: t½ of Selpercatinib in plasma

  26. PK: t½ of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: t½ of [14C] Selpercatinib in plasma

  27. PK: CL/F of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: CL/F of Selpercatinib in plasma

  28. PK: Systemic Clearance (CL) of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: CL of [14C] Selpercatinib in plasma

  29. PK: Vz/F of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Vz/F of Selpercatinib in plasma

  30. PK: Volume of Distribution During the Terminal Phase (Vz) of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Pre-dose up to 168 hour post-dose

    PK: Vz of [14C] Selpercatinib in plasma

  31. PK: Volume of Distribution at Steady State (Vss) of [14C] Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    PK: Vss of [14C] Selpercatinib in plasma

  32. PK: Absolute Bioavailability (F) of Selpercatinib in Plasma (Part 2)

    Time frame: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

    Absolute bioavailability was determined by comparing the plasma exposure of LOXO-292 following oral dosing with the plasma exposure of [14C]-LOXO-292 following IV dosing.

Sponsors and collaborators

Lead sponsor

Eli Lilly and Company

Industry

Collaborators

  • Loxo Oncology, Inc.

Registry information

Official study title

A Phase 1, Open-label, Two-part Study to Investigate the Absorption, Metabolism, and Excretion, and the Absolute Bioavailability of [14C]-LOXO-292 in Healthy Male Subjects

Important dates

Study start
2018
Primary completion
2018
Study completion
2018
First posted
Nov 29, 2022
Registry last updated
Apr 23, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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