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

Sponsor
Eli Lilly and Company (Industry)
Overall Status
Completed
CT.gov ID
NCT05630287
Collaborator
Loxo Oncology, Inc. (Industry)
12
Enrollment
1
Location
2
Arms
1.8
Actual Duration (Months)
6.8
Patients Per Site Per Month

Study Details

Study Description

Brief 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.

Condition or Disease Intervention/Treatment Phase
Phase 1

Study Design

Study Type:
Interventional
Actual Enrollment :
12 participants
Allocation:
Non-Randomized
Intervention Model:
Parallel Assignment
Masking:
None (Open Label)
Primary Purpose:
Basic Science
Official 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
Actual Study Start Date :
Aug 1, 2018
Actual Primary Completion Date :
Sep 24, 2018
Actual Study Completion Date :
Sep 24, 2018

Arms and Interventions

Arm Intervention/Treatment
Experimental: [14C] Selpercatinib - Part 1

[14C] Selpercatinib administered as an oral solution

Drug: [14C] Selpercatinib
Administered as an oral solution
Other Names:
  • LY3527723
  • LOXO-292

    		•
    Experimental: Selpercatinib and [14C] Selpercatinib - Part 2

    Single oral dose of Selpercatinib followed 2 hours later by single dose of [14C] Selpercatinib administered as an intravenous (IV) push.

    Drug: Selpercatinib
    Administered orally
    Other Names:
  • LY3527723
  • LOXO-292

    • Drug: [14C] Selpercatinib
    Administered intravenously
    Other Names:
  • LY3527723
  • LOXO-292

    		•

    Outcome Measures

    Primary Outcome Measures

    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) [Pre-dose up to 168 hour post-dose]

      PK: AUClast of Selpercatinib in plasma

    2. PK: AUClast of [14C] Selpercatinib in plasma and whole blood (Part 1) for Total Radioactivity [Pre-dose up to 168 hour post-dose]

      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) [Pre-dose up to 168 hour post-dose]

      PK: AUC0-inf of Selpercatinib in plasma

    4. PK: AUC0-inf of [14C] Selpercatinib in plasma and whole blood (Part 1) for Total Radioactivity [Pre-dose up to 168 hour post-dose]

      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) [Pre-dose up to 168 hour 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 [Pre-dose up to 168 hour 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) [Pre-dose up to 168 hour post-dose]

      PK: Cmax of Selpercatinib in plasma

    8. PK: Cmax of [14C] Selpercatinib in plasma and whole blood (Part 1) for Total Radioactivity [Pre-dose up to 168 hour post-dose]

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

    9. PK: Time to reach Cmax (Tmax) of Selpercatinib in plasma (Part 1) [Pre-dose up to 168 hour post-dose]

      PK: Tmax of Selpercatinib in plasma

    10. PK: Tmax of [14C] Selpercatinib in plasma and whole blood (Part 1) for Total Radioactivity [Pre-dose up to 168 hour post-dose]

      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) [Pre-dose up to 168 hour post-dose]

      PK: t½ of Selpercatinib in plasma

    12. PK: t½ of [14C] Selpercatinib in plasma and whole blood (Part 1) for Total Radioactivity [Pre-dose up to 168 hour post-dose]

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

    13. PK: Apparent systemic clearance (CL/F) of Selpercatinibin plasma (Part 1) [Pre-dose up to 168 hour post-dose]

      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) [Pre-dose up to 168 hour post-dose]

      PK: Vz/F of Selpercatinib in plasma

    15. PK: Plasma Selpercatinib/Total Radioactivity AUC0-24 Ratio (Part 1) [Pre-dose up to 168 hour post-dose]

      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) [Pre-dose up to 168 hour post-dose]

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

    17. PK: AUClast of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: AUClast of Selpercatinib in plasma

    18. PK: AUClast of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: AUClast of [14C] Selpercatinib in plasma

    19. PK: AUC0-inf of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: AUC0-inf of Selpercatinib in plasma

    20. PK: AUC0-inf of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

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

    21. PK: Cmax of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: Cmax of Selpercatinib in plasma

    22. PK: Cmax of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: Cmax of [14C] Selpercatinib in plasma

    23. PK: Tmax of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: Tmax of Selpercatinib in plasma

    24. PK: Tmax of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: Tmax of [14C] Selpercatinib in plasma

    25. PK: t½ of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: t½ of Selpercatinib in plasma

    26. PK: t½ of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: t½ of [14C] Selpercatinib in plasma

    27. PK: CL/F of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: CL/F of Selpercatinib in plasma

    28. PK: Systemic clearance (CL) of [14C] Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: CL of [14C] Selpercatinib in plasma

    29. PK: Vz/F of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: Vz/F of Selpercatinib in plasma

    30. PK: Volume of distribution during the terminal phase (Vz) of [14C] Selpercatinib in plasma (Part 2) [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) [Pre-dose up to 168 hour post-dose]

      PK: Vss of [14C] Selpercatinib in plasma

    32. PK: Absolute bioavailability (F) of Selpercatinib in plasma (Part 2) [Pre-dose up to 168 hour post-dose]

      PK: F of Selpercatinib in plasma

    Eligibility Criteria

    Criteria

    Ages Eligible for Study:
    18 Years to 55 Years
    Sexes Eligible for Study:
    Male
    Accepts Healthy Volunteers:
    Yes
    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)

    Contacts and Locations

    Locations

    Site City State Country Postal Code
    1 LabCorp CRU, Inc. Madison Wisconsin United States 53704

    Sponsors and Collaborators

    • Eli Lilly and Company
    • Loxo Oncology, Inc.

    Investigators

    • Study Director: Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST), Eli Lilly and Company

    Study Documents (Full-Text)

    None provided.

    More Information

    Publications

    None provided.
    Responsible Party:
    Eli Lilly and Company
    ClinicalTrials.gov Identifier:
    NCT05630287
    Other Study ID Numbers:
    • 17768
    • J2G-OX-JZJT
    • LOXO-RET-18016
    First Posted:
    Nov 29, 2022
    Last Update Posted:
    Nov 29, 2022
    Last Verified:
    Nov 1, 2022
    Individual Participant Data (IPD) Sharing Statement:
    No
    Plan to Share IPD:
    No
    Studies a U.S. FDA-regulated Drug Product:
    Yes
    Studies a U.S. FDA-regulated Device Product:
    No

    Study Results

    No Results Posted as of Nov 29, 2022