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Completed

NCT Number: NCT05338489

A Study of Effects of Itraconazole and Rifampin on Selpercatinib (LY3527723) in Healthy Participants

The main purpose of this study is to assess the effect of itraconazole and rifampin on how fast selpercatinib gets into the blood stream and how long it takes the body to remove it when administered in healthy participants. Information about safety and tolerability will be collected. The study is conducted in two parts and it will last up to 54 days (part 1) and 59 days (part 2), respectively, inclusive of screening period.

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Key information

Conditions

Healthy

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Celerion

Tempe, Arizona, 85283, United States

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Female participants of non-childbearing potential who are agreeable to take birth control measures until study completion
  • Body mass index (BMI) ≥ 18.0 and ≤ 32.0 kilograms per meter squared (kg/m²) and had a minimum weight of at least 50 kg at screening
  • Have normal blood pressure, pulse rate, electrocardiogram (ECG), and blood and urine laboratory test results that are acceptable for the study

Exclusion criteria

  • Are currently participating in or completed a clinical trial within the last 30 days or any other type of medical research judged to be incompatible with this study
  • Have previously participated or withdrawn from this study
  • Have or used to have health problems or laboratory test results or ECG readings that, in the opinion of the doctor, could make it unsafe to participate, or could interfere with understanding the results of the study
  • Had blood loss of more than 500 milliliters (mL) within the previous 30 days of study screening
  • Require treatment with inducers or inhibitors of cytochrome P450 (CYP) CYP3A within 14 days before the first dose of study drug through the end of Period 2

Treatment and study plan

Selpercatinib

Drug

Administered orally.

Other names: LY3527723, LOXO-292

Itraconazole

Drug

Administered orally.

Rifampin

Drug

Administered orally.

Primary outcomes

  1. Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: AUC0-t of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  2. PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: AUC0-inf of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  3. PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: AUC%extrap of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  4. PK: Maximum Observed Concentration (Cmax) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: Maximum observed concentration (Cmax) of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

  5. PK: Time to Reach Cmax (Tmax) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: Tmax of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  6. PK: Apparent First-order Terminal Elimination Rate Constant (Kel) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: Kel of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  7. PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: CL/F of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  8. PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib

    Time frame: (contd.) Part 2, Period 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose; (Day 10) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    PK: t½ of Selpercatinib was reported.

    Outcome measure timeframe:

    Parts 1 and 2, Period 1: (Day 1) Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose.

    Part 1, Period 2; (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose. (contd.)

  9. Part 2 - PK: Area Under the Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24) of Selpercatinib Post Dose Day 1

    Time frame: Part 2, Periods 1 and 2: (Day 1) pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours post dose.

    PK: AUC0-24 of Selpercatinib in Part 2 was reported.

Sponsors and collaborators

Lead sponsor

Eli Lilly and Company

Industry

Collaborators

  • Loxo Oncology, Inc.

Registry information

Official study title

A 2-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole and Rifampin on the Single-Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects

Important dates

Study start
2018
Primary completion
2018
Study completion
2018
First posted
Apr 21, 2022
Registry last updated
Sep 19, 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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