Phase 1
Completed N=24
A Study of Effects of Itraconazole and Rifampin on Selpercatinib (LY3527723) in Healthy Participants
Healthy
Source: ClinicalTrials.gov NCT05338489 ↗
Enrolled (actual)
24
Serious AEs
0.0%
Results posted
Sep 2025
Primary outcomePrimary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib — 22380; 51570; 21070; 14080 nanogram *hour per milliliter (ng*h/mL)
Summary
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib |
22380; 51570; 21070; 14080; 2784 | — |
| PRIMARY PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib |
22490; 52450; 21180; 16310; 2820 | — |
| PRIMARY PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib |
0.3377; 1.531; 0.3405; 12.33; 1.081 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Selpercatinib |
1442; 1880; 1364; 1624; 411.2 | — |
| PRIMARY PK: Time to Reach Cmax (Tmax) of Selpercatinib |
1.502; 1.502; 1.500; 2.003; 1.503 | — |
| PRIMARY PK: Apparent First-order Terminal Elimination Rate Constant (Kel) of Selpercatinib |
0.03428; 0.02493; 0.03567; 0.08861; 0.06487 | — |
| PRIMARY PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib |
7.474; 3.305; 7.758; 10.40; 60.12 | — |
| PRIMARY PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib |
20.617; 28.098; 20.437; 8.117; 12.508 | — |
| PRIMARY Part 2 - PK: Area Under the Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24) of Selpercatinib Post Dose Day 1 |
13240; 14090 | — |
Eligibility Criteria
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
Data sourced from ClinicalTrials.gov (NCT05338489). 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.