A Study of Selpercatinib (LY3527723) in Healthy Participants

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: Selpercatinib

Registration Number: NCT05338515

Lead Sponsor: Eli Lilly and Company

Brief Summary: The main purpose of this study is to determine how safe and how well tolerated selpercatinib is when given as oral doses to healthy participants. The study will also assess how fast selpercatinib gets into the blood stream and how long it takes the body to remove it. The study will last up to about 6 weeks, inclusive of screening period.

Detailed Description: Not available

Recruitment & Eligibility

Status: COMPLETED

Sex: All

Target Recruitment: 18

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Have previously participated or withdrawn from this study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

Study & Design

Study Type: INTERVENTIONAL

Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Selpercatinib Cohort 3	Selpercatinib	Selpercatinib administered orally.
Selpercatinib Cohort 2	Selpercatinib	Selpercatinib administered orally.
Selpercatinib Cohort 1	Selpercatinib	Selpercatinib administered orally.
720 mg Selpercatinib	Selpercatinib	Participants received a single oral dose of 720 mg selpercatinib on Day 1, preceded by an overnight fast of at least 10 hours, followed by a fast from food (not including water) for at least 4 hours post dose.
320 mg Selpercatinib	Selpercatinib	Participants received a single oral dose of 320 mg selpercatinib on Day 1, preceded by an overnight fast of at least 10 hours, followed by a fast from food (not including water) for at least 4 hours post dose.
640 mg Selpercatinib	Selpercatinib	Participants received a single oral dose of 640 mg selpercatinib on Day 1, preceded by an overnight fast of at least 10 hours, followed by a fast from food (not including water) for at least 4 hours post dose.

Primary Outcome Measures

Name	Time	Method
Number of Participants With One or More Serious Adverse Event(s) (SAEs) Considered by the Investigator to be Related to Study Drug Administration	Baseline up to Day 8	Data presented are the number of participants who experienced SAEs considered by the investigator to be related to study drug administration. A summary of SAEs and all other non-serious Adverse Event(s) (AEs), regardless of causality, is located in the Reported Adverse Event module.

Secondary Outcome Measures

Name	Time	Method
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: AUC0-t is calculated using the linear trapezoidal with linear interpolation method.
PK: Area Under the Concentration-time Curve, From Time 0 to Hour 24 (AUC0-24) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 hours postdose	PK: AUC0-24 was calculated using the linear trapezoidal with linear interpolation method.
PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: AUC0-inf was calculated as AUC0-inf = AUC0-t + (Clast/Kel) where Clast is the last observed/measured concentration and Kel is the apparent terminal elimination rate constant, which represents the fraction of drug eliminated per unit time.
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib	Predose -168 hours post dose	PK: Percent of AUC0-inf extrapolated was calculated as (1-AUC0-t/AUC0-inf) \*100.
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: CL/F was calculated as Dose/(AUC0-inf).
PK: Maximum Observed Concentration (Cmax) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: Cmax was taken directly from bioanalytical data.
PK: Time to Reach Cmax (Tmax) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: Tmax was time to reach Cmax. If the maximum value occurs at more than one time point, Tmax is defined as the first time point with this value taken from clinical database as the difference in the time of administration and the time of the blood draw which is associated with the Cmax.
PK: Apparent First-order Terminal Elimination Rate Constant (Kel) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: Apparent terminal elimination rate constant; represents the fraction of drug eliminated per unit time calculated by linear least squares regression analysis using the maximum number of points in the terminal log linear phase (e.g., three or more non zero plasma concentrations).
PK: Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Selpercatinib	Predose (within 30 minutes), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 hours postdose	PK: Vz/F calculated as Dose/(AUC0-inf x Kel).