A Study Comparing Two Formulations of Selpercatinib (LY3527723) in Healthy Participants

Phase 1

Completed

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, when given as different formulations. The information about any adverse effects experienced will be collected and the tolerability of selpercatinib will also be evaluated. The study may last up to 56 days including the 28 days of screening period.

Recruitment & Eligibility

Inclusion Criteria

Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, and vital signs.
Participants who have clinical laboratory test results within the normal reference range for the population or investigative site, or results with acceptable deviations that are judged to be not clinically significant by the investigator.

Exclusion Criteria

Have a history of allergic reactions to medications or food products
Have a clinically significant abnormality of blood pressure and/or pulse rate as determined by the investigator
Clinically significant abnormalities on ECG as determined by the investigator or prolongation of the QTcB or QTcF >450 msec at screening
Have clinically significant active cardiovascular disease or history of myocardial infarction within 6 months prior to the planned start of selpercatinib
Have a history or presence of cardiovascular, respiratory, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the investigational product; or of interfering with the interpretation of data. Appendectomy, splenectomy, and cholecystectomy are considered as acceptable
Use of H2 blockers, proton pump inhibitors, and other drugs that affect selpercatinib exposure within 7 days of screening
Are intending to use over-the-counter or prescription medication, including dietary supplements, within 14 days prior to dosing and until study discharge (apart from occasional acetaminophen (≤2 g/24 hours), hormonal contraception, or hormone replacement therapy)

Arm && Interventions

Group	Intervention	Description
Selpercatinib (Test)	Selpercatinib	160 mg Selpercatinib (tablet formulation) given orally on days 1 and 15.
Selpercatinib (Reference)	Selpercatinib	160 mg Selpercatinib (2 X 80 mg capsule formulation) given orally on days 1 and 15.

Primary Outcome Measures

Name	Time	Method
Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib	Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;	PK: Cmax of Selpercatinib
PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib	Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;	PK: AUC\[0-∞\] of Selpercatinib.
Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib	Day 1 and Day 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 192, 240, and 312 hours (h) postdose;	PK: AUC\[0-tlast\] of Selpercatinib

Secondary Outcome Measures

Name	Time	Method

Locations (3): LabCorp CRU, Inc.
🇺🇸
Madison, Wisconsin, United States
Covance Dallas
🇺🇸
Dallas, Texas, United States
Anaheim Clinical Trials, LLC
🇺🇸
Anaheim, California, United States