Phase 1 Completed N=42 Randomized Basic Science

A Relative Bioavailability Study of Selpercatinib (LY3527723) in Healthy Participants

Healthy

Source: ClinicalTrials.gov NCT05136404 ↗

Enrolled (actual)

Serious AEs

0.0%

Results posted

Mar 2025

Primary outcomePrimary: Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib — 176; 174; 180 nanograms per milliliter (ng/mL)

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 three different formulations in adult healthy participants. 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 59 days including the 28 days of screening period.

Outcome Measures

Outcome	Result	p-value
PRIMARY Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib	176; 174; 180	—
PRIMARY PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib	2540; 2410; 2490	—
PRIMARY PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib	2180; 2160; 2190	—
PRIMARY PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib	1.50; 1.50; 1.50	0.4728

Eligibility Criteria

Inclusion Criteria

Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, and vital signs
Body mass index (BMI) within the range 18.0 to 35.0 kilograms per meter squared (kg/m²)

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)

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Data sourced from ClinicalTrials.gov (NCT05136404). 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.