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

An Open-Label, Randomized Study to Evaluate the Relative Bioavailability of Selpercatinib in 3 Formulations for Pediatric Use

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Selpercatinib

• Study Type: Interventional
• Enrollment (Actual): 42
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Florida
    • Daytona Beach, Florida, United States, 32117
      • LabCorp CRU, Inc.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 21 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

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)

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Selpercatinib Sequence A: Period 1: 20 milligram (mg) Selpercatinib capsule single oral dose administered orally on Day 1. Period 2: 20 mg per milliliter (mL) Selpercatinib Powder for Oral suspension (PFOS) single oral suspension dose on Day 8. Period 3: 20 mg/mL Selpercatinib Ready to Use (RTU) single oral suspension on Day 15.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723
Experimental: Selpercatinib Sequence B; Period 1: 20 mg/mL Selpercatinib RTU single oral suspension on Day 1. Period 2: 20 mg Selpercatinib capsule single oral dose administered orally on Day 8. Period 3: 20 mg/mL PFOS single oral suspension dose on Day 15.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723
Experimental: Selpercatinib Sequence C; Period 1: 20 mg/mL PFOS single oral suspension dose on Day 1. Period 2: 20 mg/mL Selpercatinib RTU single oral suspension on Day 8. Period 3: 20 mg Selpercatinib capsule single oral dose administered orally on Day 15.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib	PK: Cmax of Selpercatinib	Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours (h) postdose
PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib	PK AUC[0-∞] of Selpercatinib	Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose
PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib	PK: AUC[0-tlast] of Selpercatinib	Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose
PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib	PK: Tmax of Selpercatinib	Days 1, 8, and 15: Predose, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 h postdose

Collaborators and Investigators

• Sponsor: Loxo Oncology, Inc.
• Collaborators: Eli Lilly and Company
• Investigators: Study Director: Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST), Eli Lilly and Company

Study record dates

Study Major Dates

• Study Start (Actual): December 3, 2021
• Primary Completion (Actual): March 14, 2022
• Study Completion (Actual): March 14, 2022

Study Registration Dates

• First Submitted: November 25, 2021
• First Submitted That Met QC Criteria: November 25, 2021
• First Posted (Actual): November 29, 2021

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 27, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Other Study ID Numbers: 17821; J2G-MC-JZJU (Other Identifier: Eli Lilly and Company)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No