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

Loxo Oncology

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Selpercatinib

Study type: Interventional

Funder types: Industry

Identifiers

NCT05136404

17821

J2G-MC-JZJU (Other Identifier)

Details and patient eligibility

About

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.

Enrollment: 42 patients

Sex: All

Ages: 21+ years old

Volunteers: Accepts Healthy Volunteers

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)

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

---

42 participants in 3 patient groups

Selpercatinib Sequence A:

Experimental group

Description:

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.

Treatment:

Drug: Selpercatinib

Selpercatinib Sequence B

Experimental group

Description:

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.

Treatment:

Drug: Selpercatinib

Selpercatinib Sequence C

Experimental group

Description:

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.

Treatment:

Drug: Selpercatinib