NCT05136404

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

Completed Phase 1 Results posted Last updated 17 March 2025

What this trial tests

Phase 1 trial testing Selpercatinib in Healthy in 42 participants. Completed in 14 March 2022.

Timeline

3 December 2021

Primary endpoint
14 March 2022

14 March 2022

Quick facts

Lead sponsor	Loxo Oncology, Inc.
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	none
Primary purpose	basic science
Enrollment	42
Start date	3 December 2021
Primary completion	14 March 2022
Estimated completion	14 March 2022
Sites	1 location across United States

Drugs / interventions tested

• Selpercatinib (SELPERCATINIB) — full drug profile →

Conditions studied

• Healthy — all drugs for Healthy →

Sponsor

Loxo Oncology, Inc. — full company profile →

Who can join

21 and older, any sex, with Healthy. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Pharmacokinetics (PK): Maximum Concentration (Cmax) of Selpercatinib Primary · 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: Cmax of Selpercatinib

Group	Value	95% CI
20 mg Selpercatinib Capsule (Reference)	176	± 64.2
20 mg Selpercatinib RTU Suspension (Test)	174	± 36.9
20 mg/mL PFOS (Test)	180	± 39.8

PK: Area Under the Plasma Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Selpercatinib Primary · 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 AUC\[0-∞\] of Selpercatinib

Group	Value	95% CI
20 mg Selpercatinib Capsule (Reference)	2540	± 28.0
20 mg Selpercatinib RTU Suspension (Test)	2410	± 29.0
20 mg/mL PFOS (Test)	2490	± 27.0

PK: Area Under the Plasma Concentration Versus Time Curve From Time Zero to the Last Measured Concentration Value (AUC[0-tlast]) of Selpercatinib Primary · 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: AUC\[0-tlast\] of Selpercatinib

Group	Value	95% CI
20 mg Selpercatinib Capsule (Reference)	2180	± 36.9
20 mg Selpercatinib RTU Suspension (Test)	2160	± 31.6
20 mg/mL PFOS (Test)	2190	± 30.8

PK: Time to Maximum Observed Concentration (Tmax) of Selpercatinib Primary · 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: Tmax of Selpercatinib

Group	Value	95% CI
20 mg Selpercatinib Capsule (Reference)	1.50	1.00 – 24.02
20 mg Selpercatinib RTU Suspension (Test)	1.50	1.00 – 3.00
20 mg/mL PFOS (Test)	1.50	1.00 – 3.50

Sponsor's own description

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.

Publications & conference data

No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.