A Study of Effect of Food and a Proton Pump Inhibitor on Selpercatinib (LY3527723) in Healthy Participants

An Open-Label, Randomized, Crossover Study to Evaluate the Effect of Food and a Proton Pump Inhibitor on the Single-Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects

The main purpose of this study is to assess the effect of food on how fast selpercatinib gets into the bloodstream and how long it takes the body to remove it after a high-fat meal, and the effect of a change in gastric pH after multiple doses of omeprazole on how fast selpercatinib gets into the bloodstream and how long it takes the body to remove it when administered under fasted and fed conditions in healthy participants. The study will also evaluate the safety and tolerability of selpercatinib in healthy participants. The study will last up to 33 days excluding the screening period.

Study Overview

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

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Arizona
    • Tempe, Arizona, United States, 85283
      • Celerion

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Non-vasectomized, male participants must have agreed to use a condom with spermicide or abstain from sexual intercourse during the study until 6 months after the last dosing. (No restrictions were required for a vasectomized male provided his vasectomy had been performed 4 months or more prior to the first dosing of study drug)
• If male, must have agreed not to donate sperm from the first dosing until 6 months after the last dosing
• Female participants of non-childbearing potential who are agreeable to take birth control measures until study completion
• Body mass index (BMI) ≥ 18.0 and ≤ 32.0 kilograms per meter squared (kg/m²) and had a minimum weight of at least 50 kg at screening
• Have normal blood pressure, pulse rate, electrocardiogram (ECG), and blood and urine laboratory test results that are acceptable for the study

Exclusion Criteria:

• Had a history of gastritis, gastrointestinal tract or hepatic disorder or other clinical condition that might have, in the opinion of the Principal Investigator or designee, and as confirmed by the Sponsor, affected the absorption, distribution, biotransformation, or excretion of LOXO 292 or omeprazole

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

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Treatment Sequence 1: ABCD; Participants received: Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.; Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state. Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723; Drug: Omeprazole; Administered orally
Experimental: Treatment Sequence 2: ABDC; Participants received: Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fasted state.; Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fed state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state. Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723; Drug: Omeprazole; Administered orally
Experimental: Treatment Sequence 3: BACD; Participants received: Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.; Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fasted state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fed state. Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723; Drug: Omeprazole; Administered orally
Experimental: Treatment Sequence 4: BADC; Participants received: Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 1 in fed state.; Single oral dose of 160 mg selpercatinib administered on Day 1 of Period 2 in fasted state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 3 in fed state.; Multiple daily oral doses of 40 mg omeprazole administered on Day 1 to Day 7 along with single oral dose of 160 mg selpercatinib on Day 1 of Period 4 in fasted state. Periods 1 and 2, 2 and 3 were separated by a 7-day washout period. There was no washout between Periods 3 and 4.	Drug: Selpercatinib; Administered orally; Other Names: LOXO-292; LY3527723; Drug: Omeprazole; Administered orally

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib	PK: AUC0-t of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib	PK: AUC0-inf of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib	PK: AUC%extrap of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Maximum Observed Concentration (Cmax) of Selpercatinib	PK: Cmax of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Time to Reach Cmax (Tmax) of Selpercatinib	PK: Tmax of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib	PK: Kel of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib	PK: CL/F of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.
PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib	PK: t½ of Selpercatinib was reported.	Day 1: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 hours post dose in Periods 1, 2, 3, and 4.

Collaborators and Investigators

• Sponsor: Eli Lilly and Company
• Collaborators: Loxo Oncology, Inc.
• 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): May 31, 2018
• Primary Completion (Actual): September 13, 2018
• Study Completion (Actual): September 13, 2018

Study Registration Dates

• First Submitted: July 19, 2022
• First Submitted That Met QC Criteria: July 19, 2022
• First Posted (Actual): July 21, 2022

Study Record Updates

• Last Update Posted (Estimated): September 19, 2025
• Last Update Submitted That Met QC Criteria: August 29, 2025
• Last Verified: August 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Omeprazole; selpercatinib
• Other Study ID Numbers: 17752; J2G-MC-JZJQ (Other Identifier: Eli Lilly and Company); LOXO-RET-18015 (Other Identifier: Loxo Oncology, Inc.)

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