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

NCT05468164 | Completed Phase 1 Results FDA Drug

• 3 other identifiers: 17752J2G-MC-JZJQLOXO-RET-18015
• Study Type: interventional
• Target: 20
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy

Outcome Measures

Primary Outcomes (8)

• 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.

Study Arms (4)

Treatment Sequence 1: ABCD

EXPERIMENTAL

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; Drug: Omeprazole

Treatment Sequence 2: ABDC

EXPERIMENTAL

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; Drug: Omeprazole

Treatment Sequence 3: BACD

EXPERIMENTAL

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; Drug: Omeprazole

Treatment Sequence 4: BADC

EXPERIMENTAL

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; Drug: Omeprazole

Interventions

Selpercatinib DRUG

Administered orally

Also known as: LY3527723, LOXO-292

Treatment Sequence 1: ABCD; Treatment Sequence 2: ABDC; Treatment Sequence 3: BACD; Treatment Sequence 4: BADC

Omeprazole DRUG

Administered orally

Treatment Sequence 1: ABCD; Treatment Sequence 2: ABDC; Treatment Sequence 3: BACD; Treatment Sequence 4: BADC

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Eli Lilly and Company: lead
• Loxo Oncology, Inc.: collaborator

Study Sites (1)

Celerion

Tempe, Arizona, 85283, United States

Location

MeSH Terms

Interventions

selpercatinib; Omeprazole

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

ClinicalTrials.gov@lilly.com

800-545-5979

Study Officials

• 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 DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 19, 2022
• First Posted: July 21, 2022
• Study Start: May 31, 2018
• Primary Completion: September 13, 2018
• Study Completion: September 13, 2018
• Last Updated: September 19, 2025
• Results First Posted: September 19, 2025

Record last verified: 2025-08

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)