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Phase 1 Completed N=20 Randomized Basic Science

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

Healthy
Source: ClinicalTrials.gov NCT05468164 ↗
Enrolled (actual)
20
Serious AEs
0.0%
Results posted
Sep 2025
Primary outcomePrimary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib — 26160; 28400; 7973; 26570 nanogram*hour per milliliter (ng*h/mL)

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.

Outcome Measures

OutcomeResultp-value
PRIMARY
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Observed Non-zero Concentration (AUC0-t) of Selpercatinib
26160; 28400; 7973; 26570
PRIMARY
PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib
26280; 28530; 8256; 26770
PRIMARY
PK: Percent of AUC0-inf Extrapolated (AUC%Extrap) of Selpercatinib
0.4468; 0.4541; 3.065; 0.7158
PRIMARY
PK: Maximum Observed Concentration (Cmax) of Selpercatinib
2024; 1745; 251.5; 1023
PRIMARY
PK: Time to Reach Cmax (Tmax) of Selpercatinib
1.502; 3.997; 2.501; 6.011
PRIMARY
PK: Apparent First Order Terminal Elimination Rate Constant (Kel) of Selpercatinib
0.02445; 0.02282; 0.02207; 0.02214
PRIMARY
PK: Apparent Total Plasma Clearance After Oral (Extravascular) Administration (CL/F) of Selpercatinib
6.585; 5.717; 50.45; 6.031
PRIMARY
PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib
29.801; 31.641; 37.288; 35.841

Eligibility Criteria

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
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05468164). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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