Study to Evaluate the Effect of Repotrectinib on the Drug Levels of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants

NCT07223671 | Completed Phase 1 FDA Drug

• 1 other identifier: CA127-1088
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of the study if to evaluate the effect of Repotrectinib on the drug levels of transporter and CYP P450 probe substrates in healthy adult participants.

Conditions

Healthy Volunteers

Keywords

Drug-Drug Interactions; Pharmacokinetics; Transporter Probe Substrates; CYP P450 Probe Substrates

Outcome Measures

Primary Outcomes (15)

• Cohort 1: Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration of AUC (0-T) of Probe Substrate With Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin.

  Up to approximately Day 17 post dose

• Cohort 1: AUC (0-T) of Probe Substrate Without Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin.

  Up to approximately Day 17 post dose

• Cohort 1: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC(INF)) of Probe Substrate With Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin.

  Up to approximately Day 17 post dose

• Cohort 1: AUC(INF) of Probe Substrate Without Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin.

  Up to approximately Day 17 post dose

• Cohort 1: Maximum Observed Plasma Concentration (Cmax) of Probe Substrate With Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin

  Up to approximately Day 17 post dose

• Cohort 1: Cmax of Probe Substrate Without Repotrectinib

  Probe substrate contains metformin, digoxin, and rosuvastatin

  Up to approximately Day 17 post dose

• Cohort 1: Area Under the Plasma Concentration-time Curve From Time Zero to 48 Hours Post Dose (AUC (0-48)) of Metformin With Repotrectinib

  Up to approximately Day 17 post dose

• Cohort 1: AUC (0-48) of Metformin Without Repotrectinib

  Up to approximately Day 17 post dose

• Cohort 1: Renal Clearance (CLR) of Metformin in Urine

  Up to approximately Day 16 post dose

• Cohort 2: AUC (0-T) of Probe Substrate With Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

• Cohort 2: AUC (0-T) of Probe Substrate Without Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

• Cohort 2: AUC (INF) of Probe Substrate With Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

• Cohort 2: AUC (INF) of Probe Substrate Without Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

• Cohort 2: Cmax of Probe Substrate With Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

• Cohort 2: Cmax of Probe Substrate Without Repotrectinib

  Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

  Up to approximately Day 17 post dose

Secondary Outcomes (6)

• Number of Participants with Adverse Events (AEs)

  Up to approximately Day 45 post dose

• Number of Participants with Serious Adverse Events (SAEs)

  Up to approximately Day 45 post dose

• Number of Participants With Clinically Significant Physical Examination Findings

  Up to approximately Day 17 post dose

• Number of Participants With Clinically Significant Vital Sign Measurements

  Up to approximately Day 17 post dose

• Number of Participants With Clinically Significant 12-lead Electrocardiogram (12-lead ECG) Findings

  Up to approximately Day 17 post dose

Study Arms (2)

Cohort 1

EXPERIMENTAL

Drug: Repotrectinib; Drug: Metformin; Drug: Digoxin; Drug: Rosuvastatin

Cohort 2

EXPERIMENTAL

Drug: Repotrectinib; Drug: Bupropion; Drug: Flurbiprofen; Drug: Omeprazole

Interventions

Metformin DRUG

Specified dose on specified days

Cohort 1

Repotrectinib DRUG

Specified dose on specified days

Cohort 1; Cohort 2

Digoxin DRUG

Specified dose on specified days

Cohort 1

Rosuvastatin DRUG

Specified dose on specified days

Cohort 1

Bupropion DRUG

Specified dose on specified days

Cohort 2

Flurbiprofen DRUG

Specified dose on specified days

Cohort 2

Omeprazole DRUG

Specified dose on specified days

Cohort 2

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants must have a body mass index (BMI) of 18.0 to 32.0 kg/m2 and should be between the ages of 18-60 years inclusive.
• Healthy female (as assigned at birth) participants who are individuals not of childbearing potential (INOCBP) and healthy males with no clinically significant deviation from normal for the following: medical history, physical examination, vital signs, 12-lead ECG, and clinical laboratory assessment results as determined by the investigator.

You may not qualify if:

• Participants must not have a significant history of clinical manifestation of any metabolic, allergic, dermatological, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, psychiatric, neoplastic, or genitourinary abnormalities/diseases as determined by the investigator or designee.

Sponsors & Collaborators

• Bristol-Myers Squibb: lead

Study Sites (1)

Local Institution - 0001

Daytona Beach, Florida, 32117-5116, United States

Location

Related Links

• BMS Clinical Trial Information
• BMS Clinical Trial Patient Recruiting

MeSH Terms

Interventions

repotrectinib; Metformin; Digoxin; Rosuvastatin Calcium; Bupropion; Flurbiprofen; Omeprazole

Intervention Hierarchy (Ancestors)

Biguanides; Guanidines; Amidines; Organic Chemicals; Digitalis Glycosides; Cardenolides; Cardiac Glycosides; Cardanolides; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Glycosides; Carbohydrates; Sulfonamides; Amides; Fluorobenzenes; Hydrocarbons, Fluorinated; Hydrocarbons, Halogenated; Hydrocarbons; Sulfones; Sulfur Compounds; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Propiophenones; Ketones; Propionates; Acids, Acyclic; Carboxylic Acids; Biphenyl Compounds; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Pyridines; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Officials

• Bristol-Myers Squibb

  Bristol-Myers Squibb

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 30, 2025
• First Posted: November 3, 2025
• Study Start: December 31, 2025
• Primary Completion: February 19, 2026
• Study Completion: March 19, 2026
• Last Updated: March 27, 2026

Record last verified: 2026-03

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, CSR
• Time Frame: See Plan Description
• Access Criteria: See Plan Description

Locations

US (1)