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

NCT07223671 — Phase 1, Completed, 30 participants, Bristol-Myers Squibb

ClinicalTrials Daily  ·  Areas  ·  Conditions  ·  Drugs  ·  Sponsors  ·  

Phase 1, 2-Cohort, Open-label, Fixed-sequence, Drug-drug Interaction Study to Evaluate the Effect of Repotrectinib on the Pharmacokinetics of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants

RegistryNCT07223671
StatusCompleted
PhasePhase 1
Study typeInterventional; non randomized, parallel, masking: none, treatment
Enrollment30 (Actual)
SponsorBristol-Myers Squibb (Industry)
ConditionsHealthy Volunteers
InterventionsRepotrectinib, Metformin, Digoxin, Rosuvastatin, Bupropion, Flurbiprofen, Omeprazole (Drug)
Datesstart 2025-12-31, primary completion 2026-02-19, completion 2026-03-19, first posted 2025-11-03, last updated 2026-03-27
Locations1 site in United States

Related Papers Related Patents Related Grants Related Experts
All trials for Healthy Volunteers All trials of Repotrectinib All trials of Metformin

-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.

Expand all sections  ·  Collapse all

+Arms and interventions

ArmTypeInterventionsDescription
Cohort 1ExperimentalDrug: Repotrectinib; Drug: Metformin; Drug: Digoxin; Drug: Rosuvastatin
Cohort 2ExperimentalDrug: Repotrectinib; Drug: Bupropion; Drug: Flurbiprofen; Drug: Omeprazole
  • Repotrectinib (Drug): Specified dose on specified days
  • Metformin (Drug): Specified dose on specified days
  • Digoxin (Drug): Specified dose on specified days
  • Rosuvastatin (Drug): Specified dose on specified days
  • Bupropion (Drug): Specified dose on specified days
  • Flurbiprofen (Drug): Specified dose on specified days
  • Omeprazole (Drug): Specified dose on specified days

+Outcome measures

Primary outcomes

  • 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 [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin.
  • Cohort 1: AUC (0-T) of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin.
  • Cohort 1: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC(INF)) of Probe Substrate With Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin.
  • Cohort 1: AUC(INF) of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin.
  • Cohort 1: Maximum Observed Plasma Concentration (Cmax) of Probe Substrate With Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin
  • Cohort 1: Cmax of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains metformin, digoxin, and rosuvastatin
  • 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 [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)
  • Cohort 2: AUC (0-T) of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)
  • Cohort 2: AUC (INF) of Probe Substrate With Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)
  • Cohort 2: AUC (INF) of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)
  • Cohort 2: Cmax of Probe Substrate With Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)
  • Cohort 2: Cmax of Probe Substrate Without Repotrectinib [Up to approximately Day 17 post dose]: Probe substrate contains bupropion, hydroxybupropion, flurbiprofen, 4'-hydroxyflurbiprofen, omeprazole, 5'- hydroxyomeprazole)

Secondary outcomes

  • 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]
  • Number of Participants With Clinically Significant Safety Laboratory Test Results [Up to approximately Day 17 post dose]

+Eligibility

Sex: All, ages: 18 Years to 60 Years, accepts healthy volunteers

Inclusion Criteria

* 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.

Exclusion Criteria

* 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.
* Other protocol-defined Inclusion/Exclusion criteria apply.

+Locations (1)

FacilityCityCountryStatus
Local Institution - 0001Daytona Beach, FloridaUnited States

+Investigators

  • Bristol-Myers Squibb, Study director, Bristol-Myers Squibb