Evaluate the Effect of Vimseltinib on the Pharmacokinetics of a BCRP and OATP1B1 Substrate

A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate the Effect of Vimseltinib on BCRP and OATP1B1 Inhibition in Healthy Male Participants

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT07158398

Enrollment

Registered

2025-09-05

Start date

2025-10-31

Completion date

2025-12-08

Last updated

2026-01-15

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Participants

Brief summary

The main purpose of this study is to determine the effect of Vimseltinib dosing on breast cancer resistance protein (BCRP) and organic-anion-transporting polypeptide 1 B1 (OAT1PB1) activity by using rosuvastatin in healthy male participants. This study will also evaluate the safety and tolerability when vimseltinib is co-administered with rosuvastatin in healthy male participants. This study will last approximately 26 days.

Interventions

DRUGVimseltinib

Administered orally

DRUGRosuvastatin

Administered orally

Study design

Allocation

Intervention model

SEQUENTIAL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

1. Participants are in good general health, as required by the protocol and as determined by Principal Investigator. 2. Body mass index (BMI) from 18 to 32 kilogram per square meter (kg/m\^2). 3. Adequate organ function and blood and urine tests, as required by the protocol and as determined by Principal Investigator.

Exclusion criteria

1. History or presence of clinically significant diseases of the neurological, dermatological, renal, hepatic, gastrointestinal, cardiovascular, or musculoskeletal systems or history or presence of clinically significant psychiatric, immunological, endocrine, or metabolic disease as determined by Principal Investigator. 2. Unwilling or unable to comply with the requirements of the protocol. 3. Determined by Principal Investigator to be unsuitable to participate in the study for any other reason.

Design outcomes

Primary

Measure	Time frame
Pharmacokinetic (PK): Maximum Observed Plasma Drug Concentration (Cmax) of rosuvastatin	Predose up to 72 hours postdose
PK: Area Under the Concentration Versus Time Curve (AUC) of rosuvastatin	Predose up to 72 hours postdose

Secondary

Measure	Time frame
Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)	Baseline through Day 26

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026