A Study to Assess the Effect of Oral Belumosudil on Inhibition of Various Proteins in the Fed State in Healthy Male Subjects

NCT05806567 | Completed Phase 1 FDA Drug

• 2 other identifiers: INT17676U1111-1277-6732
• Study Type: interventional
• Target: 52
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate safety and pharmacokinetics (PK) effect of belumosudil on the uridine diphosphate glucuronosyltransferase (UGT)1A1 (Part 1), P glycoprotein (P-gp) (Part 2) and breast cancer resistance protein (BCRP)/organic anion transporting polypeptide (OATP)1B1 (Part 3) inhibition in the fed state in healthy male subjects.

Conditions

Immune System Disorder; Healthy Volunteers

Outcome Measures

Primary Outcomes (2)

• AUC(0-last)- Parts 1,2, and 3 (victim drugs)

  Area under the curve from time 0 to the time of last measurable concentration

  Multiple timepoints up to approximately 15 days

• AUC(0-inf)- Parts 1,2, and 3 (victim drugs

  Area under the curve from time 0 extrapolated to infinity

  Multiple timepoints up to approximately 15 days

Secondary Outcomes (11)

• Tmax- Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)

  Multiple timepoints up to approximately 15 days

• Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)

  Multiple timepoints up to approximately 15 days

• T1/2 -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)

  Multiple timepoints up to approximately 15 days

• AUC(0-last)-Part 1 (victim metabolite)

  Multiple timepoints up to approximately 10 days

• AUC(0-inf)- Part 1 (metabolite of victim drug)

  Multiple timepoints up to approximately 10 days

Study Arms (3)

Part 1

EXPERIMENTAL

Belumosudil + UGT1A1 victim drug administered in the fed state

Drug: Belumosudil; Drug: UGT1A1 victim drug

Part 2

EXPERIMENTAL

Belumosudil + P-gp victim drug administered in the fed state

Drug: Belumosudil; Drug: P-gp victim drug

Part 3

EXPERIMENTAL

Belumosudil + OATP1B1/BCRP victim drug administered in the fed state

Drug: Belumosudil; Drug: OATP1B1/BCRP victim drug

Interventions

Belumosudil DRUG

Pharmaceutical form: Tablet; Route of administration: Oral

Also known as: REZUROCK/KD025/SAR445761

Part 1; Part 2; Part 3

UGT1A1 victim drug DRUG

Pharmaceutical form: Tablet; Route of administration: Oral

Part 1

P-gp victim drug DRUG

Pharmaceutical form: Capsule; Route of administration: Oral

Part 2

OATP1B1/BCRP victim drug DRUG

Pharmaceutical form: Tablet; Route of administration: Oral

Part 3

Eligibility Criteria

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

You may qualify if:

• Healthy male participants aged 18 to 55 years old
• Must agree to use an adequate method of contraception
• Must be able to understand and provide a written informed consent

You may not qualify if:

• Participants are excluded from the study if any of the following criteria apply:
• Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients.
• Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active.
• Significant serious skin disease, including rash, food allergy, eczema, psoriasis, or urticaria.
• Failure to satisfy the investigator of fitness to participate for any other reason.
• The above information is not intended to contain all considerations relevant to the potential participation in a clinical trial.

Sponsors & Collaborators

• Kadmon, a Sanofi Company: lead

Study Sites (1)

Investigational Site Number: 8400001

Miami, Florida, 33126, United States

Location

Related Links

• INT17676 Plain Language Results Summary

MeSH Terms

Conditions

Immune System Diseases

Interventions

belumosudil

Study Officials

• Clinical Sciences & Operations

  Sanofi

  STUDY DIRECTOR

Study Design

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

Study Record Dates

• First Submitted: March 28, 2023
• First Posted: April 10, 2023
• Study Start: July 27, 2022
• Primary Completion: October 20, 2022
• Study Completion: October 28, 2022
• Last Updated: September 25, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will share

Locations

US (1)