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

A Three-part, Sequential, Non-randomized, Open-label Study Designed to Evaluate the Effect of Oral Belumosudil on UGT1A1, P-gp, BCRP and OATP1B1 Inhibition in the Fed State in Healthy Male Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers; Immune System Disorder
• Intervention / Treatment: Drug: Belumosudil; Drug: UGT1A1 victim drug; Drug: P-gp victim drug; Drug: OATP1B1/BCRP victim drug

Detailed Description

Part 1: The estimated time from screening until the follow-up phone call is approximately 6 weeks per subject.

Part 2: The estimated time from screening until the follow-up phone call is approximately 7 weeks per subject.

Part 3: The estimated time from screening until the follow-up phone call is approximately 7 weeks per subjects.

• Study Type: Interventional
• Enrollment (Actual): 52
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Florida
    • Miami, Florida, United States, 33126
      • Investigational Site Number: 8400001

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• 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

Exclusion Criteria:

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Sequential Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Part 1; Belumosudil + UGT1A1 victim drug administered in the fed state	Drug: Belumosudil; Pharmaceutical form: Tablet; Route of administration: Oral; Other Names: REZUROCK/KD025/SAR445761; Drug: UGT1A1 victim drug; Pharmaceutical form: Tablet; Route of administration: Oral
Experimental: Part 2; Belumosudil + P-gp victim drug administered in the fed state	Drug: Belumosudil; Pharmaceutical form: Tablet; Route of administration: Oral; Other Names: REZUROCK/KD025/SAR445761; Drug: P-gp victim drug; Pharmaceutical form: Capsule; Route of administration: Oral
Experimental: Part 3; Belumosudil + OATP1B1/BCRP victim drug administered in the fed state	Drug: Belumosudil; Pharmaceutical form: Tablet; Route of administration: Oral; Other Names: REZUROCK/KD025/SAR445761; Drug: OATP1B1/BCRP victim drug; Pharmaceutical form: Tablet; Route of administration: Oral

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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 Outcome Measures

Outcome Measure	Measure Description	Time Frame
Tmax- Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)	Time of maximum observed concentration.	Multiple timepoints up to approximately 15 days
Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)	Maximum observed concentration	Multiple timepoints up to approximately 15 days
T1/2 -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)	Terminal elimination half-life	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
Tmax- Part 1(metabolite of victim drug)		Multiple timepoints up to approximately 10 days
Cmax- Part 1 (metabolite of victim drug)		Multiple timepoints up to approximately 10 days
T1/2- Part 1 (metabolite of victim drug)		Multiple timepoints up to approximately 10 days
AUC(0-last) - Parts 1, 2, and 3 (Belumosudil and metabolites)		Multiple timepoints up to approximately 15 days
Area under the curve for the defined interval between doses (tau) [AUC(0 tau)] - Parts 1, 2, and 3	Area under the curve for the defined interval between doses (tau)	Multiple timepoints up to approximately 15 days
Number of participants with adverse events (AEs) and serious adverse events (SAEs)	To provide additional safety and tolerability information for belumosudil by assessing: AEs, vital signs, ECGs, physical examinations and laboratory safety tests following administration of the three victim drugs alone and in combination with belumosudil.	Up to 30 days after the administration of last dose of study drug i.e., up to approximately 43 days

Collaborators and Investigators

• Sponsor: Kadmon, a Sanofi Company
• Investigators: Study Director: Clinical Sciences & Operations, Sanofi

Publications and helpful links

Helpful Links

• INT17676 Plain Language Results Summary

Study record dates

Study Major Dates

• Study Start (Actual): July 27, 2022
• Primary Completion (Actual): October 20, 2022
• Study Completion (Actual): October 28, 2022

Study Registration Dates

• First Submitted: March 28, 2023
• First Submitted That Met QC Criteria: March 28, 2023
• First Posted (Actual): April 10, 2023

Study Record Updates

• Last Update Posted (Estimated): September 25, 2025
• Last Update Submitted That Met QC Criteria: September 21, 2025
• Last Verified: September 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Immune System Diseases; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Kinase Inhibitors; belumosudil
• Other Study ID Numbers: INT17676; U1111-1277-6732 (Registry Identifier: ICTRP)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES
• IPD Plan Description: Qualified researchers may request access to patient level data and related study documents including the clinical study report, study protocol with any amendments, blank case report form, statistical analysis plan, and dataset specifications. Patient level data will be anonymized and study documents will be redacted to protect the privacy of trial participants. Further details on Sanofi's data sharing criteria, eligible studies, and process for requesting access can be found at: https://vivli.org

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No