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

Phase 1
Completed
Conditions
Immune System Disorder (Healthy Volunteers)
Interventions
Drug: P-gp victim drug
Drug: UGT1A1 victim drug
Drug: OATP1B1/BCRP victim drug
Registration Number
NCT05806567
Lead Sponsor
Kadmon, a Sanofi Company
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.

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.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
52
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 & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Part 2BelumosudilBelumosudil + P-gp victim drug administered in the fed state
Part 2P-gp victim drugBelumosudil + P-gp victim drug administered in the fed state
Part 3BelumosudilBelumosudil + OATP1B1/BCRP victim drug administered in the fed state
Part 1UGT1A1 victim drugBelumosudil + UGT1A1 victim drug administered in the fed state
Part 3OATP1B1/BCRP victim drugBelumosudil + OATP1B1/BCRP victim drug administered in the fed state
Part 1BelumosudilBelumosudil + UGT1A1 victim drug administered in the fed state
Primary Outcome Measures
NameTimeMethod
AUC(0-inf)- Parts 1,2, and 3 (victim drugsMultiple timepoints up to approximately 15 days

Area under the curve from time 0 extrapolated to infinity

AUC(0-last)- Parts 1,2, and 3 (victim drugs)Multiple timepoints up to approximately 15 days

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

Secondary Outcome Measures
NameTimeMethod
AUC(0-last) - Parts 1, 2, and 3 (Belumosudil and metabolites)Multiple timepoints up to approximately 15 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
T1/2 -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)Multiple timepoints up to approximately 15 days

Terminal elimination half-life

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
Tmax- Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)Multiple timepoints up to approximately 15 days

Time of maximum observed concentration.

Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)Multiple timepoints up to approximately 15 days

Maximum observed concentration

Area under the curve for the defined interval between doses (tau) [AUC(0 tau)] - Parts 1, 2, and 3Multiple timepoints up to approximately 15 days

Area under the curve for the defined interval between doses (tau)

Number of participants with adverse events (AEs) and serious adverse events (SAEs)Up to 30 days after the administration of last dose of study drug i.e., up to approximately 43 days

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.

Trial Locations

Locations (1)

Investigational Site Number: 8400001

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Miami, Florida, United States

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