Immune System Disorder, Healthy Volunteers
Conditions
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.
Interventions
DRUGBelumosudil
Pharmaceutical form: Tablet; Route of administration: Oral
DRUGUGT1A1 victim drug
Pharmaceutical form: Tablet; Route of administration: Oral
DRUGP-gp victim drug
Pharmaceutical form: Capsule; Route of administration: Oral
DRUGOATP1B1/BCRP victim drug
Pharmaceutical form: Tablet; Route of administration: Oral
Sponsors
Kadmon, a Sanofi Company
Study design
Allocation
NON_RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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 |
| AUC(0-inf)- Parts 1,2, and 3 (victim drugs | Multiple timepoints up to approximately 15 days | Area under the curve from time 0 extrapolated to infinity |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| 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. |
| 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 | Multiple 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. |
| Cmax- Part 1 (metabolite of victim drug) | Multiple timepoints up to approximately 10 days | — |
| Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites) | Multiple timepoints up to approximately 15 days | Maximum observed concentration |
Countries
United States
Outcome results
None listed