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.
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
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
52
Pharmaceutical form: Tablet; Route of administration: Oral
Pharmaceutical form: Tablet; Route of administration: Oral
Pharmaceutical form: Capsule; Route of administration: Oral
Investigational Site Number: 8400001
Miami, Florida, United States
AUC(0-last)- Parts 1,2, and 3 (victim drugs)
Area under the curve from time 0 to the time of last measurable concentration
Time frame: 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
Time frame: Multiple timepoints up to approximately 15 days
Tmax- Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)
Time of maximum observed concentration.
Time frame: Multiple timepoints up to approximately 15 days
Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)
Maximum observed concentration
Time frame: Multiple timepoints up to approximately 15 days
T1/2 -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)
Terminal elimination half-life
Time frame: Multiple timepoints up to approximately 15 days
AUC(0-last)-Part 1 (victim metabolite)
Time frame: Multiple timepoints up to approximately 10 days
AUC(0-inf)- Part 1 (metabolite of victim drug)
Time frame: Multiple timepoints up to approximately 10 days
Tmax- Part 1(metabolite of victim drug)
Time frame: Multiple timepoints up to approximately 10 days
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Pharmaceutical form: Tablet; Route of administration: Oral
Cmax- Part 1 (metabolite of victim drug)
Time frame: Multiple timepoints up to approximately 10 days
T1/2- Part 1 (metabolite of victim drug)
Time frame: Multiple timepoints up to approximately 10 days
AUC(0-last) - Parts 1, 2, and 3 (Belumosudil and metabolites)
Time frame: 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)
Time frame: 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.
Time frame: Up to 30 days after the administration of last dose of study drug i.e., up to approximately 43 days