Bioavailability of Belumosudil (KD025) in Healthy Male Subjects
Condition: Bioavailability
Study type: Interventional
Phase: Phase 1

Summary: 
      Phase 1 bioavailability study to evaluate the pharmacokinetics (PK) and tolerability/safety
      of the belumosudil tablet formulation in the fasted and fed states and compared to the
      belumosudil capsule formulation in the fed state.
    

Detailed description: 
      This is a Phase 1, 3-way, crossover, randomized, open-label study in healthy subjects
      designed to compare the bioavailability of belumosudil (previously known as KD025) tablet
      formulation administered in the fed and fasted states and to assess the relative
      bioavailability of belumosudil tablet and capsule formulations in the fed state.

      The primary objective of the study is to determine the PK parameters of belumosudil tablet
      formulation in the fed and fasted states.

      The secondary objectives of the study are: (1) to assess the relative bioavailability of a
      tablet (test) to capsule (reference formulation of belumosudil; (2) to assess and compare the
      variability in the maximum concentration (Cmax) and area under the concentration-time curve
      (AUC) for belumosudil treatments (belumosudil 200 mg tablet in the fasting state, belumosudil
      200 mg tablet in the fed state, and belumosudil as two 100 mg capsules in the fed state); and
      (3) to provide additional safety and tolerability information for belumosudil.

      This is a single-center, open-label, randomized, single-dose, 3-period, 3-way, crossover
      study in healthy subjects.

      In each of 3 study periods, each subject receives 1 of the following single-dose treatments:

        -  Regimen A: Belumosudil 200 mg tablet in the fasted state

        -  Regimen B: Belumosudil 200 mg tablet in the fed state

        -  Regimen C: Belumosudil 200 mg as two 100-mg capsules in the fed state

      Subjects are randomized to receive 1 dose of investigational product (IP; belumosudil tablet
      or capsule) in the morning of Day 1 in a randomized manner following an overnight fast or a
      high-fat breakfast. Administration is performed on Day 1 with an appropriate interval between
      subjects based on logistical requirements. Start time is determined based on logistics.

      Subjects undergo a screening visit in the 21 days preceding first dose. Subjects are admitted
      to the clinical unit on the evening prior to dosing (Day -1), remain on site until 24 hours
      post-dose, and return to the clinic at 36 and 48 hours post-dose for PK assessments.

      There is a minimum washout period of 6 days between each dose administration. All other meals
      are standardized for each of the in-clinic phases of the 3 treatment periods. Each period
      follows the same study design.

      The randomized cohorts for the 3-periods were as follows:

        -  Cohort ABC: Regimen A (Period 1); Regimen B (Period 2); Regimen C (Period 3)

        -  Cohort BCA: Regimen B (Period 1); Regimen C (Period 2); Regimen A (Period 3)

        -  Cohort CAB: Regimen C (Period 1); Regimen A (Period 2); Regimen B (Period 3)

      A follow-up call is made 3 to 5 days after the final dose of IP.

      Planned enrollment is 24 subjects to insure there are 20 evaluable subjects. A subject is
      considered evaluable if (s)he completes treatment with fasted and fed tablet formulations
      (Regimens A and B) without major protocol deviations.
    

Intervention name(s): Belumosudil Tablet; Belumosudil Capsule
Intervention type(s): Drug; Drug
Other intervention name(s): Rezurock (brand); SLx-2119; Rezurock (brand); SLx-2119
Intervention MeSH terms: Belumosudil
Allocation: Randomized
Intervention model: Crossover Assignment
Masking: None (Open Label)
Primary purpose: Other