A Study to Determine the Effect of 500 mg Oral Dose of KD025 in Healthy Male and Post-menopausal Female Subjects

Study Overview
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Brief Summary
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The purpose of this study is to determine the safety, tolerability, and pharmacokinetics of 500 mg oral BID dose of KD025 in healthy male and post-menopausal female participants.

Detailed Description
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Up to approximately 58 days including safety follow up period of 30 days after participant is treated with the last dose of study drug.

Official Title
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A Phase 1, Placebo-Controlled, Double-Blind Study to Examine the Safety, Tolerability, and Pharmacokinetics of 500 mg KD025 Administered Twice Daily in Healthy Male and Post-Menopausal Female Subjects

Conditions
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Immune System Disorder (Healthy Volunteer)

Intervention / Treatment
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* Drug: Belumosudil mesylate
* Drug: Placebo


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy participants between the ages of 18 and 55 years, inclusive. Female who is not of reproductive potential. Able to provide written informed consent prior to the performance of any study specific procedures. Body mass index (BMI) range of 19-30 kilogram per square meter (kg/m2), inclusive. Exclusion Criteria: Past or present disease that is judged by the investigator to have the potential to interfere with the study procedures, compromise safety, or affect the PK evaluations. Known sensitivity to Rho-associated coiled-coil containing serine/threonine protein kinases (ROCK2) inhibitor agents or to any of the constituents of the KD025 formulation. The above information is not intended to contain all considerations relevant to the potential participation in a clinical trial.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Double


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: KD025<br>500 mg KD025 administered orally twice daily (BID) for 28 days | Drug: Belumosudil mesylate<br>* Pharmaceutical form: capsule; Route of administration: oral<br>* Other names: SAR445761;|
| Placebo Comparator: Placebo<br>Placebo administered orally BID for 28 days | Drug: Placebo<br>* Pharmaceutical form: capsule; Route of administration: oral<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Number of participants with adverse events and serious adverse events | Number of participants with adverse events and serious adverse events | Up to approximately 58 days | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Cmax of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | Cmax maximum plasma concentration determined directly from the concentration time profile | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| Tmax of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | tmax, observed time to reach peak plasma concentration | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| Cmin of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | Cmin, Minimum or trough plasma concentration after its administration and just prior to the administration of a subsequent dose as determined from the concentration time cprofile | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| AUC0 -τ of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | AUC0 -τis area under the plasma concentration-time curve from predose (time 0) to end of dosing collection (30 hours) | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| AUCinf of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | AUCinf, area under the concentration-time curve from predose (time 0) extrapolated to Infinity | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| Accumulation ratio (R) of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | Accumulation ratio, determined as the ratio of Day 28 AUC divided by Day 1 AUC and as the ratio of Day 28 Cmax divided by Day 1 Cmax | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 | 
| t1/2 of KD025 and its metabolites [M1 (KD025m1) and M2 (KD025m2)] | t1/2 terminal elimination half-life | Predose and multiple timepoints up to 30 hours postdose on Days 1 and 28 |