A Three-part, Sequential, Non-randomized, Open-label Study Designed to Evaluate the Effect of Oral Belumosudil on UGT1A1, P-gp, BCRP and OATP1B1 Inhibition in the Fed State in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 52
- 试验地点
- 1
- 主要终点
- AUC(0-inf)- Parts 1,2, and 3 (victim drugs
研究概览
简要总结
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.
详细描述
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.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Sequential
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •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
排除标准
- •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.
研究组 & 干预措施
Part 1
Belumosudil + UGT1A1 victim drug administered in the fed state
干预措施: UGT1A1 victim drug (Drug)
Part 1
Belumosudil + UGT1A1 victim drug administered in the fed state
干预措施: Belumosudil (Drug)
Part 2
Belumosudil + P-gp victim drug administered in the fed state
干预措施: Belumosudil (Drug)
Part 2
Belumosudil + P-gp victim drug administered in the fed state
干预措施: P-gp victim drug (Drug)
Part 3
Belumosudil + OATP1B1/BCRP victim drug administered in the fed state
干预措施: Belumosudil (Drug)
Part 3
Belumosudil + OATP1B1/BCRP victim drug administered in the fed state
干预措施: OATP1B1/BCRP victim drug (Drug)
结局指标
主要结局
AUC(0-inf)- Parts 1,2, and 3 (victim drugs
时间窗: Multiple 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)
时间窗: Multiple timepoints up to approximately 15 days
Area under the curve from time 0 to the time of last measurable concentration
次要结局
- T1/2 -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)(Multiple timepoints up to approximately 15 days)
- 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)
- 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)
- Tmax- Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)(Multiple timepoints up to approximately 15 days)
- Cmax -Parts 1, 2, and 3 (victim drugs, belumosudil and belumosudil metabolites)(Multiple timepoints up to approximately 15 days)
- T1/2- Part 1 (metabolite of victim drug)(Multiple timepoints up to approximately 10 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)
- 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)