A Phase 1, Randomized, Open-Label, Single-Dose Study to Evaluate Potential Pharmacokinetic Interaction Between Lesinurad and Metformin and Between Lesinurad and Furosemide in Health Adult Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 23
- 主要终点
- PK profile of metformin and furosemide from plasma
研究概览
简要总结
This study will assess the potential effects of lesinurad on the pharmacokinetics (PK) of metformin and furosemide in healthy, adult male subjects.
详细描述
Leinurad is a weak in vitro inhibitor of the hepatic transporter OCT1 and the renal transporters OAT1 and OAT3 (OAT1/3). To assess the clinical relevance of these in vitro findings, this clinical study will evaluate the effect of lesinurad on the PK of metformin (OCT1 substrate) and furosemide (OAT1/3 substrate).
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 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
- •Subject has a body weight ≥ 50 kg (110 lbs) and body mass index ≥ 18 and ≤ 30 kg/m
- •Subject is free of any clinically significant disease or medical condition, per the Investigator's judgment.
排除标准
- •Subject has a history or suspicion of kidney stones, prostatic hyperplasia, or urinary stricture.
- •Subject has undergone major surgery within 3 months prior to Screening.
- •Subject donated blood or experienced significant blood loss (>450 mL) within 12 weeks prior to Screening or gave a plasma donation within 4 weeks prior to Screening.
- •Subject has inadequate venous access or unsuitable veins for repeated venipuncture.
研究组 & 干预措施
Lesinurad and Metformin
Sequence A- Day 1: Metformin 850 mg; Day 5: Lesinurad 400 mg with metformin 850 mg
Sequence B- Day 1: Lesinurad 400 mg with metformin 850 mg; Day 5: Metformin 850 mg
干预措施: Lesinurad 400 mg (Drug)
Lesinurad and Metformin
Sequence A- Day 1: Metformin 850 mg; Day 5: Lesinurad 400 mg with metformin 850 mg
Sequence B- Day 1: Lesinurad 400 mg with metformin 850 mg; Day 5: Metformin 850 mg
干预措施: Metformin 850 mg (Drug)
Lesinurad and Furosemide
Sequence C - Day 1: Furosemide 40 mg; Day 5: Lesinurad 400 mg with furosemide 40 mg
Sequence D - Day 1: Lesinurad 400 mg with furosemide 40 mg; Day 5: Furosemide 40 mg
干预措施: Lesinurad 400 mg (Drug)
Lesinurad and Furosemide
Sequence C - Day 1: Furosemide 40 mg; Day 5: Lesinurad 400 mg with furosemide 40 mg
Sequence D - Day 1: Lesinurad 400 mg with furosemide 40 mg; Day 5: Furosemide 40 mg
干预措施: Furosemide 40 mg (Drug)
结局指标
主要结局
PK profile of metformin and furosemide from plasma
时间窗: Day 1 and Day 5
Profile in terms of maximum observed concentration (Cmax), time of occurence of maximum observed concentration (Tmax), area under the concentration-time curve (AUC), and apparent terminal half-life (t1/2).
PK profile of furosemide from urine
时间窗: Day 1 and Day 5
Profile in terms of renal clearance (CLr) and amount of compound excreted into urine unchanged (Ae).
次要结局
- Incidence of Adverse Events and Changes in Laboratory, Electrocardiogram, and Vital Signs Parameters(5 weeks)