A Phase 1, Open-label Study of the Absorption, Metabolism, and Excretion of [14C]-Olinciguat ([14C]-IW-1701) Following a Single Oral Dose in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 8
- 试验地点
- 1
- 主要终点
- Cumulative feu and cumulative fef
研究概览
简要总结
The primary objective is to characterize the pharmacokinetics (PK) of olinciguat and total radioactivity and to assess the elimination of total radioactivity from a single oral dose of [14C]-olinciguat.
详细描述
OLI-103 is a Phase 1 open-label, nonrandomized, single-dose study in up to 8 subjects that will be conducted at a single center in the US. Safety assessments will be performed throughout the clinic period and multiple PK samples will be collected. Subjects will be confined to the clinical research center for at least 8 days.
The purpose of the study is to determine the absorption, metabolism, and excretion of [14C]-olinciguat and to characterize and determine, where possible, the metabolites present in plasma, urine, and feces after a single oral dose. The study will help identify and characterize olinciguat metabolites, evaluate the likelihood of effects of liver or kidney impairment on the disposition of olinciguat, and assess the likelihood of drug-drug interactions with olinciguat.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Other
- 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
- •Males of any race, between 18 and 55 years of age, inclusive
- •Body mass index between 18 and 32 kg/m2, inclusive
- •Subject is in good health and has no clinically significant findings on physical examination
- •Men must agree to use protocol-specified contraception and also to not donate sperm throughout the study and for at least 90 days after the final dose of study drug
排除标准
- •Any active or unstable clinically significant medical condition
- •Use of any prescribed or non-prescribed medication
- •Additional inclusion/exclusion criteria may apply per protocol
研究组 & 干预措施
Healthy Male Volunteers
Single oral dose of [14C]-olinciguat
干预措施: [14C]-olinciguat (Drug)
结局指标
主要结局
Cumulative feu and cumulative fef
时间窗: up to Day 15
Cmax of total radioactivity in plasma and whole blood
时间窗: up to Day 15
Tmax of total radioactivity in plasma and whole blood
时间窗: up to Day 15
Apparent volume of distribution of olinciguat (Vz/F)
时间窗: up to Day 15
AUC0-inf of total radioactivity in plasma and whole blood
时间窗: up to Day 15
Maximum observed concentration (Cmax) of olinciguat in plasma
时间窗: up to Day 15
Amount of total radioactivity excreted in urine (Aeu) and feces (Aef)
时间窗: up to Day 15
Cumulative Aeu and cumulative Aef
时间窗: up to Day 15
Percentage of total radioactivity excreted in urine (feu) and feces (fef)
时间窗: up to Day 15
Percentage of total radioactivity in total excreta (feces + urine)
时间窗: up to Day 15
Area under the concentration-time curve (AUC) from time zero to infinity (AUC0-inf) of olinciguat in plasma
时间窗: up to Day 15
AUC from time zero to the last quantifiable concentration (AUC0-last) of olinciguat in plasma
时间窗: up to Day 15
AUC0-last of total radioactivity in plasma and whole blood
时间窗: up to Day 15
Time of Cmax (Tmax) of olinciguat in plasma
时间窗: up to Day 15
Apparent total clearance of olinciguat (CL/F)
时间窗: up to Day 15
Apparent terminal elimination half-life (t1/2) of olinciguat in plasma
时间窗: up to Day 15
t1/2 total radioactivity in plasma and whole blood
时间窗: up to Day 15
AUC0-inf of plasma olinciguat concentration relative to AUC0-inf of plasma total radioactivity (AUC0-inf Ratio of Plasma Olinciguat/Plasma Total Radioactivity)
时间窗: up to Day 15
AUC0-inf of whole blood total radioactivity to AUC0-inf of plasma total radioactivity (AUC0-inf Ratio of Blood Total Radioactivity/Plasma Total Radioactivity)
时间窗: up to Day 15
次要结局
- AUC0-inf of metabolite radioactivity levels in plasma(up to Day 15)
- Molecular ion mass of metabolites(up to Day 15)
- Levels of metabolite radioactivity excreted in urine and feces(up to Day 15)
- AUC0-inf of plasma metabolite radioactivity levels relative to AUC0-inf of plasma total radioactivity (Plasma AUC0-inf Ratio of Metabolite Radioactivity/Total Radioactivity)(up to Day 15)
- Chromatographic retention time of metabolites(up to Day 15)
- Characteristic mass spectrometry fragmentation ions of metabolites(up to Day 15)
- Chemical structures (graphical representations showing atom connectivity) proposed for plasma, urine, and feces metabolites(up to Day 15)
- Number(s) of participants with ≥1 treatment-emergent serious adverse event (SAE)(up to Day 15)
- Number(s) of participants with ≥1 clinically significant abnormal physical examination finding(up to Day 15)
- Number(s) of participants with ≥1 adverse event (AE) leading to study drug discontinuation(up to Day 15)
- Number(s) of participants with ≥1 Grade ≥3 AE (per CTCAE v. 5.0)(up to Day 15)