Double-blind, Placebo-controlled, Randomized, Single Ascending Dose Study to Investigate the Tolerability, Safety, Pharmacokinetics, Pharmacodynamics, Absolute Bioavailability, Mass Balance, and Metabolism of ACT-541468 in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 40
- 试验地点
- 1
- 主要终点
- Number of subjects with treatment-emergent adverse events and serious adverse events
研究概览
简要总结
The main objectives of this first-into-man study were to investigate the safety, tolerability and the pharmacokinetic profile of single oral doses of ACT-541468 in healthy male adults. Pharmacodynamic effects (through a battery of Central Nervous System tests) were also assessed.
详细描述
The study consisted of ascending dose groups; each dose group was investigated in a new group of 8 healthy male subjects (6 on active drug and 2 on placebo). In addition, the study included a biocomparison part (dose group 2), an absolute bioavailability part (dose group 4), and a mass balance / metabolism part (dose group 3).
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Other
- 盲法
- Triple (Participant, Care Provider, Investigator)
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- 未提供
排除标准
- 未提供
研究组 & 干预措施
Dose group 1
Six subjects received 5 mg of ACT-541468 (formulation A) as a single oral dose and two subjects received the matching placebo.
干预措施: ACT-541468 (Formulation A) (Drug)
Dose group 1
Six subjects received 5 mg of ACT-541468 (formulation A) as a single oral dose and two subjects received the matching placebo.
干预措施: Placebo (Formulation A) (Drug)
Dose group 2
Three subjects received a single oral dose (25 mg) of ACT-541468 formulation A during Period 1 and a single oral dose (25 mg) of ACT-541468 formulation B during Period 2. Three other subjects Subjects received ACT-541468 formulation B during Period 1 and ACT-541468 formulation A during Period 2. Two additional subjects received the matching placebos in both treatment periods.
干预措施: ACT-541468 (Formulation A) (Drug)
Dose group 2
Three subjects received a single oral dose (25 mg) of ACT-541468 formulation A during Period 1 and a single oral dose (25 mg) of ACT-541468 formulation B during Period 2. Three other subjects Subjects received ACT-541468 formulation B during Period 1 and ACT-541468 formulation A during Period 2. Two additional subjects received the matching placebos in both treatment periods.
干预措施: ACT-541468 (Formulation B) (Drug)
Dose group 2
Three subjects received a single oral dose (25 mg) of ACT-541468 formulation A during Period 1 and a single oral dose (25 mg) of ACT-541468 formulation B during Period 2. Three other subjects Subjects received ACT-541468 formulation B during Period 1 and ACT-541468 formulation A during Period 2. Two additional subjects received the matching placebos in both treatment periods.
干预措施: Placebo (Formulation A) (Drug)
Dose group 2
Three subjects received a single oral dose (25 mg) of ACT-541468 formulation A during Period 1 and a single oral dose (25 mg) of ACT-541468 formulation B during Period 2. Three other subjects Subjects received ACT-541468 formulation B during Period 1 and ACT-541468 formulation A during Period 2. Two additional subjects received the matching placebos in both treatment periods.
干预措施: Placebo (Formulation B) (Drug)
Dose group 3
Six subjects received 50 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 oral tracer for the mass balance and metabolism analyses. Two other subjects received the matching placebos.
干预措施: ACT-541468 (Formulation A) (Drug)
Dose group 3
Six subjects received 50 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 oral tracer for the mass balance and metabolism analyses. Two other subjects received the matching placebos.
干预措施: Placebo (Formulation A) (Drug)
Dose group 3
Six subjects received 50 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 oral tracer for the mass balance and metabolism analyses. Two other subjects received the matching placebos.
干预措施: 14C-labeled ACT-541468 (Drug)
Dose group 3
Six subjects received 50 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 oral tracer for the mass balance and metabolism analyses. Two other subjects received the matching placebos.
干预措施: Placebo tracer (Drug)
Dose group 4
Six subjects received 100 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 intravenous tracer for the absolute bioavailability assessment. Two other subjects received the matching placebos.
干预措施: ACT-541468 (Formulation A) (Drug)
Dose group 4
Six subjects received 100 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 intravenous tracer for the absolute bioavailability assessment. Two other subjects received the matching placebos.
干预措施: Placebo (Formulation A) (Drug)
Dose group 4
Six subjects received 100 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 intravenous tracer for the absolute bioavailability assessment. Two other subjects received the matching placebos.
干预措施: 14C-labeled ACT-541468 (Drug)
Dose group 4
Six subjects received 100 mg of ACT-541468 (formulation A) as a single oral dose in combination with a [14C]-ACT-541468 intravenous tracer for the absolute bioavailability assessment. Two other subjects received the matching placebos.
干预措施: Placebo tracer (Drug)
Dose group 5
Six subjects received 200 mg of ACT-541468 (formulation A) as a single oral dose and two subjects received the matching placebo.
干预措施: ACT-541468 (Formulation A) (Drug)
Dose group 5
Six subjects received 200 mg of ACT-541468 (formulation A) as a single oral dose and two subjects received the matching placebo.
干预措施: Placebo (Formulation A) (Drug)
结局指标
主要结局
Number of subjects with treatment-emergent adverse events and serious adverse events
时间窗: Day 8
Collection of any adverse event at each dose level
次要结局
- Maximum plasma concentration (Cmax) of ACT-541468(From pre-dose up to 168 hours post-dose)
- Time to reach Cmax (tmax) of ACT-541468(From pre-dose up to 168 hours post-dose)
- Terminal half-life (t1/2) of ACT-541468(From pre-dose up to 168 hours post-dose)
- Area under the plasma concentration-time curves [AUC(0-inf)] of ACT-541468(From pre-dose up to 168 hours post-dose)
- Percentage of dose excreted in feces and urine(From pre-dose up to 168 hours post-dose)
- Absolute bioavailability (F) of ACT-541468(Up to 96 hours post-dose)