Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of 5 mg, 20 mg, 60 mg, 100 mg, 200 mg, 400 mg, 600 mg, 800 mg, 1000 mg, 1200 mg, 1500 mg, 2000 mg and 2400 mg BILN 2061 ZW (PEG 400: Ethanol Solution) in Healthy Male Subjects, Combined With Preliminary Evaluation of Food Effect of the Dose of 200 mg (Two-Stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Part and Subsequent Open Intraindividual Comparison Part)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 103
- 主要终点
- Total mean residence time of the analyte in plasma (MRT)
研究概览
简要总结
To assess the safety, tolerance and pharmacokinetics of 5 mg to 2400 mg BILN 2061 ZW
- In rising single doses
- With and without a 64 g fat breakfast at one selected dose
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- Double
入排标准
- 年龄范围
- 18 Years 至 50 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subjects as determined by results of screening
- •Signed written informed consent in accordance with good clinical practice (GCP) and local legislation
- •Age ≥ 18 and ≤ 50 years
- •Broca ≥ - 20 % and ≤ + 20 %
排除标准
- •Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
- •History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection
- •History of orthostatic hypotension, fainting spells and blackouts
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
- •Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
- •Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
- •Participation in another trial with an investigational drug within 1 month prior to administration or during the trial
- •Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial days
- •Alcohol abuse (> 60 g/day)
- •Drug abuse
- •Blood donation within 1 month prior to administration or during the trial
- •Excessive physical activities within 5 days prior to administration or during the trial
- •Any laboratory value outside the clinically accepted reference range and of clinical relevance
- •History of any familial bleeding disorder
研究组 & 干预措施
BILN 2061 ZW single rising doses
干预措施: BILN 2061 ZW single rising doses (Drug)
Placebo
干预措施: Placebo (Drug)
BILN 2061 ZW fixed dose fed
干预措施: BILN 2061 ZW fixed dose (Drug)
BILN 2061 ZW fixed dose fed
干预措施: Standardized breakfast (Other)
BILN 2061 ZW fixed dose fasted
干预措施: BILN 2061 ZW fixed dose (Drug)
结局指标
主要结局
Total mean residence time of the analyte in plasma (MRT)
时间窗: up to 48 hours after drug administration
Apparent volume of distribution during the terminal elimination phase (Vz/F)
时间窗: up to 48 hours after drug administration
Number of patients with clinically relevant changes in vital signs (systolic and diastolic blood pressure, pulse rate)
时间窗: Pre-dose, up to 48 hours after drug administration
Changes from baseline in laboratory tests
时间窗: Pre-dose and 48 hours after drug administration
Number of patients with clinically relevant changes in 12-lead ECG
时间窗: Pre-dose, up to 48 hours after drug administration
Amount of intact drug excreted in urine (Au)
时间窗: up to 48 hours after drug administration
Changes from baseline in physical examination
时间窗: Pre-dose and 48 hours after drug administration
Number of patients with adverse events
时间窗: Up to 48 hours after drug administration
Global assessment of tolerability by the investigator on a 4-point scale
时间窗: Up to 48 hours after drug administration
Maximum concentration of the analyte in plasma after a single dose administration (Cmax)
时间窗: up to 48 hours after drug administration
Area under the concentration-time curve of the analyte in plasma from time 0 to infinity (AUC0-infinity)
时间窗: up to 48 hours after drug administration
Time to reach Cmax following a single dose administration (tmax)
时间窗: up to 48 hours after drug administration
Elimination half-life of the analyte in plasma (t1/2)
时间窗: up to 48 hours after drug administration
Total oral clearance of the analyte from plasma after oral administration, divided by F (bioavailability factor) (CL/F)
时间窗: up to 48 hours after drug administration
次要结局
未报告次要终点