An Open Study to Investigate the Effect of Different Boosting Agents on Pharmacokinetics of Single Doses of BILR 355 BS (Dose Steps: 5 and 12.5 mg) Dissolved in 5 mL PEG 400 After Oral Administration in Healthy Male Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 44
- 主要终点
- Maximum observed concentration of the analyte in the plasma (Cmax)
研究概览
简要总结
Assessment of the effect of different boosting agents on pharmacokinetics of a single dose of BILR 355 BS dissolved in PEG 400
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
- None
入排标准
- 年龄范围
- 21 Years 至 50 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •All participants in the study were to be healthy males, range from 21 to 50 years of age and their body mass index (BMI) be within 18.5 to 29.9 kg/m2 (BMI calculation: weight in kilograms divided by the square of height in meters)
- •In accordance with good clinical practice (GCP) and the local legislation all volunteers had to give their written informed consent prior to admission to the study
排除标准
- •Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •History of orthostatic hypotension, fainting spells or blackouts
- •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 at least one month or less than ten half-lives of the respective drug before enrolment in the study or during the study
- •Use of any drugs which might influence the results of the trial up to 7 days prior to enrolment in the study or during the study
- •Participation in another trial with an investigational drug (<= two months prior to administration or during the trial)
- •Smoker (> 10 cigarettes or > 3 cigars of > 3 pipes/day)
- •Inability to refrain from smoking on trial days
- •Alcohol abuse (> 60 g/day)
- •Drug abuse
- •Blood donation (>= 100 mL within four weeks prior to administration or during the trial)
- •Any laboratory value outside the clinically accepted reference range
- •Excessive physical activities within the last week before the trial or during the trial
- •Following exclusion criteria are of special interest for this study:
- •Erythema, exanthema and comparable skin alterations
- •For the boosting agents atazanavir and atazanavir plus ritonavir, subjects with a PQ interval length in the screening ECG of > 200 ms or any higher degree of atrio-ventricular (AV) block were to be excluded
研究组 & 干预措施
Single rising dose of BILR 355 BS with grapefruit juice
干预措施: Grapefruit juice (Other)
Single rising dose of BILR 355 BS with nelfinavir
干预措施: BILR 355 BS (Drug)
Single rising dose of BILR 355 BS with nelfinavir
干预措施: Nelfinavir (Drug)
Single rising dose of BILR 355 BS with grapefruit juice
干预措施: BILR 355 BS (Drug)
Single dose of BILR 355 BS with atazanavir
干预措施: BILR 355 BS (Drug)
Single dose of BILR 355 BS with atazanavir
干预措施: Atazanavir (Drug)
Single dose of BILR 355 BS with atazanavir, ritonavir
干预措施: BILR 355 BS (Drug)
Single dose of BILR 355 BS with atazanavir, ritonavir
干预措施: Atazanavir (Drug)
Single dose of BILR 355 BS with atazanavir, ritonavir
干预措施: Ritonavir (Drug)
结局指标
主要结局
Maximum observed concentration of the analyte in the plasma (Cmax)
时间窗: up to 120 hours after start of treatment
Time from dosing to the maximum concentration of the analyte in plasma (tmax)
时间窗: up to 120 hours after start of treatment
Area under the concentration-time curve of the analyte in plasma at different time points (AUC)
时间窗: up to 120 hours after start of treatment
Apparent terminal half-life of the analyte in plasma (t1/2)
时间窗: up to 120 hours after start of treatment
Apparent clearance of the analyte in plasma after extravascular multiple dose administration (CL/F)
时间窗: up to 120 hours after start of treatment
Total mean residence time of the analyte in the body (MRTtot)
时间窗: up to 120 hours after start of treatment
Apparent volume of distribution of the analyte during the terminal phase λz following extravascular administration (Vz/F)
时间窗: up to 120 hours after start of treatment
Renal clearance of the analyte determined over the dosing interval τ (CLR)
时间窗: up to 120 hours after start of treatment
Amount of the analyte excreted into urine (Ae)
时间窗: up to 72 hours after start of treatment
次要结局
- Number of participants with clinically relevant changes in laboratory parameters(up to 10 days after start of treatment)
- Number of participants with clinically relevant changes in vital signs (blood pressure, pulse-, respiratory rate, body temperature)(up to 10 days after start of treatment)
- Number of participants with clinically relevant changes in 12-lead ECG(up to 10 days after start of treatment)
- Number of participants with clinically relevant changes in faecal occult blood testing(up to 10 days after start of treatment)
- Number of participants with adverse events(Up to 25 days)
- Global tolerability assessment by investigator on a 5-point scale(Up to 10 days after start of treatment)
- Number of participants with clinically relevant changes in neurological assessment(up to 10 days after start of treatment)