Safety, Tolerability and Pharmacokinetics of Single Rising Oral Doses of BI 137882 in Healthy Male Volunteers (A Randomised, Single-blind, Placebo-controlled Phase I Study)
试验速览
- 阶段
- 1 期
- 状态
- 终止
- 入组人数
- 40
- 主要终点
- Number of Subjects With Drug Related Adverse Events
研究概览
简要总结
Safety, Tolerability and Pharmacokinetics of Single Rising Oral Doses of BI 137882 in Healthy Male Volunteers
详细描述
As a transition from preclinical investigations to clinical development in this first-in-man trial, safety, tolerability, and pharmacokinetics of BI 137882 will be assessed in healthy male volunteers using single rising oral doses in order to provide the basis for a potential ongoing clinical development of BI 137882 in the indication of COPD.
Healthy male subjects aged 21 - 50 years will be recruited for this study. They provide a relatively stable physiological, biochemical and hormonal basis (steady state) for studying drug effects, they show no disease-related variation and they are not taking concomitant medication.
Within each dose group, all actively treated individuals will receive the same BI 137882 dose. The next higher dose will only be administered if the treatment in the preceding dose group was safe and well tolerated.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- Single
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
- 未提供
排除标准
- 未提供
研究组 & 干预措施
BI 137882 Dose 3
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 1
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 2
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 4
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 5
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 6
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 7
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 8
Powder for oral solution
干预措施: BI 137882 (Drug)
BI 137882 Dose 9
Powder for oral solution
干预措施: BI 137882 (Drug)
Placebo
Powder for oral solution
干预措施: Placebo (Drug)
结局指标
主要结局
Number of Subjects With Drug Related Adverse Events
时间窗: From baseline up to 28 days
Number of subjects with drug related adverse events (AEs)
Blood Pressure
时间窗: Baseline and 28 days
Change from baseline for systolic blood pressure (SBP) and diastolic blood pressure (DBP)
Pulse Rate (PR)
时间窗: Baseline and 28 days
Change from Baseline to 28 Days in Pulse Rate
Respiratory Rate (RR)
时间窗: Baseline and 28 days
Change from Baseline to 28 Days in Respiratory rate (RR)
Body Temperature
时间窗: Baseline and 28 days
Change from baseline to 28 Days in Body temperature
Assessment of Tolerability by Investigator
时间窗: 28 days
The investigator assessed tolerability based on adverse events and the laboratory evaluation according to the categories 'good', 'satisfactory', 'not satisfactory', and 'bad'.
次要结局
- Maximum Measured Concentration (Cmax)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Time to Maximum Measured Concentration (Tmax)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Area Under the Curve 0 to Infinity (AUC0-infinity)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Terminal Half-life (t1/2)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Renal Clearance of BI 137882 From the Time Point t1 Until the Time Point t2(0-4, 4-8, 8-12, and 12-24 hours after drug administration)
- Concentration of Tumour Necrosis Factor-alpha (TNF-α) Induced by Lipopolysaccharide (LPS) in Whole Blood ex Vivo(0.5 hours (h) before drug administration and 2h, 6h, 24h and 48h after drug administration)
- Concentration of Leukotriene B4 (LTB4) Induced by N-formyl-methionine-leucine-phenylalanine (fMLP) in Whole Blood ex Vivo.(0.5 hours (h) before drug administration and 2h, 6h, 24h and 48h after drug administration)
- Area Under the Effect Curve (AUEC)(30 minutes (min) before drug administration and 2 hours (h), 6h, 24h and 48h after drug administration)
- Maximum Effect (Emax)(30 minutes (min) before drug administration and 2 hours (h), 6h, 24h and 48h after drug administration)
- Minimum Effect (Emin)(30 minutes (min) before drug administration and 2 hours (h), 6h, 24h and 48h after drug administration)
- Area Under the Curve 0 to the Last Quantifiable Data Point (AUC0-tz)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Terminal Rate Constant (λz)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Mean Residence Time (MRTpo)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Apparent Clearance (CL/F)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Apparent Volume of Distribution (Vz/F)(30 minutes (min) before drug administration and 30min, 1 hour (h), 2h, 4h, 6h, 8h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 264h, 336h and 480h after drug administration)
- Amount of BI 137882 Eliminated in Urine From the Time Point t1 to Time Point t2(0-4, 4-8, 8-12, and 12-24 hours after drug administration)
- Fraction of BI 137882 Eliminated in Urine From Time Point t1 to Time Point t2(0-4, 4-8, 8-12, and 12-24 hours after drug administration)