A Randomised, Double-blind, Placebo-controlled Trial to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Rising Oral Doses of 10 mg to 1200 mg of BI 135585 XX Administered as a Solution to Healthy Male Volunteers (Trial Part 1), Followed by an Open, Randomised, Single-dose, Intra-individual Bioavailability Comparison of 200 mg BI 135585 XX as Tablet and as Solution (Trial Part 2)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 60
- 试验地点
- 1
- 主要终点
- Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])
研究概览
简要总结
The purpose of the study is to investigate the safety, tolerability, pharmacokinetics incl. dose proportionality, and pharmacodynamics of BI 135585 XX (Part 1), as well as the relative bioavailability of two different immediate release tablet formulations versus oral solution (Part 2)
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 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
BI 135585
1 single dose per subject as oral solution in Part 1, or 3 single doses per subject as oral solution and 2 different tablet formulations in Part 2
干预措施: BI 135585 (Drug)
Placebo to BI 135585
1 single dose per subject as oral solution in Part 1
干预措施: Placebo to BI 135585 (Drug)
结局指标
主要结局
Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])
时间窗: up to 14 days post treatment
Assessment of tolerability by the investigator
时间窗: up to 14 days post treatment
Change from baseline in 12-lead ECG with special attention to QTc prolongation
时间窗: up to 14 days post treatment
Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland
时间窗: up to 14 days post treatment
Change from baseline in Physical examination (occurrence of findings)
时间窗: up to 14 days post treatment
Cardiopulmonary monitoring resulting in clinically relevant findings
时间窗: up to 14 days post treatment
Number of patients with Adverse events (AE)
时间窗: up to 14 days post treatment
次要结局
- tmax (time from dosing to maximum measured concentration)(up to 72 hours post treatment)
- AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)(up to 72 hours post treatment)
- t1/2 (terminal half-life of the analyte in plasma)(up to 72 hours post treatment)
- AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)(up to 72 hours post treatment)
- %AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)(up to 72 hours post treatment)
- λz (terminal rate constant in plasma)(up to 72 hours post treatment)
- CLR,t1-t2 (renal clearance of the analyte from timepoint t1 to timepoint t2) SRD part only[(up to 72 hours post treatment)
- UFF/UFE ratio as an indicator of 11β-HSD2 inhibition(up to 24h)
- (5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition(up to 24h)
- Cmax (maximum measured concentration of the analyte in plasma)(up to 72 hours post treatment)
- CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)(up to 72 hours post treatment)
- Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)(up to 72 hours post treatment)
- MRToral (mean residence time of the analyte in the body after oral administration)(up to 72 hours post treatment)
- Aet1-t2 (amount of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only(up to 72 hours post treatment)
- fet1-t2 (fraction of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only(up to 72 hours post treatment)
- Total urinary corticosteroids (5α-THF + 5β-THF + THE + UFF + UFE) as an indicator of the activation of the HPA axis(up to 24h)