A Double-micro-tracer Human Absorption, Distribution, Metabolism and Excretion (hADME) and Absolute Bioavailability Trial After a Single Oral Dose of BI 1569912 (C-14) and a Single, Concomitant, Intravenous Micro-dose of BI 1569912 (C-13) in Healthy Male Subjects (a Phase I, Open-label, Non-randomised, Single-dose, Fixed-sequence Trial)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 8
- 试验地点
- 1
- 主要终点
- Fraction Excreted in Urine as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (fe Urine,0-tz) of [14C]-Radioactivity
研究概览
简要总结
The main objectives of this trial are:
- To investigate basic pharmacokinetics of BI 1569912 and total radioactivity, including mass balance, excretion pathways and metabolism following oral administration of BI 1569912 (C-14) to healthy male subjects (test treatment, T).
- To investigate the absolute bioavailability of BI 1569912 as single oral solution dose, using a single, concomitant intravenous micro-tracer administration of BI 1569912 (C-13) (reference treatment, R)
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Subjects will only be included in the trial if they meet the following criteria:
- •Healthy male subjects according to the assessment of the investigator, as based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), and clinical laboratory tests
- •Age of 18 to 55 years (inclusive)
- •Body mass index (BMI) of 18.5 to 29.9 kg/m 2 (inclusive)
- •Signed and dated written informed consent in accordance with ICH-GCP and local legislation prior to admission to the trial
排除标准
- •Subjects will not be allowed to participate, if any of the following general criteria apply:
- •Any finding in the medical examination (including BP, PR or ECG) deviating from normal and assessed as clinically relevant by the investigator
- •Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 40 to 100 beats per minute (bpm)
- •Any laboratory value outside the reference range that the investigator considers to be of clinical relevance, in particular hepatic parameters (alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin) or renal parameters (creatinine) exceeding the upper limit of normal (ULN) after repeated measurements
- •Any evidence of a concomitant disease assessed as clinically relevant by the investigator
- •Further exclusion criteria apply
研究组 & 干预措施
10 mg BI 1569912 (C-14) oral solution (test) - 100 μg BI 1569912 (C-13) i.v. infusion (reference)
Healthy male participants received a single dose of 10 milligram (mg) [14C]-labeled BI 1569912 mixed with unlabeled BI 1569912 taken as an oral solution and 30 minutes later received a single dose of 100 microgram (µg) [13C]-labeled BI 1569912 taken as an intravenous (i.v.) infusion.
干预措施: BI 1569912 (C-14) (Drug)
10 mg BI 1569912 (C-14) oral solution (test) - 100 μg BI 1569912 (C-13) i.v. infusion (reference)
Healthy male participants received a single dose of 10 milligram (mg) [14C]-labeled BI 1569912 mixed with unlabeled BI 1569912 taken as an oral solution and 30 minutes later received a single dose of 100 microgram (µg) [13C]-labeled BI 1569912 taken as an intravenous (i.v.) infusion.
干预措施: BI 1569912 (C-13) (Drug)
结局指标
主要结局
Fraction Excreted in Urine as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (fe Urine,0-tz) of [14C]-Radioactivity
时间窗: Up to 14 days.
Mass balance recovery for \[14C\]-radioactivity in urine after oral administration of BI 1569912 (C-14): Fraction excreted in urine as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (fe urine,0-tz).
Fraction Excreted in Faeces as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (fe Faeces,0-tz) of [14C]-Radioactivity
时间窗: Up to 14 days.
Mass balance recovery for \[14C\]-radioactivity in faeces after oral administration of BI 1569912 (C-14): Fraction excreted in faeces as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (fe faeces,0-tz) of \[14C\]-radioactivity.
Total Recovery of [14C]-Radioactivity
时间窗: Up to 14 days.
Mass balance recovery for \[14C\]-radioactivity in urine and faeces after oral administration of BI 1569912 (C-14). The total recovery is calculated based on the individual values and hence can differ from the sum of the urine and faeces gMean values.
Area Under the Concentration-time Curve of BI 1569912 Over the Time Interval From 0 Extrapolated to Infinity in Plasma (AUC0-∞)
时间窗: Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only.
Area under the concentration-time curve of BI 1569912 over the time interval from 0 extrapolated to infinity in plasma (AUC0-∞) for BI 1569912 and \[13C\]-BI 1569912 after a single oral administration of BI 1569912 (C-14) (test treatment) and a single concomitant intravenous administration of BI 1569912 (C-13) (reference treatment). The presented data was derived from an analysis of variance (ANOVA) on the logarithmic scale including the fixed effect for 'treatment' and 'subject' as a random effect.
次要结局
- Maximum Measured Concentration of BI 1569912 in Plasma (Cmax)(Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only.)
- Area Under the Concentration-time Curve of BI 1569912 Over the Time Interval From 0 to the Last Quantifiable Time Point in Plasma (AUC 0-tz)(Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only.)