A Phase I, Open-label, Non-randomized, Single-dose, Single-arm, Single-period Study to Investigate the Metabolism and Pharmacokinetics of [C-14]-Labelled BI 1015550 After Oral Administration in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 6
- 试验地点
- 1
- 主要终点
- Percentage of the Amount of [14C]-Radioactivity Excreted Among the Administered Single Oral Dose of [14-C] BI 1015550-EQ in Urine (Feurine, 0-tz), Faeces (Fefaeces, 0-tz) and Vomit (Fevomit, 0-tz)
研究概览
简要总结
The main objective of this trial is to investigate the basic pharmacokinetics of BI 1015550 and its metabolite BI 764333 (M480), [14C]-radioactivity, including mass balance, excretion pathways and metabolism following a single oral dose BI 1015550 (C-14) administered to healthy male subjects.
The primary objective is:
- To assess the mass balance recovery of [14C]-radioactivity from urine and faeces as well as vomit in case of occurrence after a single oral dose of BI 1015550 (C-14) administered to healthy male subjects
The secondary objectives are:
- To assess the pharmacokinetics of [C-14]-BI 1015550 and BI 1015550 as well as its metabolite BI 764333 in plasma following a single oral dose of BI 1015550 (C-14)
- To assess the safety and tolerability of BI 1015550
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 65 Years（Adult, Older Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •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 electrocardiograms (ECG), and clinical laboratory tests
- •Age of 18 to 65 years (inclusive)
- •Body mass index (BMI) of 18.5 to 29.9 kg/m2 (inclusive)
- •Signed and dated written informed consent prior to admission to the study, in accordance with Good Clinical Practice (GCP) and local legislation
- •Male subjects who meet any of the following criteria from screening until 90 days after trial completion:
- •Use of adequate contraception of the female partner, e.g. any of the following methods plus condom: implants, injectables, combined oral or vaginal contraceptives, intrauterine device, which started at least two months prior to first study drug administration or barrier method (e.g. diaphragm with spermicide) or,
- •Sexually abstinent or,
- •A vasectomy performed at least 1 year prior to screening (with medical assessment of the surgical success) or,
- •Surgically sterilised female partner (including hysterectomy, bilateral tubal occlusion, or bilateral oophorectomy) or,
- •Postmenopausal female partner, defined as at least 1 year of spontaneous amenorrhea (in questionable cases a blood sample with levels of Follicle-Stimulating Hormone (FSH) above 40 U/L and estradiol below 30 ng/L is confirmatory)
排除标准
- •Any finding in the medical examination (including blood pressure (BP), pulse rate (PR) or electrocardiogram (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 millimetre of mercury (mmHg), diastolic blood pressure outside the range of 45 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
- •Any evidence of a concomitant disease assessed as clinically relevant by the investigator
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Cholecystectomy or other surgery of the gastrointestinal tract that could interfere with the pharmacokinetics of the trial medication (except appendectomy or simple hernia repair)
- •Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders
- •History of relevant orthostatic hypotension, fainting spells, or blackouts
- •Further exclusion criteria apply
研究组 & 干预措施
BI 1015550 (C-14)
Participants received a single dose of 18 milligrams (mg) BI 1015550 (C-14) consisting of 17.16 mg non-labelled BI 1015550 mixed with 0.84 mg [14C]BI 1015550-EQ as 36 milliliters (mL) of oral solution (0.5 mg/mL) labelled with a radioactive dose of 3.7 megaBecquerel (MBq) (100 micro Curie (μ Ci), corresponding to 0.2864 miliSievert (mSV)) on Day 1 with 240 mL of water after an overnight fast of at least 10 hours.
干预措施: BI 1015550 (C-14) (Drug)
结局指标
主要结局
Percentage of the Amount of [14C]-Radioactivity Excreted Among the Administered Single Oral Dose of [14-C] BI 1015550-EQ in Urine (Feurine, 0-tz), Faeces (Fefaeces, 0-tz) and Vomit (Fevomit, 0-tz)
时间窗: From Day -1 or Day 1 - 2 hours (h) before drug administration until release criteria for radioactivity recovery had been met, up to Day 30-31. See also description section.
0-tz refers to 0 until latest individually available cumulative fraction after drug administration. Vomit=Not applicable. Amount excreted calculated by volume multiplied with concentration of sample for respective time interval. Amount then refers to administered dose as fraction excreted in percent (dose=100%), done cumulatively. Time frames: Urine: on Day -1 or 1 -2 hours (h) before drug administration + at 0-4, 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216 h after drug administration. Faeces: on Day -1 or 1 -2 hours (h) before drug administration + 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216 h after drug administration. Thereafter, if warranted, 24 h collections for urine and faeces were to be performed every 7 days starting on Day 16, at Day 16-17, Day 23-24, Day 30-31. When the release criteria for radioactivity recovery had been met then urine/faeces sampling was stopped (earliest stop on Day 10).
次要结局
- Area Under the Concentration-time Curve of BI 1015550 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Area Under the Concentration-time Curve of BI 764333 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Area Under the Concentration-time Curve of [14-C] BI 1015550-EQ in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Maximum Measured Concentration of BI 1015550 in Plasma (Cmax)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Maximum Measured Concentration of BI 764333 in Plasma (Cmax)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Maximum Measured Concentration of [14-C] BI 1015550-EQ in Plasma (Cmax)(Within 2 hours (h) before drug administration and 30 minutes (min), 45 min, 1h, 1h 30 min, 2h, 4h, 8h, 12h, 24h, 36h, 48h, 96h, 144h, 168h, 192h and 216h after drug administration.)
- Percentage of Participants With Treatment-emergent Adverse Events (TEAE)(From the first administration of the trial drug until end of the trial, up to 31 days.)