Metabolism and Pharmacokinetics of [14C]-BIBF 1120 After Administration of Single Doses of 100 mg [14C]-BIBF 1120 Oral Solution in Healthy Male Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 8
- 主要终点
- Maximum observed concentration of the analyte in plasma (Cmax)
研究概览
简要总结
To assess the metabolic profile,
to obtain the mass balance after oral administration,
to determine the concentration of [14C]-radioactivity in blood cells, plasma, urine and faeces,
to determine BIBF 1120 and BIBF 1202 concentrations in plasma, urine, and faeces, if feasible,
to determine the protein binding of [14C]-radioactivity,
to determine the pharmacokinetics of BIBF 1120, BIBF 1202 and total radioactivity after a single oral administration of [14C]-BIBF 1120 in healthy volunteers
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
- 21 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subjects as determined by results of screening
- •Signed written informed consent in accordance with GCP and local legislation
- •Age ≥21 and ≤55 years
- •Body Mass Index ≥18.5 kg/m2 and ≤29.9 kg/m2
排除标准
- •Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
- •History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
- •History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months
- •History of orthostatic hypotension, fainting spells and blackouts
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
- •History of any bleeding disorder including prolonged or habitual bleeding, other haematologic disease or cerebral bleeding (e.g. after a car accident) or commotio cerebri
- •Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
- •Planned use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
- •Participation in another trial with an investigational drug within 2 months prior to administration or during trial
- •Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
- •Alcohol abuse (> 60 g/day)
- •Blood donation within 1 month prior to administration or during the trial
- •Excessive physical activities within 5 days prior to administration or during the trial
- •Any laboratory value outside the reference range, unless considered to lack clinical reference
- •Female gender
- •Male subjects must agree to minimize the risk of female partners becoming pregnant from the dosing day until 3 months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than 3 months prior to dosing, barrier contraception or a medically accepted contraceptive method. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, hormonal contraceptive since at least two months and diaphragm with spermicide
研究组 & 干预措施
BIBF 1120 ES
干预措施: BIBF 1120 ES (Drug)
结局指标
主要结局
Maximum observed concentration of the analyte in plasma (Cmax)
时间窗: Up to 96 h after drug administration
[14C]-radioactivity in plasma and whole blood (C Blood cells/C plasma ratio of [14C]-radioactivity)
时间窗: Up to 96 h after drug administration
[14C]-radioactivity in urine
时间窗: Up to 120 h after drug administration
Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo
时间窗: Up to 96 h after drug administration
Plasma concentration-time profiles of total radioactivity in whole blood and plasma
时间窗: Up to 96 h after drug administration
[14C]-metabolic profile and identification of metabolites in urine, in comparison with various animal species
时间窗: Up to 120 h after drug aministration
[14C]-radioactivity in faeces
时间窗: up to 120 h after administration
[14C]-metabolic profile and identification of metabolites in faeces, in comparison with various animal species
时间窗: Up to 120 h after drug aministration
[14C]-metabolic profile and identification of metabolites in plasma, in comparison with various animal species
时间窗: Up to 96 h after drug aministration
Time from dosing to peak concentration (tmax)
时间窗: Up to 96 h after drug administration
Terminal half-life of the analyte in plasma (t1/2)
时间窗: Up to 96 h after drug administration
Terminal rate constant of the analyte in plasma (λz)
时间窗: Up to 96 h after drug administration
Area under the concentration-time curve of the analyte in plasma from zero time to 24 hours (AUC0-24)
时间窗: Up to 24 h after drug administration
Area under the concentration-time curve of the analyte in plasma from zero time to the time of the last quantifiable drug concentration (AUC0-tz)
时间窗: Up to 96 h after drug administration
Area under the concentration-time curve of the analyte in plasma from zero time to infinity (AUC0-∞)
时间窗: Up to 96 h after drug administration
Mean residence time of the analyte molecules in the body after oral administration (MRTpo)
时间窗: Up to 96 h after drug administration
Total clearance of the analyte in plasma following extravascular administration (CL/F)
时间窗: Up to 96 h after drug administration
Apparent volume of distribution during the terminal phase λz following extravascular administration (Vz/F)
时间窗: Up to 96 h after drug administration
Fraction of analyte eliminated in urine from 0 to the limit of the last quantifiable data point (fe0-tz)
时间窗: Up to 96 h after drug administration
Fraction of analyte eliminated in faeces from 0 to the limit of the last quantifiable data point (fe faeces,0-tz)
时间窗: Up to 96 h after drug administration
Amount of analyte that was eliminated in faeces from 0 to the limit of the last quantifiable data point (Ae faeces,0-tz)
时间窗: Up to 96 h after drug administration
Amount of analyte that was eliminated in urine from 0 to the limit of the last quantifiable data point (Ae0-tz)
时间窗: Up to 96 h after drug administration
次要结局
- Change from baseline in vital signs(Baseline, day 14 after drug administration)
- Change from baseline in routine laboratory(Baseline, day 14 after drug aministration)
- Number of participants with adverse events(Up to day 14 after drug aministration)
- Change from baseline in electrocardiogram(Baseline, day 14 after drug aministration)
- Assessment of tolerability by investigator according a 4 point scale(Day 14 after drug administration)