An Open-label Study to Evaluate the Pharmacokinetics of YM178 After Single Oral Administration of 14C-labeled YM178 in Healthy Male Volunteers
概览
- 阶段
- 1 期
- 干预措施
- 14C-labeled YM178
- 疾病 / 适应症
- Metabolic Processes
- 发起方
- Astellas Pharma Europe B.V.
- 入组人数
- 4
- 试验地点
- 1
- 主要终点
- The assessment of pharmacokinetic profile of radioactivity after single-dose administration of 14C-YM178, measured by whole blood and plasma concentration
- 状态
- 已完成
- 最后更新
- 12年前
概览
简要总结
The study aims to assess the routes and the extent of metabolism and excretion of YM178 after a single dose of 14C-radiolabeled YM178 administered as a drinking solution in healthy male volunteers.
详细描述
Four subjects are studied in one group. Each subject stays in the clinic for 6 days, and receives a single oral dose of 14C-labeled YM178. Blood, plasma, urine, feces and expired air are collected for 96h after dosing. If 14C-radioactivity quick counts show that radioactivity in urine or feces is above acceptable limits (ie. \> 50 dpm/ml in urine; \>75 dpm in 400 mg feces) on day 5, subjects are requested to stay in the clinic until the levels decrease. If, after 3 days, radioactivity is still \> 50 dpm/ml in urine and/or \>75 dpm in 400 mg feces, urine and/or feces is collected at home, until the amount of radioactivity decreases.
研究者
入排标准
入选标准
- •Body weight between 60 and 100 kg, and BMI ≤30 kg/m2
排除标准
- •Known or suspected hypersensitivity to β-adrenergic receptor agonists or constituents of the formulations used
- •Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug
- •Any clinically significant history of upper gastrointestinal symptoms (such as nausea, vomiting, abdominal discomfort or upset, or heartburn) in the 4 weeks prior to admission to the Research Unit
- •Any clinically significant history of any other disease or disorder - gastrointestinal, cardiovascular, respiratory, renal, hepatic, neurological, dermatological, psychiatric or metabolic
- •Abnormal pulse rate measurement (\<40 or \>90 bpm) taken by manual counting at the pre-study visit after subject has been resting in supine position for 5 min
- •Abnormal blood pressure measurements taken at the pre-study visit after subject has been resting in supine position for 5 min as follows:
- •Systolic blood pressure \<95 or \>160 mmHg;
- •Diastolic blood pressure \<40 or \>95 mmHg.
- •Positive orthostatic test at screening i.e. any symptoms of dizziness, light-headedness etc. and/or a fall of ≥ 20 mmHg in systolic blood pressure after 2 min standing (preceded by 5 min. supine rest) and/or an increase in pulse rate of ≥ 20 bpm
- •Regular use of any prescribed or OTC (over the counter) drugs except paracetamol up to 3 g/day, in the 4 weeks prior to admission to the Research Unit OR any use of such drugs in the 2 weeks prior to admission to the Research Unit
研究组 & 干预措施
14C-labeled YM178
Single oral administration of 14C-labeled YM178
干预措施: 14C-labeled YM178
结局指标
主要结局
The assessment of pharmacokinetic profile of radioactivity after single-dose administration of 14C-YM178, measured by whole blood and plasma concentration
时间窗: Baseline to Day 5 (optional (Day 6-8) [maximum of 19 assessments]
Cmax, tmax, AUC0-last, AUC0-inf, t1/2 and the blood-to-plasma ratio (Ratio Cb/p)
The excretion rate and cumulative excretion of radioactivity in urine, feces and expired air after single-dose administration of 14C-YM178
时间窗: Baseline to Day 5 (optional (Day 6-8) [maximum of 10 assessments]
The assessment of pharmacokinetic profile of parent YM178 after single-dose administration of 14C-YM178, measured plasma and urine concentration
时间窗: Baseline to Day 5 (optional (Day 6-8) [maximum of 19 assessments]
plasma (Cmax, tmax, AUC0-last, AUC0-inf, t1/2 and Vz/F), urine (Ae0-24, Ae0-last, CLR and % dose excreted)
次要结局
- Safety assessed through Adverse Events, vital signs, laboratory analyses and ECG (electrocardiogram)(Through to Day 19)