A Phase I Open-label Study to Investigate the Mass Balance and Biotransformation of a Single Oral 160 mg (100 µCi) Dose of 14C-MDV3100 (ASP9785) 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
- Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Time to reach quantifiable concentrations (tlag)
研究概览
简要总结
A study to investigate the excretion routes of radio-labelled MDV3100.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Basic Science
- 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
- •Body Mass Index within 18.5 to 30.0kg/m2
- •Regular defecation pattern (minimum once per 2 days).
- •Subject must be non-fertile, i.e., surgically sterilized or must practice an adequate contraceptive method to prevent pregnancies as defined in the protocol.
排除标准
- •Known or suspected hypersensitivity to MDV3100, or any components of the formulation used.
- •Any of the liver function tests above the upper limit of normal. A retest to confirm the result may be performed once.
- •Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug (excluding non-active hay fever).
- •Abnormal pulse and/or blood pressure measurements at the pre-study visit as follows: Pulse <40 or >90 bpm; mean systolic blood pressure >140 mmHg ; mean diastolic blood pressure >90 mmHg (blood pressure measurements taken in triplicate after subject has been resting in supine position for 5 min; pulse will be measured automatically).
- •A QTc interval of > 430 ms after repeated measurements (consistently after duplicate measurements), a history of unexplained syncope, cardiac arrest, unexplained cardiac arrhythmias or torsades de pointes, structural heart disease, or a family history of Long QT Syndrome (LQTS).
- •Use of any prescribed or OTC (over-the-counter) drugs (including vitamins, natural and herbal remedies, e.g. St. John's wort) in the 2 weeks prior to admission to the Clinical Unit, except for occasional use of paracetamol (up to 3 g/day).
- •Regular use of any inducer of metabolism (e.g., barbiturates, rifampin) in the 3 months prior to admission to the Clinical Unit.
- •Positive serology test for HBsAg, anti HAV (IgM), anti-HCV or anti-HIV 1+
- •Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton (excluding spinal column)), during work or during participation in a clinical study in the previous year.
研究组 & 干预措施
Single Oral MDV3100 dose
干预措施: MDV3100 (Drug)
结局指标
主要结局
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Time to reach quantifiable concentrations (tlag)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Maximum concentration (Cmax)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Time to attain Cmax (tmax)
时间窗: Day 1 through Day 78 (21 times)
Time to attain Cmax (tmax)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by AUC from the time of dosing to the last measurable concentration (AUC0-t)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by AUC extrapolated to infinity (AUC0-inf)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Terminal Disposition Rate Constant (λz)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent terminal elimination half life (t1/2)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent total body clearance after extra vascular dosing (CL/F)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by Apparent volume of distribution during the terminal phase after extra vascular dosing (Vz/F)
时间窗: Day 1 through Day 78 (21 times)
Assessment of Pharmacokinetic profile of total radioactivity in plasma and whole blood by blood-to-plasma ratio (Ratio Cb/p)
时间窗: Day 1 through Day 78 (21 times)
Assessment of 14C recovery in urine
时间窗: Day 1 through Day 78 (17 times)
Assessment of 14C recovery in feces
时间窗: Day 1 through Day 78 (16 times)
Assessment of total 14C recovery (urine and feces combined) within 24 hours
时间窗: Day 1 through Day 78 (17 times for urine and 16 times for feces)
Assessment of total 14C recovery (urine and feces combined) after Time of last quantifiable concentration (tlast)
时间窗: Day 1 through Day 78 (17 times for urine and 16 times for feces)
Assessment of Pharmacokinetic profile of MDV3100 and metabolites in plasma
时间窗: Day 1 through Day 78 (21 times)
PK of MDV3100, MDPC0001, and MDPC0002 in plasma based on validated LC-MS/MS methods: * In plasma: Cmax, tmax, tlag, AUC0-t, AUC0-inf, λz, t1/2, CL/F (parent only), and Vz/F (parent only) The ratios of AUCMDV3100/AUC14C , AUCMDPC0001/AUCMDV3100 and AUCMDPC0001/AUC14C (and the same for MDPC0002) will be calculated
Assessment of Pharmacokinetic profile of MDV3100 and metabolites in urine
时间窗: Day 1 through Day 78 (17 times)
PK of MDV3100, MDPC0001, and MDPC0002 in urine based on validated LC-MS/MS methods: * In urine: Cumulative amount excreted in urine from time zero to the last measurable concentration after dosing (Ae0-t), Renal clearance (CLR), Percent of dose excreted in urine from time zero to the last measurable concentration after dosing (Ae0-t%), Cumulative amount excreted in urine from time zero extrapolated to infinity (Ae0-inf), Percent of dose excreted in urine from time zero extrapolated to infinity (Ae0-inf%) The ratios of AUCMDV3100/AUC14C , AUCMDPC0001/AUCMDV3100 and AUCMDPC0001/AUC14C (and the same for MDPC0002) will be calculated
Metabolic Profile: Profiling of possible metabolites of MDV3100 in plasma, urine, and feces
时间窗: Day 1 through Day 78 (14 times)
Identification and possible quantification of metabolites in plasma, and if applicable, in urine and feces
次要结局
- Safety as assessed by recording adverse events, laboratory assessments, vital signs and electrocardiograms (ECGs)(Day 1 through Day 78)