14C-ARN-509 Microdose Absolute Bioavailability and Microtracer Absorption, Metabolism, and Excretion Study in Healthy Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 12
- 试验地点
- 1
- 主要终点
- Mass Balance
研究概览
简要总结
This is study in healthy human volunteers to determine the absorption, metabolism, and excretion (AME) profile of ARN-509 as well as its absolute oral bioavailability (BA).
详细描述
Two cohorts of 6 healthy volunteers will be enrolled for the AME and absolute BA parts, respectively. The dose for both cohorts is 240 mg. The expected exposure of the dose is 7-fold lower than the steady state reached in patients with castration-resistant prostate cancer.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 50 Years 至 80 Years（Adult, Older Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Gender : male
- •Age : 50 - 80 years, inclusive
- •Body Mass Index (BMI) : 18.5-30.0 kg/m2
- •Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, "power drinks"), grapefruit (juice) and tobacco products from 48 h prior to entry in the clinical research center until discharge
- •Medical history without major pathology
排除标准
- •Evidence of clinically relevant pathology.
- •Mental handicap.
- •History of relevant drug and/or food allergies.
- •Regular/routine treatment with non-topical medications within 30 days prior to entry into the clinical research center.
- •History of alcohol abuse or drug addiction (including soft drugs like cannabis products).
- •Use of concomitant medication, except for acetaminophen (paracetamol) and topical medications
- •Irregular defecation pattern (less than once per 2 days).
- •Positive drug screen (opiates, methadone, cocaine, amphetamines, cannabinoids, barbiturates, benzodiazepines, and alcohol).
- •Intake of more than 24 units of alcohol per week (one unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits).
- •Positive screen on HBsAg, anti-HCV or anti-HIV 1/
- •Illness within five days prior to drug administration.
研究组 & 干预措施
Part B: 14C labeled ARN-509
Single oral dose of 240 mg ARN-509, followed after 2 hours (at the average tmax of ARN-509) by an oral dose of 240 mg ARN-509 with 37 kBq (1000 nCi) of 14C-ARN-509
干预措施: ARN-509 (Drug)
Part A - 14C labeled ARN-509
Single oral dose of 240 mg ARN-509, followed after 2 hours (at the average tmax of ARN-509) by an intravenous (i.v.) microdose of 100 μg (9.25 kBq, 250 nCi) 14C-ARN-509
干预措施: ARN-509 (Drug)
结局指标
主要结局
Mass Balance
时间窗: 2 months 10 days
To determine the rate and routes of excretion of ARN-509 in urine, feces, and expired air
Absolute Oral Bioavailability
时间窗: 2 months 10 days
To determine absolute oral bioavailability of ARN-509
次要结局
- Metabolite Profile(2 months 10 days)