A Phase One Open-Label Single-Radiolabeled Dose Study To Investigate The Absorption, Metabolism, And Excretion Of [14C] PD-0332991 In Healthy Male Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Pfizer
- 入组人数
- 6
- 试验地点
- 2
- 主要终点
- Time to Reach Maximum Observed Plasma Concentration (Tmax) of PD-0332991
研究概览
简要总结
This will be an open-label, single-center study to evaluate the mass-balance and pharmacokinetics of PD-0332991 in approximately 6 healthy male subjects receiving a single oral 125 mg dose of PD-0332991 containing approximately 100 microcuries of [14C]-PD-0332991. Subjects will be checked in to the research unit from approximately 12 hours prior to dosing and remain in house until greater than 90% of the administered radioactivity is collected from bodily excreta or until less than 1% of the administered radioactivity is recovered from excreta on consecutive days. This study will investigate the extent of involvement of the renal and hepatic systems in the elimination of PD-0332991 and will seek to identify the compound's major metabolites.
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
- •A Healthy Male Volunteer between 18 and 55 years of age inclusive
- •A Body Mass Index (BMI) of 17.5 to 30.5 kg/m2 and a total body weight >50kg
- •A signed informed consent document
排除标准
- •Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular,hepatic,psychiatric, neurologic, or allergic disease.
- •A positive urine drug or urine cotinine screen.
- •Concurrent use of herbal or prescription medications or treatment with an investigational drug within 30 days or 5 half-lives preceding first dose of study medication.
- •Subjects whose occupation requires exposure to radiation or monitoring of radiation exposure.
- •Subjects with a history of irregular bowel movements (eg, regular episodes of diarrhea or constipation, irritable bowel syndrome (IBS) or lactose intolerance).
结局指标
主要结局
Time to Reach Maximum Observed Plasma Concentration (Tmax) of PD-0332991
时间窗: 1-24hrs
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PD-0332991
时间窗: 0-192 hrs
AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8).
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PD-0332991
时间窗: 0-192hrs
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)
Cumulative radioactivity recovery in urine.
时间窗: 0-192hrs
Cumulative radioactivity recovered in urine is the percent of the administered radioactive dose that is observed in the cumulative urine samples.
Cumulative radioactivity recovery in feces.
时间窗: 0-192hrs
Cumulative radioactivity recovered in fecal is the percent of the administered radioactive dose that is observed in the cumulative fecal samples.
Maximum Observed Plasma Concentration (Cmax) of PD-0332991
时间窗: 1-24hrs
Plasma Decay Half-Life (t1/2) of PD-0332991
时间窗: 0-192hrs
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Apparent Volume of Distribution (Vz/F) of PD-0332991
时间窗: 0-192hrs
Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.
Apparent Oral Clearance (CL/F) of PD-0332991
时间窗: 0-192hrs
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
次要结局
- Maximum Observed Plasma Concentration (Cmax) of PF-05089326.(0-192hrs)
- Apparent Volume of Distribution (Vz/F) of radioactivity in plasma.(0-192 hrs)
- Maximum Observed Concentration (Cmax) of radioactivity in plasma.(0-192hrs)
- Time to Reach Maximum Observed Concentration (Tmax) of radioactivity in plasma.(0-192hrs)
- Apparent Oral Clearance (CL/F) of radioactivity in plasma.(0-192hrs)
- Plasma Decay Half-Life (t1/2) of PF-05089326.(0-192hrs)
- Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of radioactivity in plasma.(0-192hrs)
- Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of radioactivity in plasma.(0-192hrs)
- Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PF-05089326.(0-192hrs)
- Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05089326.(0-192hrs)
- Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05089326.(0-192hrs)
- Plasma Decay Half-Life (t1/2) of radioactivity in plasma.(0-192hrs)