A Phase 1, Open-label, 3-period, Randomized, Partially Fixed Sequence, 2-way Crossover Study With A Microdose Of [11c]Pf-06427878 Administered With And Without Two Non-radioactive Doses Of Pf-06427878 To Characterize Tissue Distribution Using Positron Emission Tomography In Healthy Adult Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Pfizer
- 入组人数
- 8
- 试验地点
- 3
- 主要终点
- Percent injected radioactivity (per gram) over time in the liver
研究概览
简要总结
In this study, radioactive PF-06427878 will be administered, through a vein, alone and with 2 different oral doses of non-radioactive PF-06427878 to healthy, adult, male subjects. Positron emission tomography will be used to characterize tissue distribution. The study will also characterize how the study drug behaves in the body, its safety, and how the body tolerates it.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 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
- •healthy males
- •body mass index 17.5-30.5 kg/m2 ; body weight >50 kg
- •signed and dated informed consent document
- •willing and able to comply with study requirements
排除标准
- •tobacco/nicotine containing products > equivalent of 5 cigarettes per day
- •history of cumulative ionizing radiation exposure in the past year, including anticipated exposure in this study, and subjects with current, past or anticipated exposure to radiation in the workplace
- •severe claustrophobia
- •unable to lie still for the required period to acquire images
研究组 & 干预措施
[11C]PF-06427878
Single intravenous infusion of [11C]PF-06427878 in Periods 1, 2 and 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability
干预措施: [11C]PF-06427878 (Drug)
PF-06427878 10 mg
Single oral dose of 10 mg PF-06427878 in Period 2 or 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability
干预措施: PF-06427878 10 mg (Drug)
PF-06427878 600 mg
Single oral dose of 600 mg PF-06427878 in Period 2 or 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability
干预措施: PF-06427878 600 mg (Drug)
结局指标
主要结局
Percent injected radioactivity (per gram) over time in the liver
时间窗: All Periods;Day 1;0-120min
Percent injected radioactivity (per gram) over time in the plasma
时间窗: All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min
次要结局
- Relative radioactivity in liver versus plasma(All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the gall bladder, if this region is identifiable(All Periods;Day 1;0-2hr)
- Plasma PK of PF-06427878: AUClast, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: AUClast, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the biliary tree, if this region is identifiable(All Periods;Day 1;0-2hr)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the abdominal fat, if this region is identifiable(All Periods;Day 1;0-2hr)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the kidney, if this region is identifiable(All Periods;Day 1;0-2hr)
- % of parent in plasma over time(All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min)
- Plasma PK of PF-06427878: AUCinf, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: Cmax, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: Tmax, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: t½, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: CL, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Plasma PK of PF-06427878: Vss, as data permit(Period 1;Day 1;0,3,5,15,30,60,90,120,135min)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the urinary bladder, if this region is identifiable(All Periods;Day 1;0-2hr)
- Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the thigh muscle, if this region is identifiable(All Periods;Day 1;0-2hr)
- Plasma PK of PF-06427878: Vss, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Plasma PK of PF-06427878: AUCinf, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Plasma PK of PF-06427878: Cmax, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Plasma PK of PF-06427878: Tmax, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Plasma PK of PF-06427878: t½, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)
- Plasma PK of PF-06427878: CL/F, as data permit.(Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min)