A Phase 1, Open Label, Dose Escalation, Single Oral Dose Study In Japanese Healthy Male Volunteers To Investigate The Safety, Tolerability And Pharmacokinetics Of PF-02341066
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Pfizer
- 入组人数
- 18
- 试验地点
- 1
- 主要终点
- Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Plasma Active Metabolite (PF-06260182)
研究概览
简要总结
The purpose of this study is to investigate the pharmacokinetics of single doses of PF-02341066 (150, 250, and 400 mg) in the fasted condition in Japanese healthy male volunteers.
详细描述
The purpose of this study is to investigate the pharmacokinetics of single doses of PF-02341066 (150, 250, and 400 mg) in the fasted condition in Japanese healthy male volunteers.
研究设计
- 研究类型
- Interventional
- 干预模型
- Parallel
- 盲法
- None
入排标准
- 年龄范围
- 20 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subjects, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests).
- •Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg
排除标准
- •Subjects who are smoking,
- •Subjects with evidence of disease,
- •Subjects with conditions affecting absorption,
- •Subjects with treatment with other investigational drug within 30 days,
- •Subjects with history of regular alcohol consumption,
- •Subjects with use of prescription, nonprescription drugs and dietary supplement within 28 days,
- •Subjects with blood donation of approximately 400 mL within 3 months or 200 mL within 1 month prior to dosing
研究组 & 干预措施
1.0
This study will consist of three cohorts: PF-02341066 150 mg treatment group (n = 6), PF-02341066 250 mg treatment group (n = 6) and PF-02341066 400 mg treatment group (n = 6).
干预措施: PF-02341066 (Drug)
结局指标
主要结局
Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Plasma Active Metabolite (PF-06260182)
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method.
Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time [AUC(0-inf)] of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
AUC(0-inf) of crizotinib is estimated from the crizotinib concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant.
Area Under the Plasma Concentration-time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
AUClast of crizotinib is estimated from the crizotinib concentration. It is obtained from Linear/Log trapezoidal method.
Maximum Plasma Concentration (Cmax) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Time to Cmax (Tmax) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Terminal Elimination Half-life (t1/2) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
t1/2 of crizotinib is the time measured for the plasma concentration to decrease by one half. It is obtained from a Loge(2)/kel. Kel = terminal phase elimination rate constant
Apparent Oral Clearance (CL/F) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
CL/F of crizotinib is obtained from a Dose per AUCinf.
Apparent Volume of Distribution (Vz/F) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Vz/F of crizotinib is obtained from a Dose / (AUCinf \*kel). Kel = terminal phase elimination rate constant
Dose Normalized AUC(0-inf) of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Dose normalized (to 150 mg dose) AUC(0-inf) is obtained from AUC(0-inf) / (Dose/150).
Dose Normalized AUClast of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Dose normalized (to 150 mg dose) AUClast is obtained from AUClast / (Dose/150).
Dose Normalized Cmax of Crizotinib
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Dose normalized (to 150 mg dose) Cmax is obtained from Cmax / (Dose/150).
Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time (AUC0-inf) of Plasma Active Metabolite (PF-06260182)
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
AUC(0-inf) of PF-06260182 is estimated from the PF-06260182 concentration. It is obtained from AUClast plus (Clast/kel). AUClast = area under the plasma concentration-time curve from zero time until the last measurable concentration. Clast = the last quantifiable concentration. Kel = terminal phase elimination rate constant.
Maximum Plasma Concentration (Cmax) of Plasma Active Metabolite (PF-06260182)
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Time to Cmax (Tmax) of Plasma Active Metabolite (PF-06260182)
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Metabolite to Parent Ratio AUC(0-inf)
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
The metabolic ratio (MR) is calculated by first converting the AUC(0-inf) for both crizotinib and metabolite (PF-06260182) from mass units to molar units.
Metabolite to Parent Ratio AUClast
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
The metabolic ratio (MR) is calculated by first converting the AUClast for both crizotinib and metabolite (PF-06260182) from mass units to molar units.
Metabolite to Parent Ratio Cmax
时间窗: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
The metabolic ratio (MR) is calculated by first converting the Cmax for both crizotinib and metabolite (PF-06260182) from mass units to molar units.
次要结局
未报告次要终点