A Study In Japanese Healthy Male Volunteers To Investigate The Safety, Tolerability And Pharmacokinetics Of PF-02341066

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: PF-02341066

• Registration Number: NCT01250730
• Lead Sponsor: Pfizer

Brief Summary

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.

Detailed Description

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.

Study Timeline

• Study First Submitted: 2010-11-17
• Study First Submitted QC: 2010-11-29
• Study Start: 2010-12
• Study First Posted: 2010-12-01
• Primary Completion: 2011-01
• Study Completion: 2011-01
• Status Verified: 2011-10
• Results First Submitted: 2011-10-20
• Results First Submitted QC: 2011-10-20
• Last Update Submitted: 2011-10-20
• Results First Posted: 2011-11-29
• Last Update Posted: 2011-11-29

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 18

Inclusion Criteria

• 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

Exclusion Criteria

• 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

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
1.0	PF-02341066	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).

Primary Outcome Measures

Name	Time	Method
Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time [AUC(0-inf)] of Crizotinib	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	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	0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose
Time to Cmax (Tmax) of Crizotinib	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	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	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	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	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	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	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)	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.
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)	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 Plasma Active Metabolite (PF-06260182)	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)	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)	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	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	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.

Trial Locations

Locations (1)

Pfizer Investigational Site; 🇯🇵 Hachioji-shi, Tokyo, Japan