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

This study has been completed.
Sponsor:
ClinicalTrials.gov Identifier:
NCT01250730
First Posted: December 1, 2010
Last Update Posted: November 29, 2011
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
Information provided by (Responsible Party):
Pfizer
  Purpose
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.

Condition Intervention Phase
Healthy Drug: PF-02341066 Phase 1

Study Type: Interventional
Study Design: Intervention Model: Parallel Assignment
Masking: None (Open Label)
Official Title: 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

Further study details as provided by Pfizer:

Primary Outcome Measures:
  • Area Under the Plasma Concentration-time Profile From Time Zero Extrapolated to Infinite Time [AUC(0-inf)] of Crizotinib [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 0, 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, 144 hours post-dose ]
  • Time to Cmax (Tmax) of Crizotinib [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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) [ Time Frame: 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) [ Time Frame: 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) [ Time Frame: 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) [ Time Frame: 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) [ Time Frame: 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 [ Time Frame: 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 [ Time Frame: 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.


Enrollment: 18
Study Start Date: December 2010
Study Completion Date: January 2011
Primary Completion Date: January 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: 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).
Drug: PF-02341066
Cohort 1: a 150 mg single dose of PF-02341066 administered as 1 x 50 mg IRT and 1 x 100 mg IRT.
Other Name: Not Specified
Drug: PF-02341066
Cohort 2: a 250 mg single dose of PF-02341066 administered as 1 x 50 mg IRT and 2 x 100 mg IRTs.
Other Name: Not Specified
Drug: PF-02341066
Cohort 3: a 400 mg single dose of PF-02341066 administered as 4 x 100 mg IRTs.
Other Name: Not Specified

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.
  Eligibility

Information from the National Library of Medicine

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.


Ages Eligible for Study:   20 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

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
  Contacts and Locations
Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01250730


Locations
Japan
Pfizer Investigational Site
Hachioji-shi, Tokyo, Japan
Sponsors and Collaborators
Pfizer
Investigators
Study Director: Pfizer CT.gov Call Center Pfizer
  More Information

Additional Information:
Responsible Party: Pfizer
ClinicalTrials.gov Identifier: NCT01250730     History of Changes
Other Study ID Numbers: A8081022
First Submitted: November 17, 2010
First Posted: December 1, 2010
Results First Submitted: October 20, 2011
Results First Posted: November 29, 2011
Last Update Posted: November 29, 2011
Last Verified: October 2011

Keywords provided by Pfizer:
PK profile in Japanese healthy male volunteers

Additional relevant MeSH terms:
Crizotinib
Protein Kinase Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action