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Completed

NCT Number: NCT01250730

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

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.

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Key information

Conditions

Healthy

Age range

20 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Pfizer Investigational Site

Hachioji-shi, Tokyo, Japan

About this study

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.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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

Treatment and study plan

PF-02341066

Drug

Cohort 1: a 150 mg single dose of PF-02341066 administered as 1 x 50 mg IRT and 1 x 100 mg IRT.

Primary outcomes

  1. 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.

  2. 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.

  3. 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

  4. 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

  5. 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

  6. 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.

  7. 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

  8. 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).

  9. 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).

  10. 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).

  11. 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.

  12. 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.

  13. 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

  14. 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

  15. 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.

  16. 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.

  17. 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.

Sponsors and collaborators

Lead sponsor

Pfizer

Industry

Registry information

Official study 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

Important dates

Study start
2010
Primary completion
2011
Study completion
2011
First posted
Dec 1, 2010
Registry last updated
Nov 29, 2011

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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