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Completed

NCT Number: NCT01082380

Radiolabeled [14C]PF-02341066 Study To Investigate The Absorption, Metabolism And Excretion In Healthy Male Volunteers

The rationale for this study is to investigate the absorption, metabolism and excretion of [14C]PF 02341066 and characterize plasma, fecal and urinary radioactivity, and identify any metabolites, if possible, of [14C]PF 02341066 in humans.

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Key information

Conditions

Healthy Volunteer

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Pfizer Investigational Site

New Haven, Connecticut, 06511, United States

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Healthy male subjects between the ages of 18 and 55 years, 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/m^2; and a total body weight >50 kg (110 lbs).

Exclusion criteria

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Any condition possibly affecting drug absorption (eg, gastrectomy).
  • A positive urine drug screen.

Treatment and study plan

PF-02341066

Drug

oral suspension, single 250 mg dose of PF 02341066 containing approximately 100 µCi of [14C]PF 02341066

Other names: crizotinib

Primary outcomes

  1. Maximum Observed Plasma Concentration (Cmax)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hours (hrs), 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

  2. Time to Reach Maximum Observed Plasma Concentration (Tmax)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

  3. Area Under the Curve From Time Zero to Last Quantifiable Plasma Concentration (AUClast)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Area under the concentration time-curve from zero to the last measured plasma concentration (AUClast).

  4. Area Under the Plasma Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).

  5. Plasma Decay Half Life (t1/2)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Plasma Decay half-life is the time measured for the concentration to decrease by one half.

  6. Apparent Oral Clearance (CL/F) of Plasma PF-02341066

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed.

  7. Apparent Volume of Distribution (V/F) in Plasma

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed.

  8. Renal Clearance (CLr) of PF-02341066

    Time frame: Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose

    CLr is the volume of plasma from which a substance is completely removed by the kidney in a given amount of time.

  9. Total Amount of Unchanged Drug Excreted in the Urine From Time Zero to Infinite Time (Ae)

    Time frame: Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose

    Ae = concentration of unchanged drug excreted in the urine multiplied by volume of unchanged drug excreted in urine.

  10. Total Amount of Unchanged Drug Excreted in the Urine Expressed as Percent of Dose From Time Zero to Infinite Time [Ae(%)]

    Time frame: Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose

  11. Maximum Observed Concentration in Plasma Radioactivity (Cmax)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  12. Time to Reach Maximum Observed Plasma Radioactivity Concentration (Tmax)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  13. Area Under the Curve From Time Zero to Last Quantifiable Plasma Radioactivity Concentration (AUClast)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Area under the concentration time-curve from zero to the last measured plasma concentration. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  14. Area Under the Plasma Radioactivity Concentration Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in plasma. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  15. Decay Half Life (t1/2) of Radioactivity in Plasma

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Plasma decay half-life is the time measured for the plasma radioactivity concentration to decrease by one half. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  16. Apparent Oral Clearance (CL/F) of Plasma Radioactivity

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  17. Apparent Volume of Distribution (V/F) in Plasma Radioactivity

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  18. Maximum Observed Concentration of Radioactivity in Whole Blood (Cmax)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  19. Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in Whole Blood

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Time to Reach Maximum Observed Concentration (Tmax) of Radioactivity in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  20. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Radioactivity in Whole Blood

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Area under the concentration time-curve from zero to the last measured concentration (AUClast) in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  21. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Radioactivity in Whole Blood

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Area under the concentration curve from time zero to extrapolated infinite time [AUC (0 - ∞)] in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  22. Decay Half-life (t1/2) of Radioactivity in Whole Blood

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Decay half life (t1/2) is the time measured for the concentration to decrease by one half in whole blood. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  23. Apparent Oral Clearance of Radioactivity From Whole Blood (CL/F)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  24. Apparent Volume of Distribution of Radioactivity in Whole Blood (V/F)

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (V/F) is influenced by the fraction absorbed. Radioactivity corresponds to 100 μCi [14C]PF-02341066.

  25. Total [14C] Data in Urine

    Time frame: Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose

    Cumulative amount excreted in urine at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066.

  26. Total [14C] Data in Feces

    Time frame: From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose

    Cumulative amount excreted in feces at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066.

  27. Overall Cumulative Percent Recovery of Radioactivity

    Time frame: Pre-dose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose for urine and Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose for feces

    Overall cumulative percent of radioactive dose recovered in urine, feces and toilet tissue at specified intervals after administration of a single 250-mg (100 μCi) oral dose of [14C]PF-02341066.

  28. Identification and Profiling of Metabolites of [14C]PF-02341066 in Plasma

    Time frame: Pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24 hrs, 36 hrs, 48 hrs, then after every 24 hrs until up to 480 hrs post-dose

    Identification was done by Radio-High Performance liquid chromatography (HPLC) chromatogram. Relative abundance (profiling) of metabolites in chromatogram were determined by dividing sum of radioactive content of fractions contributing to particular peak by sum of radioactive content of all fractions constructing the radio chromatogram. Metabolites accounting for an average of greater than or equal to (>=) 10% of total recoverable radioactivity in plasma were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066.

  29. Identification and Profiling of Metabolites of [14C]PF-02341066 in Feces

    Time frame: From Day 0 through pre-dose (Day1) and as passed through until up to 480 hrs post-dose

    In feces, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066.

  30. Identification and Profiling of Metabolites of [14C]PF-02341066 in Urine

    Time frame: Predose, 0 to 4, 4 to 8, 8 to 16, 16 to 24 to 36, 36 to 48 hrs and then after every 24 hrs until up to 480 hrs post-dose

    In urine, metabolite abundance (profiling) was calculated by multiplying the fractional contribution of radioactive response for the peak in the Radio-HPLC chromatogram to the total radioactivity detected by the percent of administered dose recovered in the matrix. Only those metabolites that were a component of a chromatographic peak that accounted for an average of >=1% of the administered dose, were summarized. Radioactivity corresponds to 100 μCi [14C] PF-02341066.

Sponsors and collaborators

Lead sponsor

Pfizer

Industry

Registry information

Official study title

A Phase One Open-Label Single-Radiolabeled Dose Study To Investigate The Absorption, Metabolism And Excretion Of [14C]PF-02341066 In Healthy Male Volunteers

Important dates

Study start
2010
Primary completion
2010
Study completion
2010
First posted
Mar 8, 2010
Registry last updated
Feb 29, 2012

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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