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Completed

NCT Number: NCT01756768

A Single-Radiolabeled Dose Mass Balance Study To Investigate The Absorption, Metabolism, And Excretion Of [14C] Palbociclib (PD-0332991) In Healthy Male Volunteers

This will be an open-label, single-center study to evaluate the mass-balance and pharmacokinetics of PD-0332991 in approximately 6 healthy male subjects receiving a single oral 125 mg dose of PD-0332991 containing approximately 100 microcuries of [14C]-PD-0332991. Subjects will be checked in to the research unit from approximately 12 hours prior to dosing and remain in house until greater than 90% of the administered radioactivity is collected from bodily excreta or until less than 1% of the administered radioactivity is recovered from excreta on consecutive days. This study will investigate the extent of involvement of the renal and hepatic systems in the elimination of PD-0332991 and will seek to identify the compound's major metabolites.

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Key information

Conditions

Healthy

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Pfizer Investigational Site

Tacoma, Washington, 98418, United States

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • A Healthy Male Volunteer between 18 and 55 years of age inclusive
  • A Body Mass Index (BMI) of 17.5 to 30.5 kg/m2 and a total body weight >50kg
  • A signed informed consent document

Exclusion criteria

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular,hepatic,psychiatric, neurologic, or allergic disease.
  • A positive urine drug or urine cotinine screen.
  • Concurrent use of herbal or prescription medications or treatment with an investigational drug within 30 days or 5 half-lives preceding first dose of study medication.
  • Subjects whose occupation requires exposure to radiation or monitoring of radiation exposure.
  • Subjects with a history of irregular bowel movements (eg, regular episodes of diarrhea or constipation, irritable bowel syndrome (IBS) or lactose intolerance).

Treatment and study plan

[14C]-PD-0332991

Radiation

A single 125 mg oral dose of PD-0332991 containing approximately 100 microcurie of [14C]-PD-0332991.

Primary outcomes

  1. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PD-0332991

    Time frame: 0-192 hrs

    AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8).

  2. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PD-0332991

    Time frame: 0-192hrs

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

  3. Maximum Observed Plasma Concentration (Cmax) of PD-0332991

    Time frame: 1-24hrs

  4. Time to Reach Maximum Observed Plasma Concentration (Tmax) of PD-0332991

    Time frame: 1-24hrs

  5. Plasma Decay Half-Life (t1/2) of PD-0332991

    Time frame: 0-192hrs

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

  6. Apparent Oral Clearance (CL/F) of PD-0332991

    Time frame: 0-192hrs

    Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

  7. Apparent Volume of Distribution (Vz/F) of PD-0332991

    Time frame: 0-192hrs

    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 plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

  8. Cumulative radioactivity recovery in urine.

    Time frame: 0-192hrs

    Cumulative radioactivity recovered in urine is the percent of the administered radioactive dose that is observed in the cumulative urine samples.

  9. Cumulative radioactivity recovery in feces.

    Time frame: 0-192hrs

    Cumulative radioactivity recovered in fecal is the percent of the administered radioactive dose that is observed in the cumulative fecal samples.

Secondary outcomes

  1. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PF-05089326.

    Time frame: 0-192hrs

    AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8).

  2. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05089326.

    Time frame: 0-192hrs

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

  3. Maximum Observed Plasma Concentration (Cmax) of PF-05089326.

    Time frame: 0-192hrs

  4. Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05089326.

    Time frame: 0-192hrs

  5. Plasma Decay Half-Life (t1/2) of PF-05089326.

    Time frame: 0-192hrs

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

  6. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of radioactivity in plasma.

    Time frame: 0-192hrs

    AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8).

  7. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of radioactivity in plasma.

    Time frame: 0-192hrs

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

  8. Maximum Observed Concentration (Cmax) of radioactivity in plasma.

    Time frame: 0-192hrs

  9. Time to Reach Maximum Observed Concentration (Tmax) of radioactivity in plasma.

    Time frame: 0-192hrs

  10. Plasma Decay Half-Life (t1/2) of radioactivity in plasma.

    Time frame: 0-192hrs

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

  11. Apparent Oral Clearance (CL/F) of radioactivity in plasma.

    Time frame: 0-192hrs

    Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

  12. Apparent Volume of Distribution (Vz/F) of radioactivity in plasma.

    Time frame: 0-192 hrs

    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 plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

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] PD-0332991 In Healthy Male Volunteers

Important dates

Study start
2013
Primary completion
2013
Study completion
2013
First posted
Dec 27, 2012
Registry last updated
Dec 17, 2013

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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