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

NCT01756768 | Completed Phase 1

• 1 other identifier: A5481011
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy

Keywords

Phase 1; Mass Balance study; Radio-labeled dose; PD-0332991

Outcome Measures

Primary Outcomes (9)

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

  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).

  0-192 hrs

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

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

  0-192hrs

• Maximum Observed Plasma Concentration (Cmax) of PD-0332991

  1-24hrs

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

  1-24hrs

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

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

  0-192hrs

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

  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.

  0-192hrs

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

  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.

  0-192hrs

• Cumulative radioactivity recovery in urine.

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

  0-192hrs

• Cumulative radioactivity recovery in feces.

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

  0-192hrs

Secondary Outcomes (12)

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

  0-192hrs

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

  0-192hrs

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

  0-192hrs

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

  0-192hrs

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

  0-192hrs

Study Arms (1)

Radio-labeled Dose Arm

EXPERIMENTAL

Radiation: [14C]-PD-0332991

Interventions

[14C]-PD-0332991 RADIATION

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

Radio-labeled Dose Arm

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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).

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Pfizer Investigational Site

Tacoma, Washington, 98418, United States

Location

Related Links

• To obtain contact information for a study center near you, click here.

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 20, 2012
• First Posted: December 27, 2012
• Study Start: January 1, 2013
• Primary Completion: March 1, 2013
• Study Completion: March 1, 2013
• Last Updated: December 17, 2013

Record last verified: 2013-12

Locations

US (1)