Clinical trial NCT01756768: A Single-Radiolabeled Dose Mass Balance Study To Investigate The Absorption, Metabolism, And Excretion Of [14C] Palbociclib (PD-0332991) In Healthy Male Volunteers
Official 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Phase 1
Mass Balance study
Radio-labeled dose
PD-0332991
Lead sponsor: Pfizer
Sponsor class: INDUSTRY
First posted: 2012-12-27
Enrollment: 6
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

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.


Eligibility criteria: 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).

Primary outcomes:
measure: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PD-0332991
timeFrame: 0-192 hrs
measure: Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PD-0332991
timeFrame: 0-192hrs
measure: Maximum Observed Plasma Concentration (Cmax) of PD-0332991
timeFrame: 1-24hrs
measure: Time to Reach Maximum Observed Plasma Concentration (Tmax) of PD-0332991
timeFrame: 1-24hrs
measure: Plasma Decay Half-Life (t1/2) of PD-0332991
timeFrame: 0-192hrs
measure: Apparent Oral Clearance (CL/F) of PD-0332991
timeFrame: 0-192hrs
measure: Apparent Volume of Distribution (Vz/F) of PD-0332991
timeFrame: 0-192hrs
measure: Cumulative radioactivity recovery in urine.
timeFrame: 0-192hrs
measure: Cumulative radioactivity recovery in feces.
timeFrame: 0-192hrs
Secondary outcomes:
measure: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of PF-05089326.
timeFrame: 0-192hrs
measure: Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-05089326.
timeFrame: 0-192hrs
measure: Maximum Observed Plasma Concentration (Cmax) of PF-05089326.
timeFrame: 0-192hrs
measure: Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-05089326.
timeFrame: 0-192hrs
measure: Plasma Decay Half-Life (t1/2) of PF-05089326.
timeFrame: 0-192hrs
measure: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Maximum Observed Concentration (Cmax) of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Time to Reach Maximum Observed Concentration (Tmax) of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Plasma Decay Half-Life (t1/2) of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Apparent Oral Clearance (CL/F) of radioactivity in plasma.
timeFrame: 0-192hrs
measure: Apparent Volume of Distribution (Vz/F) of radioactivity in plasma.
timeFrame: 0-192 hrs
Other outcomes:
Locations:
city: Tacoma
country: United States
facility: Pfizer Investigational Site
state: Washington
Study officials:
affiliation: Pfizer
name: Pfizer CT.gov Call Center
role: STUDY_DIRECTOR
References: