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Effect Of Modafinil And Pioglitazone On The Pharmacokinetics Of Palbociclib (PD-0332991)

Registration Number
NCT02222441
Lead Sponsor
Pfizer
Brief Summary

This study is designed to evaluate the potential effect of the moderate CYP3A inducer modafinil and the weak CYP3A inducer pioglitazone on the pharmacokinetics of palbociclib.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
14
Inclusion Criteria
  • Healthy male and/or female subjects of non childbearing potential between the ages of 18 and 55 years, inclusive.
  • Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  • Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
  • Subjects who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, and other study procedures.
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease.
  • Any condition possibly affecting drug absorption (eg, gastrectomy).
  • Subjects with a self-reported history of addiction, especially to stimulants.
  • A positive urine drug screen or alcohol breath test.
  • Pregnant female subjects; breastfeeding female subjects; female subjects of childbearing potential; male subjects with partners currently pregnant; male subjects of childbearing potential who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for 90 days after the last dose of investigational product.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Fixed sequence modafinil DDI arm (Cohort 1)Palbociclib plus ModafinilFixed sequence study with treatment A of palbociclib alone, followed by treatment B of palbociclib with modafinil in Cohort 1.
Fixed sequence pioglitazone DDI arm (Cohort 2)Palbociclib plus pioglitazoneFor Cohort 2, fixed sequence study with treatment A of palbociclib alone, followed by treatment C of palbociclib with pioglitazone.
Fixed sequence modafinil DDI arm (Cohort 1)Palbociclib aloneFixed sequence study with treatment A of palbociclib alone, followed by treatment B of palbociclib with modafinil in Cohort 1.
Fixed sequence pioglitazone DDI arm (Cohort 2)Palbociclib aloneFor Cohort 2, fixed sequence study with treatment A of palbociclib alone, followed by treatment C of palbociclib with pioglitazone.
Primary Outcome Measures
NameTimeMethod
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]0-120 hours

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).

Maximum Observed Plasma Concentration (Cmax)0-120 hours
Secondary Outcome Measures
NameTimeMethod
Plasma Palbociclib Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)0 to 120 hours

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

Plasma Palbociclib Time to Reach Maximum Observed Plasma Concentration (Tmax)0 to 120 hours
Plasma Palbociclib Decay Half-Life (t1/2)0 to 120 hours

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

Trough Plasma Concentrations of Modafinil, Modafinil sulfone, pioglitazone, hydroxy derivative of pioglitazone, and keto derivative of pioglitazone0 to 120 hours
Time of last quantifiable concentration for palbociclib0 to 120 hours
Apparent Oral Clearance (CL/F) of Palbociclib0 to 120 hours

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.

Apparent Volume of Distribution (Vz/F) of Palbociclib0 to 120 hours

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.

Trial Locations

Locations (1)

New Haven Clinical Research Unit

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New Haven, Connecticut, United States

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