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Effect Of Itraconazole On The Pharmacokinetics Of Palbociclib

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT02131298
Recruitment Status : Completed
First Posted : May 6, 2014
Last Update Posted : June 30, 2014
Information provided by (Responsible Party):

Brief Summary:
This study is designed to evaluate the potential effect of itraconazole on the pharmacokinetics of palbociclib.

Condition or disease Intervention/treatment Phase
Healthy Drug: Palbociclib Alone Drug: Palbociclib plus itraconazole Phase 1

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 12 participants
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Basic Science
Official Title: A Phase 1, Open-Label, Fixed-Sequence 2-Period Study To Investigate The Effect Of Multiple Doses Of Itraconazole On The Single Dose Pharmacokinetics of Palbociclib (PD-0332991) In Healthy Volunteers
Study Start Date : May 2014
Actual Primary Completion Date : June 2014
Actual Study Completion Date : June 2014

Resource links provided by the National Library of Medicine

Arm Intervention/treatment
Fixed sequence
Fixed sequence study with treatment A of palbociclib alone, followed by treatment B (palbociclib with itraconazole)
Drug: Palbociclib Alone
A single 125 mg dose of palbociclib free base capsule given orally alone in the fed state, followed by 120 hours of PK sample collection
Other Name: Palbociclib, PD-0332991

Drug: Palbociclib plus itraconazole
Itraconazole 200 mg once daily with food for a total of 11 days; on Day 5, a single oral 125 mg dose of palbociclib will be given with itraconazole after a meal, followed by 168 hours of PK sample collection.
Other Name: Palbociclib (PD-0332991); Itraconazole (Sporanox)

Primary Outcome Measures :
  1. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] [ Time Frame: 0 to 168 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).

  2. Maximum Observed Plasma Concentration (Cmax) [ Time Frame: 0 to 168 hours ]

Secondary Outcome Measures :
  1. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) [ Time Frame: 0 to 168 hours ]
    Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)

  2. Time to Reach Maximum Observed Plasma Concentration (Tmax) [ Time Frame: 0 to 168 hours ]
  3. Plasma Decay Half-Life (t1/2) [ Time Frame: 0 to 168 hours ]
    Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.

  4. Apparent Oral Clearance (CL/F) [ Time Frame: 0 to 168 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.

  5. Apparent Volume of Distribution (Vz/F) [ Time Frame: 0 to 168 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.

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy male and/or female subjects of non-childbearing potential between the ages of 18 and 55 years, inclusive.
  • Body mass index 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 diseases.
  • Any condition possibly affecting drug absorption.
  • A positive urine drug screen or alcohol breath test.
  • Pregnant female subjects; breast feeding 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.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT02131298

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United States, Connecticut
Pfizer Investigational Site
New Haven, Connecticut, United States, 06511
Sponsors and Collaborators
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Study Director: Pfizer Call Center Pfizer

Additional Information:
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Responsible Party: Pfizer Identifier: NCT02131298     History of Changes
Other Study ID Numbers: A5481016
First Posted: May 6, 2014    Key Record Dates
Last Update Posted: June 30, 2014
Last Verified: June 2014
Keywords provided by Pfizer:
Drug-Drug Interaction Study
Healthy Volunteers
Additional relevant MeSH terms:
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Antineoplastic Agents
Protein Kinase Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Antifungal Agents
Anti-Infective Agents
14-alpha Demethylase Inhibitors
Cytochrome P-450 Enzyme Inhibitors
Steroid Synthesis Inhibitors
Hormone Antagonists
Hormones, Hormone Substitutes, and Hormone Antagonists
Physiological Effects of Drugs
Cytochrome P-450 CYP3A Inhibitors