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A Study To Compare Pharmacokinetics Of Dacomitinib (PF-00299804) Between Healthy Subjects And Subjects With Mild And Moderate Hepatic Impairment

Phase 1
Completed
Conditions
Healthy
Otherwise Healthy Volunteers With Mild or Moderate Hepatic Dysfunction
Interventions
Registration Number
NCT01571388
Lead Sponsor
Pfizer
Brief Summary

The study will determine if there are differences in how dacomitinib is absorbed and eliminated between healthy subjects and subjects with mild and moderately impaired hepatic function.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
25
Inclusion Criteria
  • Healthy male and/or female subjects of non-childbearing potential between the ages of 18 years of age to <75 years of age. Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests. Liver function tests, albumin and prothrombin time must be within normal range.

  • Body Mass Index (BMI) of 18 to 35 kg/m2;

  • An informed consent document signed and dated by the subject.

  • Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.

  • Subjects in the normal hepatic function group (Group 1): No known or suspected hepatic impairment.

  • For subjects in the hepatic impairment groups (Groups 2 and 3):

    • Should satisfy the criteria for Class A or B of the modified Child-Pugh classification
    • A diagnosis of hepatic dysfunction due to hepatocellular disease (and not secondary to any acute ongoing hepatocellular process) documented by medical history, physical examination, liver biopsy, hepatic ultrasound, CT scan, or MRI.
    • Stable hepatic impairment, defined as no clinically significant change in disease status within the last 30 days, as documented by the subject's recent medical history
    • Must be on a stable dose of medication and/or treatment regimen.
Exclusion Criteria
  • Any condition possibly affecting drug absorption (eg, gastrectomy, chronic diarrhea, rapid transit).

  • A positive urine drug screen.

  • Females of childbearing potential, including those with tubal ligation. [To be considered for enrollment, women of at least 45 years of age who are postmenopausal (defined as being amenorrheic for at least 2 years) must have confirmatory FSH test results at screening].

  • In addition, subjects in the hepatic impairment groups (Groups 2 and 3) presenting with any of the following will not be included in the trial:

    • Hepatic carcinoma and hepatorenal syndrome or life expectancy <1 year.
    • Undergone porta-caval shunt surgery.
    • History of gastrointestinal hemorrhage due to esophageal varices or peptic ulcers less than one month prior to study entry.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Group 1dacomitinibHealthy Subjects to receive dacomitinib
Group 2dacomitinibSubjects with mildly impaired hepatic function to receive dacomitinib
Group 3dacomitinibSubjects with moderately impaired hepatic function to receive dacomitinib
Primary Outcome Measures
NameTimeMethod
Maximum Observed Plasma Concentration (Cmax)2 weeks

Maximal plasma concentration (Cmax) for dacomitinib

Plasma area under plasma concentration-time curve from time zero to time infinity post dose (AUCinf) for dacomitinib2 weeks
Secondary Outcome Measures
NameTimeMethod
Time of first observed maximal plasma concentration (Tmax) for dacomitinib2 weeks
Plasma elimination half life (t1/2) of dacomitinib2 weeks
Apparent plasma clearance (CL/F) of dacomitinib2 weeks
Apparent volume of distribution (Vz/F) of dacomitinib2 weeks
Fraction of unbound dacomitinib in plasma (fu)2 weeks
Unbound apparent plasma clearance (CL/F) of dacomitinib ,2 weeks
Unbound apparent volume of distribution (Vz/F) of dacomitinib2 weeks
Plasma area under plasma concentration-time curve from time zero to time of last quantifiable concentration post dose (AUClast) for PF-051992652 weeks
Overall safety profile as characterized by laboratory abnormalities, observed physical examination, vital signs, ECGs, and adverse event monitoring.6-8 weeks
Maximal unbound plasma concentration (Cmax) for PF-051992652 weeks
Area under the Concentration-Time Curve (AUC);Plasma area under plasma concentration-time curve from time zero to 24 hours post dose (AUC24) for dacomitinib2 weeks

AUC is a measure of the serum concentration of the drug over time. It is used to characterize drug absorption.

Plasma area under plasma concentration-time curve from time zero to 216 hours post dose (AUC216) for dacomitinib2 weeks
Plasma area under plasma concentration-time curve from time zero to time of last quantifiable concentration post dose (AUClast) for dacomitinib2 weeks
Maximal plasma concentration (Cmax) for PF-051992652 weeks
Time of first observed maximal plasma concentration (Tmax) for PF-051992652 weeks
Metabolite ratio for plasma area under plasma concentration-time curve from time zero to time infinity post dose (MRAUCinf)2 weeks
Metabolite ratio for plasma area under plasma concentration-time curve from time zero to time of last quantifiable concentration post dose (MRAUClast)2 weeks
Metabolite ratio for maximal plasma concentration (MRCmax)2 weeks
Fraction of unbound PF-05199265 in plasma (fu)2 weeks
Unbound plasma area under plasma concentration-time curve from time zero to 24 hours post dose (AUC24) for PF-051992652 weeks
Unbound plasma area under plasma concentration-time curve from time zero to 216 hours post dose (AUC216) for PF-051992652 weeks
Unbound plasma area under plasma concentration-time curve from time zero to time of last quantifiable concentration post dose (AUClast) for PF-051992652 weeks
Unbound Plasma area under plasma concentration-time curve from time zero to time infinity post dose (AUCinf) for PF-051992652 weeks
Unbound Plasma area under plasma concentration-time curve from time zero to time infinity post dose (AUCinf) for dacomitinib2 weeks
Unbound plasma area under plasma concentration-time curve from time zero to 24 hours post dose (AUC24) for dacomitinib2 weeks
Unbound plasma area under plasma concentration-time curve from time zero to 216 hours post dose (AUC216) for dacomitinib2 weeks
Unbound plasma area under plasma concentration-time curve from time zero to time of last quantifiable concentration post dose (AUClast) for dacomitinib2 weeks
Maximal unbound plasma concentration (Cmax) for dacomitinib2 weeks
Plasma area under plasma concentration-time curve from time zero to time infinity post dose (AUCinf) for PF-051992652 weeks
Plasma area under plasma concentration-time curve from time zero to 24 hours post dose (AUC24) for PF-051992652 weeks
Plasma area under plasma concentration-time curve from time zero to 216 hours post dose (AUC216) for PF-051992652 weeks

Trial Locations

Locations (1)

Pfizer Investigational Site

🇺🇸

South Miami, Florida, United States

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