Evaluation Of Hepatic Impairment On AG-013736 Pharmacokinetics
Primary Purpose
Hepatic Insufficiency
Status
Completed
Phase
Phase 1
Locations
United States
Study Type
Interventional
Intervention
AG-013736
AG-013736
AG-013736
Sponsored by
About this trial
This is an interventional treatment trial for Hepatic Insufficiency focused on measuring hepatic impairment
Eligibility Criteria
Inclusion Criteria:
- Diagnosis of reduced hepatic function (Child Pugh Classification A or B)
- Body Mass Index of 18-32 kg/m2
Exclusion Criteria:
- History of febrile illness within 5 days prior to first dose
- Any condition possibly affecting drug absorption (e.g. gastrectomy)
- Positive urine drug screen
Sites / Locations
- Pfizer Investigational Site
- Pfizer Investigational Site
Arms of the Study
Arm 1
Arm 2
Arm 3
Arm Type
Experimental
Experimental
Experimental
Arm Label
Hepatic Function - Mild Impairment
Hepatic Function - Moderate Impairment
Hepatic Function - Normal
Arm Description
Subjects with mild hepatic impairment (Child Pugh class A, score 5-6)
Subjects with moderate hepatic impairment(Child Pugh class B,score 7-9)
Group 1 1) subjects with normal hepatic function
Outcomes
Primary Outcome Measures
Maximum Observed Plasma Concentration (Cmax)
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).
Secondary Outcome Measures
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast).
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Plasma Elimination Half-life (t1/2)
Plasma elimination half-life is the time measured for the plasma concentration to decrease by one half.
Apparent Oral Clearance (CL/F)
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 oral bioavailability. Clearance was estimated from population 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)
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 oral bioavailability.
Fraction of Unbound Drug (fu)
Fraction of unbound drug (fu) is defined as the ratio of unbound drug concentration to the total drug concentration.
Unbound Apparent Oral Clearance (CLu/F)
Clearance of an unbound drug is a measure of the rate at which an unbound drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the oral bioavailability. Unbound drug clearance is a quantitative measure of the rate at which an unbound drug substance is removed from the blood.
Unbound Apparent Volume of Distribution (Vzu/F)
Volume of distribution of unbound drug is defined as the theoretical volume in which the total amount of unbound drug would need to be uniformly distributed to produce the desired plasma concentration of unbound drug. Unbound apparent volume of distribution after oral dose (Vzu/F) is influenced by the oral bioavailability.
Unbound Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)u]
AUC (0 - ∞)u = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞) for unbound drug. It is obtained from AUCu (0 - t) plus AUCu (t - ∞).
Unbound Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastu)
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClastu) for unbound drug.
Unbound Maximum Observed Plasma Concentration (Cmaxu)
Cmaxu is the highest measured unbound plasma concentration during the dosing interval.
Full Information
1. Study Identification
Unique Protocol Identification Number
NCT00692341
Brief Title
Evaluation Of Hepatic Impairment On AG-013736 Pharmacokinetics
Official Title
A Phase 1 Study To Evaluate The Pharmacokinetics Of AG-013736 In Subjects With Impaired Hepatic Function
Study Type
Interventional
2. Study Status
Record Verification Date
April 2012
Overall Recruitment Status
Completed
Study Start Date
May 2008 (undefined)
Primary Completion Date
October 2008 (Actual)
Study Completion Date
October 2008 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Sponsor
Name of the Sponsor
Pfizer
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
This study will evaluate the effects of mild and moderate impairment of hepatic function on the single-dose pharmacokinetics, safety and tolerability of AG-013736.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Hepatic Insufficiency
Keywords
hepatic impairment
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Parallel Assignment
Masking
None (Open Label)
Allocation
Non-Randomized
Enrollment
24 (Actual)
8. Arms, Groups, and Interventions
Arm Title
Hepatic Function - Mild Impairment
Arm Type
Experimental
Arm Description
Subjects with mild hepatic impairment (Child Pugh class A, score 5-6)
Arm Title
Hepatic Function - Moderate Impairment
Arm Type
Experimental
Arm Description
Subjects with moderate hepatic impairment(Child Pugh class B,score 7-9)
Arm Title
Hepatic Function - Normal
Arm Type
Experimental
Arm Description
Group 1
1) subjects with normal hepatic function
Intervention Type
Drug
Intervention Name(s)
AG-013736
Intervention Description
Single oral 5-mg dose of AG-013736, administered as a film-coated, immediate-release tablet.
Intervention Type
Drug
Intervention Name(s)
AG-013736
Intervention Description
Single oral 5-mg dose of AG-013736, administered as a film-coated, immediate-release tablet.
Intervention Type
Drug
Intervention Name(s)
AG-013736
Intervention Description
Single oral 5-mg dose of AG-013736, administered as a film-coated, immediate-release tablet.
Primary Outcome Measure Information:
Title
Maximum Observed Plasma Concentration (Cmax)
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hours (hrs) post-dose
Title
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
Description
AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞).
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Secondary Outcome Measure Information:
Title
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Description
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast).
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Plasma Elimination Half-life (t1/2)
Description
Plasma elimination half-life is the time measured for the plasma concentration to decrease by one half.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Apparent Oral Clearance (CL/F)
Description
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 oral bioavailability. Clearance was estimated from population PK modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Apparent Volume of Distribution (Vz/F)
Description
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 oral bioavailability.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Fraction of Unbound Drug (fu)
Description
Fraction of unbound drug (fu) is defined as the ratio of unbound drug concentration to the total drug concentration.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Unbound Apparent Oral Clearance (CLu/F)
Description
Clearance of an unbound drug is a measure of the rate at which an unbound drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the oral bioavailability. Unbound drug clearance is a quantitative measure of the rate at which an unbound drug substance is removed from the blood.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Unbound Apparent Volume of Distribution (Vzu/F)
Description
Volume of distribution of unbound drug is defined as the theoretical volume in which the total amount of unbound drug would need to be uniformly distributed to produce the desired plasma concentration of unbound drug. Unbound apparent volume of distribution after oral dose (Vzu/F) is influenced by the oral bioavailability.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Unbound Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)u]
Description
AUC (0 - ∞)u = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞) for unbound drug. It is obtained from AUCu (0 - t) plus AUCu (t - ∞).
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Unbound Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastu)
Description
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClastu) for unbound drug.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
Title
Unbound Maximum Observed Plasma Concentration (Cmaxu)
Description
Cmaxu is the highest measured unbound plasma concentration during the dosing interval.
Time Frame
0 (pre-dose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 12, 16, 24, 36, 48, 96 and 144 hrs post-dose
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
Diagnosis of reduced hepatic function (Child Pugh Classification A or B)
Body Mass Index of 18-32 kg/m2
Exclusion Criteria:
History of febrile illness within 5 days prior to first dose
Any condition possibly affecting drug absorption (e.g. gastrectomy)
Positive urine drug screen
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
Pfizer CT.gov Call Center
Organizational Affiliation
Pfizer
Official's Role
Study Director
Facility Information:
Facility Name
Pfizer Investigational Site
City
Miami
State/Province
Florida
ZIP/Postal Code
33169
Country
United States
Facility Name
Pfizer Investigational Site
City
Orlando
State/Province
Florida
ZIP/Postal Code
32809
Country
United States
12. IPD Sharing Statement
Links:
URL
https://trialinfoemail.pfizer.com/pages/landing.aspx?StudyID=A4061036&StudyName=Evaluation%20Of%20Hepatic%20Impairment%20On%20AG-013736%20Pharmacokinetics
Description
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