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A Study Comparing the Plasma Drug Exposure of an Oral Dose of Palbociclib (PD-0332991) to an Intravenous Dose of Palbociclib (PD-0332991)

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Oral Drug Formulation of PD-0332991
Drug: Intravenous Formulation of PD-0332991
Registration Number
NCT01802476
Lead Sponsor
Pfizer
Brief Summary

The purpose of this study is to determine approximately what percentage of an orally administered dose of PD-0332991 is absorbed from the gastrointestinal tract into the systemic circulation. This approximation is made by comparing the plasma pharmacokinetics of a 125 mg oral dose of PD-0332991 to the plasma pharmacokinetics of a 50 mg intravenous dose of PD-0332991 administered as a 4-hour infusion.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
14
Inclusion Criteria
  1. Healthy male or female of non-childbearing potential between the ages of 18 and 55 years of age.
  2. A body mass index (BMI) between 17.5 and 30.5 kg/m2, and a total body weight greater than 50kg (110 lbs)
Exclusion Criteria
  1. Any condition which could possibly affect drug absorption.
  2. Pregnancy or actively nursing females, or females of childbearing potential.
  3. A positive urine drug screen.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Fixed Sequence Crossover ArmIntravenous Formulation of PD-0332991This study arm consists of a fixed sequence crossover where study subjects will receive Treatment A and following a washout of no less than 10 days will then receive Treatment B. The drug class is a CDK4/6 inhibitor.
Fixed Sequence Crossover ArmOral Drug Formulation of PD-0332991This study arm consists of a fixed sequence crossover where study subjects will receive Treatment A and following a washout of no less than 10 days will then receive Treatment B. The drug class is a CDK4/6 inhibitor.
Primary Outcome Measures
NameTimeMethod
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]0 to 144 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).

Dose-Normalized Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]0 to 144 hours

Dose-Normalized AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8) divided by the administered dose. It is obtained from AUC (0 - t) plus AUC (t - 8).

Secondary Outcome Measures
NameTimeMethod
Time to Reach Maximum Observed Plasma Concentration (Tmax)0 to 144 hours
Systemic Clearance (CL)0 to 144 hours

CL is a quantitative measure of the rate at which a drug substance is removed from the body following an intravenous dose.

Dose-Normalized Maximum Observed Plasma Concentration (Cmax)0 to 144 hours

The maximum observed plasma concentration divided by the administered dose.

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)0 to 144 hours

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

Maximum Observed Plasma Concentration (Cmax)0 to 144 hours
Plasma Decay Half-Life (t1/2)0 to 144 hours

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

Dose-Normalized Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)0 to 144 hours

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) divided by the administered dose.

Apparent Oral Clearance (CL/F)0 to 144 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 after an Oral Dose (Vz/F)0 to 144 hours
Volume of Distribution at Steady State after an IV Infusion (Vss)0 to 144 hours

Trial Locations

Locations (1)

Pfizer Investigational Site

🇬🇧

NOttingham, Nottinghamshire, United Kingdom

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