This study will investigate the dose-proportionality of palbociclib pharmacokinetics in healthy subjects of Japanese descent. Approximately fourteen healthy Japanese subjects will receive four single doses of palbociclib (PD-0332991) with a minimum washout of 10 days between doses. Additionally, this study will investigate the effect of Japanese ethnicity of palbociclib pharmacokinetics by comparing palbociclib pharmacokinetics at a single dose-level between healthy subjects of Japanese descent and approximately fourteen healthy non-Asian subjects.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
27
In Period 1, Japanese subjects will receive a single oral 75mg dose of palbociclib with food. Serial PK assessments will be collected over the next 120 hours.
In Period 2, Japanese subjects will receive a single oral 125mg dose of palbociclib with food. Serial PK assessments will be collected over the next 120 hours.
In Period 3, Japanese subjects will receive a single oral 100mg dose of palbociclib with food. Serial PK assessments will be collected over the next 120 hours.
In Period 4, Japanese subjects will receive a single oral dose of palbociclib with food. Serial PK assessments will be collected over the next 120 hours. The amount of the dose will be determined based on an interim analysis of the PK data from Periods 1 and 2.
In Period 1, healthy non-Asian subjects will receive a single oral 125mg dose of palbociclib with food. Serial PK assessments will be collected over the next 120 hours.
Pfizer Investigational Site
New Haven, Connecticut, United States
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]
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).
Time frame: 0-120 hours
Dose-normalised Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]
AUC (0 - 8)DN= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8) divided by dose. It is obtained from AUC (0 - t) plus AUC (t - 8) all divided by the administered dose.
Time frame: 0-120 hours
Maximum Observed Plasma Concentration (Cmax)
Time frame: 0-120 hours
Dose-Normalised Maximum Observed Plasma Concentration (Cmax)
Time frame: 0-120 hours
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 frame: 0-120 hours
Dose-Normalized 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), all divided by the administered dose.
Time frame: 0-120 hours
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Time frame: 0-120 hours
Plasma Decay Half-Life (t1/2)
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Time frame: 0-120 hours
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 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.
Time frame: 0-120 hours
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 fraction absorbed.
Time frame: 0-120 hours
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