Healthy
Conditions
Keywords
palbociclib, PD-0332991, rifampin, drug-drug interaction study
Brief summary
This study will compare the plasma pharmacokinetics of a single 125mg oral dose of palbociclib in the presence and absence of rifampin-mediated enzyme induction in a fixed-sequence two-period study.
Interventions
DRUGPalbociclib
In period 1, patients will receive a single 125mg oral dose of palbociclib alone. Subjects will undergo palbociclib pharmacokinetic sampling at prespecified time points up to 120 hours post palbociclib dose. In period 2, subjects will receive 12 daily oral doses of 600mg of rifampin and a single 125mg oral dose of palbociclib on day 8. Subjects will undergo palbociclib pharmacokinetic sampling at prespecified time points up to 120 hours post palbociclib dose.
DRUGRifampin
In period 2, subjects will receive 12 daily oral doses of 600mg of rifampin and a single 125mg oral dose of palbociclib on day 8. Subjects will undergo palbociclib pharmacokinetic sampling at prespecified time points up to 120 hours post palbociclib dose.
Sponsors
Pfizer
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males or females of non-childbearing potential * body mass index between 17.5-30.5 kg/m2 with a total body weight greater than 50kg
Exclusion criteria
* Evidence or history of any clinically significant physiologic, psychological, or medical conditions * a positive drug screen or alcohol breath test * a baseline ECG demonstrating a QTc\>450msecs or a QRS interval \>120msecs
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)] | 0-120 hours post-dose | 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). |
| Maximum Observed Plasma Concentration (Cmax) | 0-120 hours post-dose | — |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Plasma Decay Half-Life (t1/2) | 0-120 hours post-dose | Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. |
| Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) | 0-120 hours post-dose | Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) |
| Apparent Volume of Distribution (Vz/F) | 0-120 hours post-dose | 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. |
| Apparent Oral Clearance (CL/F) | 0-120 hours post-dose | 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 to Reach Maximum Observed Plasma Concentration (Tmax) | 0-120 hours post-dose | — |
Countries
United States
Outcome results
None listed