Healthy
Conditions
Keywords
PD-0332991, Absolute Bioavailability Study
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.
Interventions
DRUGOral Drug Formulation of PD-0332991
Treatment A consists of a single 125 mg oral dose of PD-0332991.
DRUGIntravenous Formulation of PD-0332991
Treatment B consists of a 1000 mL intravenous infusion of 50 mg of PD-0332991 administered over 4 hours at a constant rate.
Sponsors
Pfizer
Study design
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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). |
| 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). |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) | 0 to 144 hours | — |
| Dose-Normalized Maximum Observed Plasma Concentration (Cmax) | 0 to 144 hours | The maximum observed plasma concentration divided by the administered dose. |
| Time to Reach Maximum Observed Plasma Concentration (Tmax) | 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. |
| 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) |
| 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 | — |
| 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 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. |
Countries
United Kingdom
Outcome results
None listed