Healthy
Conditions
Keywords
bosutinib, dabigatran, drug interaction, p-glycoprotein, pharmacokinetics
Brief summary
The study evaluates the effect of a single oral dose of bosutinib on the single dose pharmacokinetics of dabigatran, a p-glycoprotein substrate, in healthy subjects.
Interventions
DRUGDabigatran
Dabigatran 150 mg orally
DRUGBosutinib
Bosutinib 500 mg orally
Sponsors
Pfizer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
21 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy subjects between 21 to 55 years old and BMI between 17.5 and 30.5 kg/m2.
Exclusion criteria
* Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing). * Risks of bleeding including prior personal or familiar history of abnormal bleeding, hereditary or acquired coagulation or platelet disorder or abnormal coagulation test (PT/INR or PTT/aPTT greater than upper limit of normal) result at screening. * Pregnant or nursing females; females of childbearing potential who are unwilling or unable to use an acceptable method of non-hormonal contraception as outlined in this protocol from at least 14 days prior to the first dose of study medication.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) | 48 hours | Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) |
| Maximum Observed Plasma Concentration (Cmax) | 48 hours | Maximum Observed Plasma Concentration |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Plasma Decay Half-Life (t1/2) | 48 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) | 48 hours | Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) |
| Apparent Volume of Distribution (Vz/F) | 48 hours | 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) | 48 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. |
| Time to Reach Maximum Observed Plasma Concentration (Tmax) | 48 hours | Time to Reach Maximum Observed Plasma Concentration |
Countries
United States
Outcome results
None listed