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This is an open label, randomized, single dose, one cohort, two sequence, two period crossover study in healthy subjects. The primary objective of the study is to evaluate the effect of a single oral dose of aprepitant on the pharmacokinetic (PK) profile of a single oral dose of bosutinib in healthy subjects.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Healthy volunteers | Other | Healthy volunteers taking a single dose of bosutinib and a single dose of bosutinib plus aprepitant in random order |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| bosutinib or bosutinib + aprepitant | Drug | Single dose of bosutinib (500 mg) or single dose of bosutinib (500 mg) and aprepitant (125 mg) |
|
| Measure | Description | Time Frame |
|---|---|---|
| Area under the Concentration-Time Curve (AUC) | AUC is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. | 96 hours |
| Maximum Observed Plasma Concentration (Cmax) | Cmax is the peak concentration. | 96 hours |
| Measure | Description | Time Frame |
|---|---|---|
| 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) | 96 hours |
| Time to Reach Maximum Observed Plasma Concentration (Tmax) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Investigational Site | DeLand | Florida | 32720 | United States |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 27718000 | Derived | Hsyu PH, Pignataro DS, Matschke K. Effect of aprepitant, a moderate CYP3A4 inhibitor, on bosutinib exposure in healthy subjects. Eur J Clin Pharmacol. 2017 Jan;73(1):49-56. doi: 10.1007/s00228-016-2108-z. Epub 2016 Oct 7. |
| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| ID | Term |
|---|---|
| D015464 | Leukemia, Myelogenous, Chronic, BCR-ABL Positive |
| ID | Term |
|---|---|
| D007951 | Leukemia, Myeloid |
| D007938 | Leukemia |
| D009370 | Neoplasms by Histologic Type |
| D009369 | Neoplasms |
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| ID | Term |
|---|---|
| C471992 | bosutinib |
| D000077608 | Aprepitant |
| ID | Term |
|---|---|
| D009025 | Morpholines |
| D010078 | Oxazines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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Tmax is measure how fast a drug is absorbed |
| 96 hours |
| Plasma Decay Half-Life (t1/2) | Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. | 96 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. | 96 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. | 96 hours |
| D009196 |
| Myeloproliferative Disorders |
| D001855 | Bone Marrow Diseases |
| D006402 | Hematologic Diseases |
| D006425 | Hemic and Lymphatic Diseases |
| D002908 | Chronic Disease |
| D020969 | Disease Attributes |
| D010335 | Pathologic Processes |
| D013568 | Pathological Conditions, Signs and Symptoms |