Effect of aprepitant, a moderate CYP3A4 inhibitor, on bosutinib exposure in healthy subjects

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• 作者：Poe-Hirr Hsyu ; Daniela Soriano Pignataro…
• 关键词：Aprepitant ; Bosutinib ; Cytochrome P450 3A4 ; Drug ; drug interactions ; Pharmacokinetics ; Tyrosine kinase inhibitor
• 刊名：European Journal of Clinical Pharmacology
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：73
• 期：1
• 页码：49-56
• 全文大小：
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Pharmacology/Toxicology;
• 出版者：Springer Berlin Heidelberg
• ISSN：1432-1041
• 卷排序：73

文摘

PurposeBosutinib is an oral, dual Src and Abl tyrosine kinase inhibitor (TKI) approved for the treatment of Philadelphia chromosome—positive chronic myeloid leukemia resistant or intolerant to prior TKI therapy. Bosutinib is primarily metabolized by cytochrome P450 (CYP) 3A4, suggesting drug interaction potential with other CYP3A4 modulators. This open-label, randomized, 2-sequence, 2-period crossover study assessed the effect of single-dose aprepitant, a moderate CYP3A4 inhibitor, on the single-dose pharmacokinetic profile of oral bosutinib 500 mg.