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What is the mechanism of action of bosutinib?
Bosutinib (Bosutinib) is a tyrosine kinase inhibitor. Bosutinib inhibits the BCR-ABL kinase that promotes chronic myelogenous leukemia; it is also an inhibitor of Src family kinases including Src, Lyn, and Hck. Bosutinib inhibits 16 of 18 imatinib-resistant forms of BCR-ABL kinase expressed in murine myeloid cell lines. Bosutinib does not inhibit T315I and V299L mutant cells. It was observed in clinical studies that higher bosutinib exposure was associated with a greater likelihood of response and a greater likelihood of safety events. Following a single oral dose of 500 mg bosutinib and ketoconazole, a strong CYP3A inhibitor, bosutinib does not prolong the QT interval to any clinically relevant extent.
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