Class/mechanism: Third-generation tyrosine kinase inhibitor of Bcr-Abl, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML. Also inhibits kinases in the Src family, including Src, Lyn, and Hck. Active against many imatinib-resistant mutations (16 of 18 imatinib-resistant forms of Bcr-Abl in murine myeloid cell lines), but not active against the T315I and V299L mutations.
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Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 9/4/2012: Initial FDA approval for "the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy."
- 12/19/2017: Granted FDA accelerated approval for treatment of patients with newly-diagnosed chronic phase (CP) Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML).
Also known as
- Code name: SKI-606
- Brand name: Bosulif