Bosutinib (Bosulif)

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General information

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.[1][2][3][4]
Route: PO
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the package insert.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

History of changes in EMA indication

  • 2013-03-27: Initial authorization as Bosulif. Bosulif is indicated for the treatment of adult patients with chronic phase (CP), accelerated phase (AP), and blast phase (BP) Philadelphia chromosome positive chronic myelogenous leukaemia (Ph+ CML) previously treated with one or more tyrosine kinase inhibitor(s) and for whom imatinib, nilotinib and dasatinib are not considered appropriate treatment options. (Based on Study 200)
  • 2018-04-23: Extension of Indication to include treatment of adult patients with newly diagnosed Philadelphia Chromosome positive (Ph+) Chronic Phase (CP) Chronic Myelogenous Leukaemia (CML). (Based on BFORE)

History of changes in Health Canada indication

  • 2014-03-07: Initial notice of compliance with conditions for the treatment of chronic, accelerated, or blast phase Ph+ CML in adult patients with resistance or intolerance to prior tyrosine kinase inhibitor therapy, and for whom subsequent treatment with imatinib, nilotinib, and dasatinib is not clinically appropriate.
  • 2017-08-02: Conditions were met

History of changes in PMDA indication

Also known as

  • Code name: SKI-606
  • Brand name: Bosulif