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

Also known as

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


  1. 1.0 1.1 1.2 Bosutinib (Bosulif) package insert
  2. Bosutinib (Bosulif) package insert (locally hosted backup)
  3. Bosulif manufacturer's website
  4. ASCO Post 2/15/2012: BELA Trial Reborn: Bosutinib Produces Improved Results in Chronic Myeloid Leukemia