Bosutinib (Bosulif)

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.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org 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, UpToDate Lexidrug, Medscape, or the package insert.

Diseases for which it is used

• Chronic myeloid leukemia (CML)
  • Chronic myeloid leukemia, pediatric
• Ph+ B-cell ALL

Patient drug information

• Bosutinib (Bosulif) package insert
• Bosutinib (Bosulif) patient drug information (Chemocare)
• Bosutinib (Bosulif) patient drug information (UpToDate)

History of changes in FDA indication

• 2012-09-04: Initial 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. (Based on Study 200)
• 2017-12-19: Accelerated approval for treatment of patients with newly-diagnosed chronic phase (CP) Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML). (Based on BFORE)
  • 2021-05-14: Converted to regular approval. (Based on BFORE)
• 2023-09-26: Approved for pediatric patients 1 year of age and older with chronic phase (CP) Ph+ chronic myelogenous leukemia (CML) that is newly diagnosed (ND) or resistant or intolerant (R/I) to prior therapy. (Based on BCHILD)

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

• 2014-09-26: Initial approval for the treatment of chronic myelogenous leukemia with resistance or intolerance to prior drug therapies.
• 2020-06-29: New indication and a new dosage for the treatment of newly-diagnosed chronic phase chronic myeloid leukemia.

Also known as

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