Bosutinib (Bosulif)

FDA approved 9/4/2012. Also known as SKI-606.

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: Oral
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, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the package insert.

Diseases for which it is used

• Chronic myelogenous leukemia (CML)

Clinical trials

• BELA: Bosutinib (BOS) versus imatinib (IM) in patients (pts) with newly diagnosed chronic phase chronic myeloid leukemia (CP CML)
• Study Evaluating SKI-606 (Bosutinib) In Philadelphia Chromosome Positive Leukemias
• Compare Bosutinib To Imatinib In Subjects With Newly Diagnosed Chronic Phase Philadelphia Chromosome Positive CML

Patient drug information

• Bosutinib (Bosulif) package insert pages 14-17