Difference between revisions of "Bosutinib (Bosulif)"
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==General information== | ==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.<ref name=insert>[http://labeling.pfizer.com/ShowLabeling.aspx?id=884 Bosutinib (Bosulif) package insert]</ref><ref>[[ | + | 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.<ref name=insert>[http://labeling.pfizer.com/ShowLabeling.aspx?id=884 Bosutinib (Bosulif) package insert]</ref><ref>[[File:Bosutinib.pdf | Bosutinib (Bosulif) package insert (locally hosted backup)]]</ref><ref>[http://www.bosulif.com/ Bosulif manufacturer's website]</ref><ref>[http://www.ascopost.com/issues/february-15-2012-supplement/bela-trial-reborn-bosutinib-produces-improved-results-in-chronic-myeloid-leukemia.aspx ASCO Post 2/15/2012: BELA Trial Reborn: Bosutinib Produces Improved Results in Chronic Myeloid Leukemia]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
Revision as of 00:16, 20 September 2021
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, 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.[1]
Diseases for which it is used
Patient drug information
- Bosutinib (Bosulif) package insert[1]
- Bosutinib (Bosulif) patient drug information (Chemocare)[5]
- Bosutinib (Bosulif) patient drug information (UpToDate)[6]
History of changes in FDA indication
- 9/4/2012: 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 PACE)
- 12/19/2017: Accelerated approval for treatment of patients with newly-diagnosed chronic phase (CP) Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML). (Based on BFORE)
Also known as
- Code name: SKI-606
- Brand name: Bosulif
References
- ↑ 1.0 1.1 1.2 Bosutinib (Bosulif) package insert
- ↑ File:Bosutinib.pdf
- ↑ Bosulif manufacturer's website
- ↑ ASCO Post 2/15/2012: BELA Trial Reborn: Bosutinib Produces Improved Results in Chronic Myeloid Leukemia
- ↑ Bosutinib (Bosulif) patient drug information (Chemocare)
- ↑ Bosutinib (Bosulif) patient drug information (UpToDate)