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Bosutinib

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bosutinib

(bah-SOO-tih-nib)

A drug used to treat chronic myelogenous leukemia (CML) that is Philadelphia chromosome positive. It is used in some newly diagnosed patients. It is also used in patients who cannot be treated with or have not gotten better after other treatment. It is also being studied in the treatment of other types of cancer. Bosutinib blocks BCR-ABL and other proteins, which may help keep cancer cells from growing. It is a type of tyrosine kinase inhibitor. Also called Bosulif.

Information about Bosutinib

Bosutinib is a dual kinase inhibitor of both the BCR-ABL and Src tyrosine kinases and is used in the therapy of Philadelphia chromosome-positive chronic myelogenous leukemia.    

Liver safety of Bosutinib

Bosutinib therapy is associated with transient elevations in serum aminotransferase and bilirubin levels and rare instances of clinically apparent acute liver injury.

Mechanism of action of Bosutinib

Bosutinib (boe sue’ ti nib) is an orally available, small molecule inhibitor of the BCR-ABL tyrosine kinase receptor, which is the product of a fusion gene resulting from the reciprocal translocations between chromosomes 9 and 22 that characterize the Philadelphia chromosome of chronic myelogenous leukemia (CML).  The abnormal tyrosine kinase receptor is constitutively expressed and causes unregulated cell growth and proliferation in myeloid cells.  Inhibition of the receptor can lead to dramatic reversal of progression of leukemia, although sometimes limited by the development of tumor resistance caused by mutations in the kinase.  Bosutinib was the fourth BCR-ABL tyrosine kinase receptor inhibitor approved for use in cancer chemotherapy (after imatinib, dasatinib and nilotinib) and, like many of the BCR-ABL tyrosine kinase inhibitors, also has some activity against the abnormal tyrosine kinase (c-Kit) that is found in gastrointestinal stromal tumors (GIST).  Bosutinib also has activity against the receptors for platelet derived growth factor (PDGF) and vascular endothelial growth factor (VEGF). 

FDA approval information for Bosutinib

Bosutinib received approval for use in the United States in 2012.  Current indications are for adult patients with Philadelphia chromosome-positive CML in the chronic, accelerated or blast stages and with resistance or intolerance to previous therapy. 

Dosage and administration for Bosutinib

Bosutinib is available in tablets of 100 and 500 mg under the brand name Bosulif.  The typical dose is 500 mg orally once daily, with dose adjustment based upon tolerance and efficacy. 

Side effects of Bosutinib

Side effects include fatigue, nausea, diarrhea, abdominal pain, thrombocytopenia, anemia, fever and rash.  Uncommon, but potentially severe side effects include hypersensitivity reactions, infections and bone marrow suppression

 
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