• Expert Opin Pharmacother · Apr 2014

    Review

    Bosutinib : a review of preclinical and clinical studies in chronic myelogenous leukemia.

    • Francesca Rusconi, Rocco Piazza, Elisabetta Vagge, and Carlo Gambacorti-Passerini.
    • University of Milano-Bicocca, Department of Health Sciences , Via Cadore 48, 20900 Monza , Italy carlo.gambacorti@unimib.it.
    • Expert Opin Pharmacother. 2014 Apr 1; 15 (5): 701-10.

    IntroductionChronic myeloid leukemia (CML) is a hematopoietic stem cell disease. It is characterized by a Bcr-Abl (breakpoint cluster region-Abelson leukemia virus) tyrosine kinase fusion protein produced from the Philadelphia (Ph) chromosome. The tyrosine kinase inhibitor (TKI) imatinib was the first targeted therapy licensed for patients with chronic-phase CML. In recent years, many other TKIs have been approved for the treatment of patients with CML. For this reason, the choice of the best strategy treatment has become increasingly complex.Areas CoveredBosutinib , a dual Src/Abl kinase inhibitor, has shown potent activity against CML and it has been approved by the US FDA for the treatment of chronic, accelerated or blast-phase Ph+ CML. This review was conducted to describe the preclinical and clinical activity of bosutinib and the safety and tolerability of the drug in the treatment of CML. Included studies were identified through a search of electronic databases in July 2013 and relevant conference proceedings.Expert OpinionImatinib continues to represent the treatment of choice for CML. However, some patients develop resistance or intolerance to imatinib or to other second-generation TKIs. Bosutinib shows a good therapeutic activity with a benign safety profile, no cardiovascular toxicity, and offers an important therapeutic addition to the armamentarium that physicians can use against resistant CML.

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