BTT-30182-bosutinib-in-the-management-of-chronic-myeloid-leukemia-; published by Dove Press

Correspondence: Gunhild Keller-von Amsberg Klinik für Hämatologie und Onkologie mit der Sektion Pneumologie, Onkologisches Zentrum, Universitäts-Klinikum Hamburg-Eppendorf, Martinistraβe 52, 20246 Hamburg, Germany Tel +49 40 74105 3962 Fax +49 40 74105 8054 Email [email protected] Abstract: Bosutinib (SKI-606) is an orally available, once-daily dual Src and Abl kinase inhibitor, approved by the US Food and Drug Administration for the treatment of adults with chronic, accelerated, or blast-phase Philadelphia chromosome-positive chronic myelogenous leukemia who are intolerant of or resistant to firstor second-generation tyrosine kinase inhibitors. Bosutinib effectively overcomes the majority of imatinib-resistance-conferring BCR-ABL mutations except V299L and T315I. In the Bosutinib Efficacy and Safety in chronic myeloid LeukemiA (BELA) trial, bosutinib attained a faster and deeper molecular response than imatinib in newly diagnosed chronic-phase chronic myelogenous leukemia patients. Treatment-emergent adverse events are usually very manageable. Low grade, mostly self-limiting diarrhea represents the most frequently observed toxicity of bosutinib. Anti-diarrheal drugs, antiemetic agents, and/or fluid replacement should be used to treat these patients. The improved hematological toxicity of bosutinib compared with other tyrosine kinase inhibitors has been ascribed to its minimal activity against plateletderived growth factor receptor and KIT. In this review, we give an overview on the profile of bosutinib, the clinical potential and treatment-emergent adverse events.