The SRC-ABL inhibitor bosutinib is one of the five tyrosine kinase inhibitors currently approved for the treatment of Philadelphia chromosome-positive leukemias. Bosutinib has shown activity against all phases of resistant chronic myeloid leukemia that do not harbor the T315I or V299L ABL kinase domain mutations. Bosutinib is overall well tolerated; transient diarrhea is the most common side effect. This article summarizes the pharmacokinetics, pharmacodynamics, safety and efficacy of bosutinib for the treatment of Philadelphia chromosome-positive leukemias.
Dasatinib (DAS) is a well tolerated oral dual SRC inhibitor with remarkable activity against all phases of imatinib-resistant chronic myeloid leukemia (CML). This paper focuses on the activity of DAS in intractable CML, and reviews outcomes of patients enrolled on DAS clinical trials. Safety and tolerability as well as practical tips for management of side-effects, and drug interactions are included.
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