Summary:
BCR-ABL, a constitutively active tyrosine kinase, causes chronic myeloid leukaemia (CML). Rational development of drugs
targeting BCR-ABL has significantly improved the treatment of CML. Imatinib (a BCR-ABL tyrosine kinase inhibitor) produces
haematological and cytogenetic remissions across all phases of CML and is the present standard of care. However, imatinib
resistance occurs in a significant proportion of patients and mechanisms of resistance include BCR-ABL mutations and
activation of alternate oncogenic pathways. Dasatinib is a novel, potent, multi-targeted oral kinase inhibitor. Preclinical and
clinical investigations demonstrate that dasatinib effectively overcomes imatinib resistance and has further improved the
treatment of CML.
Key words:
chronic myeloid leukemia – dasatinib – imatinib – transplantation
|