A revolution in medical science was marked with the advent of imatinib, a site-specific drug for the management of patients with chronic myeloid leukemia (CML). Imatinib mesylate (also known as Glivec, Gleevec, STI-571, CGP57148), an orally administered 2-phenylaminopyrimidine derivative approved by FDA in 2001 for the treatment for CML, is highly effective in treating the early stages of CML, but remission induced in advanced phase was observed to be relatively short-lived. The primary cause of resistance in patients with CML is the mutations in the BCR-ABL kinase domain. This review discusses the different mechanisms leading to imatinib resistance and various treatment options to over-ride imatinib resistance.
© 2011 John Wiley & Sons A/S.