What do kinase inhibition profiles tell us about tyrosine kinase inhibitors used for the treatment of CML?

Cancer treatment has long been based upon cytotoxic therapies that affect all rapidly dividing cells, and as such, is necessarily associated with significant toxicity. More recently, drugs targeted toward pathways critical for tumor cell survival have been developed. With limited off-target activity, such therapies are expected to be better tolerated than broad-acting cytotoxic chemotherapies. BCR-ABL inhibitors in chronic myeloid leukemia are reviewed as a model to investigate the concept of targeted cancer therapies and evaluate how the kinase inhibition profiles of these agents may contribute to their toxicity profiles.