The tyrosine kinase inhibitor STI571 exemplifies the successful development of a rationally designed, molecularly targeted therapy for the treatment of cancer. This review details the steps in the development of this agent and highlights why this drug has been so successful in the treatment of chronic myelogenous leukaemia. Future directions including the mechanisms and management of resistance and new therapeutic strategies are discussed. Finally, the literature supporting the use of STI571 in other malignancies, including solid tumors is briefly reviewed.
Keywords: Tyrosine Kinase Inhibitor, myelogenous leukaemia, Ph chromosome, allogeneic stem cell, optimal anti-leukemic effects, myelosuppression, CML blast crisis, Bcr-Abl associated leukemias, chronic myelomonocytic leukemic