The role of the tyrosine kinase inhibitor STI571 in the treatment of cancer.
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.
Leukemia Program, Oregon Health Sciences University L592, 3181 SW Sam Jackson Park Road, Portland, OR 97201, USA. drukerb@ohsu.edu
M E
ME
O'Dwyer
B J
BJ
Druker
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D001549:Benzamides; D002986:Clinical Trials as Topic; D015195:Drug Design; D004341:Drug Evaluation; D004791:Enzyme Inhibitors / Q000627:therapeutic use*; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics; D010879:Piperazines / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011743:Pyrimidines / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D001549:Benzamides; D004791:Enzyme Inhibitors; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases; D016044:Fusion Proteins, bcr-abl