imatinib
Imatinib mesylate (STI 571, Gleevec) is an inhibitor of the tyrosine kinases c-kit, PDGFR and the fusion protein BCR/ABL. Imatinib also blocks the stem cell factor SCF receptor or c-KIT loop.
Imatinib is a small-molecule ABL kinase inhibitor. It is a highly effective therapy for early-phase chronic myeloid leukaemia (CML), which has constitutively active ABL kinase activity owing to the expression of the BCR-ABL fusion protein.
Therapeutics
significant response in patients with chronic myelogenous leukemia and gastrointestinal stromal tumor (GIST)
Videos
Gleevec action
Gleevec mechanism of Action
References
O’hare T, Corbin AS, Druker BJ. Targeted CML therapy: controlling drug resistance, seeking cure. Curr Opin Genet Dev. 2006 Feb;16(1):92-9. PMID: 16343892
Klein S, McCormick F, Levitzki A. Killing time for cancer cells. Nat Rev Cancer. 2005 Jul;5(7):573-80. PMID: 15965492
Mohty M, Blaise D, Olive D, Gaugler B. Imatinib: the narrow line between immune tolerance and activation. Trends Mol Med. 2005 Sep;11(9):397-402. PMID: 16087402
Hannah AL. Kinases as drug discovery targets in hematologic malignancies. Curr Mol Med. 2005 Nov;5(7):625-42. PMID: 16305489
Savage DG, Antman KH. Imatinib mesylate—a new oral targeted therapy. N Engl J Med. 2002 Feb 28;346(9):683-93. PMID: 11870247