In June 2006, the tyrosine kinase inhibitor dasatinib (Sprycel; Bristol-Myers Squibb) was approved by the US FDA for the treatment of adults with chronic myeloid leukaemia and Philadelphia-chromosome-positive acute lymphoblastic leukaemia with resistance or intolerance to previous therapy, including the kinase inhibitor imatinib (Gleevec; Novartis).
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References
Sawyers, C. L. Chronic myeloid leukemia. N. Engl. J. Med. 340, 1330–1340 (1999).
Capdeville, R. et al. Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nature Rev. Drug Discov. 1, 493–502 (2002).
Shah, N. P. et al. Multiple BCR–ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2, 117–125 (2002).
Shah, N. P. et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 305, 399–401 (2004).
Lombardo, L. J. et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J. Med. Chem. 47, 6658–6661 (2004).
Tokarski, J. S. et al. The structure of dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res. 66, 5790–5797 (2006).
Talpaz, M. et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N. Engl. J. Med. 354, 2531–2541 (2006).
FDA labelling information, [online] (2006).
Ptasznik, A. et al. Short interfering RNA (siRNA) targeting the Lyn kinase induces apoptosis in primary, and drug-resistant, BCR–ABL1(+) leukemia cells. Nature Med. 10, 1187–1189 (2004).
Donato, N. J. et al. BCR–ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571. Blood 101, 690–698 (2003).
Druker, B. J. et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of BCR–ABL positive cells. Nature Med. 2, 561–566 (1996).
Kantarjian, H. et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N. Engl. J. Med. 354, 2542–2551 (2006).
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Kantarjian, H., Jabbour, E., Grimley, J. et al. Dasatinib. Nat Rev Drug Discov 5, 717–718 (2006). https://doi.org/10.1038/nrd2135
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DOI: https://doi.org/10.1038/nrd2135
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