Protein Kinase Inhibitor; Tyrosine kinase enzymes specific inhibitor
Form:
Free Base
REVIEW Imatinib works by blocking a central tyrosine kinase enzyme, in this case, BCR-ABL from phosphorylating subsequent proteins and initiating the signaling cascade necessary for cancer development. Because the BCR-ABL tyrosine kinase enzyme exists only in cancer cells and not in healthy cells, Imatinib is able to function as a targeted cancer therapy-only cancer cells are killed through the drug''s action. In this regard, Imatinib was one of the first cancer therapies to show the potential for such targeted action and of is often cited as a paradigm for research in cancer therapeutics.
REFERENCES
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Novartis Pharma AG. Gleevec® (imatinib mesylate) tablets prescribing information. East Hanover, NJ; 2006 Sep. Anon. Drugs of choice for cancer. Treat Guidel Med Lett. 2003; 1:41-52
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Goldman, J.M. & Melo, J.V. Chronic myeloid leukemia--advances in biology and new approaches to treatment. N Engl J Med 349, 1451-1464 (2003)
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Fausel, C. Targeted chronic myeloid leukemia therapy: Seeking a cure. Am J Health Syst Pharm 64, S9-15 (2007)
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Stegmeier, F., et al. (2010). Targeted Cancer Therapies in the Twenty-First Century: Lessons From Imatinib. Clin Pharmacol Ther 87(5): 543-552.
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