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Imatinib

Imatinib (originally STI571) is a drug used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia/Latin America) as its mesylate salt, imatinib mesilate (INN). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and some other diseases. By 2011, Gleevec has been FDA approved to treat ten different cancers. In CML, the tyrosine kinase enzyme ABL is locked in its activated form. It induces the abnormal phenotypes of CML: excessive proliferation and high white blood cell count. Imatinib binds to the site of tyrosine kinase activity, and prevents its activity, thereby causing tumor cell apoptosis.

Imatinib is the first member of a new class of agents that act by specifically inhibiting a certain enzyme that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all rapidly dividing cells, and served as a model for other targeted therapy modalities through tyrosine kinase inhibition.

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