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| Systematic (IUPAC) name | |
| 4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamideImatinib (originally STI571) is a drug used to treat certain cancers. It is marketed byNovartis as Gleevec (USA) or Glivec (Europe/Australia/Latin America) as its mesylatesalt, imatinib mesilate (INN).
Imatinib is the first of a new class of drugs that act by specifically inhibiting a certainenzyme – a receptor tyrosine kinase – that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all rapidly dividing cells. Imatinib was a model for other targeted therapies that inhibited this class of enzymes. 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 in white blood cells is locked in its activated form. This causes the excessive proliferation and high white blood cell count which is characteristic of CML. Imatinib binds to the site of tyrosine kinase activity, and prevents its activity, causing tumor cell death (apoptosis). |
