Imatinib

Imatinib (originally STI571) is a drug used to treat certain cancers. It is marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia/Latin America) as its mesylate salt, imatinib mesilate (INN).

Imatinib is the first of a new class of drugs that act by specifically inhibiting a certain enzyme (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 constantly (constitutively) expressed. 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).

The developers of imatinib won the Lasker Award in 2009 and the Japan Prize in 2012.

Read more about ImatinibHistory, Adverse Effects, Interactions, Costs

Other articles related to "imatinib":

History Of Cancer Chemotherapy - Targeted Therapy - Tyrosine Kinase Inhibitors
... Bcr-Abl tyrosine kinase inhibitors The classic example of targeted development is imatinib mesylate (Gleevec), a small molecule which inhibits a signaling molecule kinase ... Imatinib precisely inhibits this kinase ... From these, imatinib was found to have the most promise in laboratory experiments ...
Nilotinib - Pharmacology
... binding potency 30 times greater than imatinib in imatinib-resistant cells, and 5-7 times greater than imatinib in imatinib-susceptible leukemic cells ... affinity is not established in patients with imatinib-susceptible disease ...
Chordoma - Prognosis and Treatment
... chordoma, however a clinical trial conducted in Italy using the PDGFR inhibitor Imatinib demonstrated a modest response in some chordoma patients ... group in Italy found that the combination of imatinib and sirolimus caused a response in several patients whose tumors progressed on imatinib alone ...
Imatinib - Costs - Legal Challenge To Generics
... In 2007, imatinib became a test case through which Novartis challenged India's patent laws ... A win for Novartis would make it harder for Indian companies to produce generic versions of drugs still manufactured under patent elsewhere in the world ...
Sunitinib - Indications - Gastrointestinal Stromal Tumor
... Imatinib was the first cancer agent proven effective for metastatic GIST and represented a major development in the treatment of this rare but challenging disease. 20% of patients do not respond to imatinib (early or primary resistance), and among those who do respond initially, 50% develop secondary imatinib resistance and disease progression ... Prior to sunitinib, patients had no therapeutic option once they became resistant to imatinib ...