Imatinib (originally STI571) is a drug used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec as its mesyate salt, imatinib mesilate (INN). It is used in treating chronic myelogenous leukemia (CML),gastrointestinal stromaltumors (GISTs) and some other diseases. By 2011, Gleevec has been FDA approved to treat ten different cancers. In CML, throsine 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.
Adverse effects:
The most common side effects include weight gain, reduced number of blood cells (neutropenia, thrombocetopenia, anemia), headache, edema, nausea,rash, and musculoskeletal pain.
Severe congestive cardiac failure is an uncommon but recognized side effect of imatinib and mice treated with large doses of imatinib show toxic damage to their myocardium.
If imatinib is used in prepubescent children, it can delay normal growth, although a proportion will experience catch-up growth during puberty.
Costs:
Prices for a 100 mg pill of Gleevec internationally range from $20 to $30, although generic imatinib is cheaper.ADDITIONAL INFORMATION:
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