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Imatinib (Gleevec)

Target and mechanism of action: it is a small molecule that inhibits the tyrosine-kinase activity associated with c-Kit receptor (expressed by the inoperable gastrointestinal stromal tumors or GISTs) and tyrosine-kinase that is activated when chromosomal translocation occurs in the gene Bcr-Abl which is the origin of chronic myeloid leukemia.

Indications: Imatinib is indicated for the treatment of adult patients with chronic myeloid leukemia with Philadelphia chromosome (bcr-abl), which is positive in chronic phase after failure of interferon-alpha therapy, or in accelerated phase or in blast crisis. It is also indicated for the treatment of GIST (Gastrointestinal Stromal Tumors); they are rare tumors of digestive tract, most often localized in the stomach (about 2/3 of cases), more rarely in the gut small intestine (20/30%) and even less frequently in other parts such as the esophagus and large intestine (about 10% of cases).

Mode of Administration: it is administered orally as tablets.

Most common side effects: adverse events associated with the drug most commonly reported are nausea/vomiting, diarrhea, myalgia, muscular cramps, rash skin, superficial edema (periorbital or lower limb), neutropenia and thrombocytopenia.

Trade Name: Gleevec (Novartis pharmaceutical company). The drug is currently marketed in Italy for the treatment of GIST and chronic myeloid leukemia resistant to interferon therapy.

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