Imatinib

Imatinib or Imatinib mesylate comes with different product brand names such as Gleevec, Glivec, etc. Gleevec imatinib is prescribed for the treatment of certain types of cancer like the chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and some other similar malignancies. Manufactured in India, this drug is now promoted by Novartis with the trade name Gleevec (USA) or Glivec (Europe/Australia).

Gleevec is prescribed to cure Ph+ chronic phase CML of pediatric patients that is caused due to the transplantation of stem cells or due to their resistance to interferon-alpha therapy. This drug is also effective in treating Kit (CD117) positive unresectable or metastatic malignant gastrointestinal stromal tumors (GIST). Imatinib is indicated for several other malignancies including Dermatofibrosarcoma Protuberans (DFSP), Hypereosinophilic Syndrome (HES), Chronic Eosinophilic Leukemia (CEL), Aggressive Systemic Mastocytosis (ASM), lymphoblastic leukemia Myelodysplastic or Myeloproliferative Diseases (MDS/MPD), and so on.

This medicine is found as a white to off-white to brownish or yellowish shaded crystalline powder. According to the imatinib package insert, 400 mg or 600 mg doses of this drug is required to be taken once daily with a meal and a large glass of water. 800 mg dosage of imatinib is directed as 400 mg twice a day. The dosage may increase or decrease with the type of malignancy. Some indications of imatinib resistance or intolerance of patients towards imatinib while in the treatment phase of CML is also reported.
The imatinib mechanism of action is simple. This drug binds to the ATP binding site of bcr-abl and suppresses the enzyme activity of the protein effectively. This suppression helps in promoting its entry in to the nucleus, but they are unable to perform any of its normal anti-apoptopic processes there. Imatinib side effects are as follows: fluid retention, dermatologic toxicities, hematologic toxicity edema, gastrointestinal disorders etc.