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CancerQuest > Drugs > Imatinib Mesylate (Gleevec®)

Imatinib Mesylate (Gleevec®)

Generic Name: Imatinib Mesylate Brand Name(s): Gleevec® IUPAC: 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide FDA Approval: yes Manufacturer Link

Usage: Imatinib was designed to treat chronic myeloid leukemia (CML). In CML, a chromosomal rearrangement in white blood cells fuses two genes together.⁽¹⁾This creates an oncogene that produces a damaged tyrosine kinase receptor protein BCR-ABL that signals the cells to grow and divide even when no growth factor is present. This results in overproduction of immature white blood cells. Imatinib was approved by the FDA to treat CML in 2001 and additionally approved in 2006 for use in pediatric, Philadelphia chromosome-positive CML patients ⁽²⁾. In 2002 the FDA approved the use of Imatinib for the treatment of gastrointestinal stromal tumors (GIST) that are CD117 positive and are unresectable or metastatic. In 2006 the FDA also approved imatinib to treat dermatofibrosarcoma protuberans, myelodysplatic or myeloproliferative conditions, aggressive systemic mastocytosis, chronic eosinophilic leukemia and refractory Philadelphia chromosome-positive acute lymphocytic leukemia.⁽²⁾

Mechanism: Imatinib mesylate (Gleevec®, Glivec®) is a tyrosine kinase inhibitor that works to prevent the growth-inducing signals sent by enzymes found in some cancerous cells. The product of the BCR-ABL gene is a kinase that adds phosphate groups onto target molecules (substrates). Imatinib binds to the the ATP binding site of the enzyme. ⁽¹⁾⁽³⁾ If it is unable to bind ATP, the BCR-ABL protein cannot carry out its kinase activity. The signals sent by the enzyme would act to stimulate cell division so Imatinib inhibits tumor growth of cancerous cells.

Side Effects: Common side effects include nausea, diarrhea, leg aches or cramps, swelling of the face, altered bone marrow function. These side effects are usually mild or moderate and frequently occur during the first month of treatment and may get better after initial treatments. ⁽¹⁾⁽⁴⁾

References for this page:

1. Genta Pharmaceuticals [http://www.genta.com]
2. U.S. Food and Drug Administration: Office of Oncology Drug Products (accessed 2/4/08) [http://www.fda.gov/cder/Offices/OODP/whatsnew.htm]
3. Giles FJ, Cortes JE and HM Kantarjian. "Targeting the kinase activity of the BCR-ABL fusion protein in patients with chronic myelogenous leukemia." Current Molecular Medicine (2005)5(7):615-23. [PUBMED]
4. Gleevec". Prescribing Information. Novartis Pharmaceuticals. December, 2002. [http://www.gleevec.com]