10 Facts About Imatinib

Imatinib, sold under the brand names Gleevec and Glivec among others, is an oral chemotherapy medication used to treat cancer.

Imatinib was approved for medical use in the United States in 2001.

Imatinib is used to treat chronic myelogenous leukemia, gastrointestinal stromal tumors and a number of other malignancies.

Imatinib is highly plasma protein-bound: dialysis is unlikely to be helpful removing imatinib.

Imatinib is a 2-phenyl amino pyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes.

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Imatinib is specific for the TK domain in abl, c-kit and PDGF-R .

Imatinib is quite selective for bcr-abl, though it does inhibit other targets mentioned above, as well as ABL2 and DDR1 tyrosine kinases and NQO2 – an oxidoreductase.

Imatinib has been reported to be an effective treatment for FIP1L1-PDGFRalpha+ mast cell disease, hypereosinophilic syndrome, and dermatofibrosarcoma protuberans.

Imatinib was initially thought to have a potential role in the treatment of pulmonary hypertension.

Imatinib is an experimental drug in the treatment of desmoid tumor or aggressive fibromatosis.