MEDI 215 |
| Imatinib (Gleevec™) is used as first-line treatment of chronic myeloid leukemia (CML) and for Philadelphia chromosome-positive acute lymphoblastic leukemia (ALL). Imatinib is a protein-tyrosine kinase inhibitor which potently inhibits the Abl tyrosine kinase activity of Bcr-Abl in vitro and in vivo. The discovery of imatinib, however, also provided insight into principal mechanisms of resistance occurring in accelerated or blast-crisis CML patients. This stimulated the tailored drug development of nilotinib and dasatinib for treatment of CML in imatinib-resistant patients. In addition, imatinib is a potent inhibitor of the receptor kinase for stem cell factor, c-Kit and of the platelet-derived growth factor receptor kinase (PDGF-R). As a consequence of these activities, Imatinib is also indicated for other indications such as the treatment of gastrointestinal stromal tumors GISTs driven by deregulated c-Kit signaling, and hypereosinophilic syndrome driven by deregulated PDGF-R signaling. |
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Heroes of Chemistry
1:30 PM-5:00 PM, Monday, August 20, 2007 BCEC -- 210 B/C, Oral
Division of Medicinal Chemistry |