Imatinib (Gleevec, Novartis, Basel, Switzerland), formerly referredto as STI571, is an inhibitor of specific protein tyrosine kinasesthat was targeted to the platelet-derived growth factor (PDGF)receptor (Figure 1). It was found to inhibit the constitutivelyactive fusion product arising from the Philadelphia (Ph) chromosomeof chronic myelogenous leukemia (CML) and c-kit (CD117), whichis overexpressed in gastrointestinal stromal tumors. Studiesof imatinib in other tumors that express c-kit or the PDGF receptorare under way. Imatinib was approved by the Food and Drug Administrationin May 2001 for the treatment of CML that is refractory to . . . [Full Text of this Article]
Protein Kinases as Therapeutic Targets
Chronic Myelogenous Leukemia
Clinical Features
Pathogenesis
Rationale for the Development of Imatinib
Standard Treatment of CML and the Need for Better Therapy
Phase 1 Trials of Imatinib for CML
Chronic Phase
Blast Phase
Phase 2 Trials of Imatinib for CML
Resistance of CML to Imatinib
Unanswered Questions
Imatinib for Gastrointestinal Stromal Tumors
Imatinib for Other Leukemias and Solid Tumors
Conclusions
Source Information
From the Herbert Irving Comprehensive Cancer Center, Columbia University College of Physicians and Surgeons, New York.
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