Journal of cancer research and clinical oncology
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J. Cancer Res. Clin. Oncol. · Feb 2004
ReviewBasic science going clinical: molecularly targeted therapy of chronic myelogenous leukemia.
Imatinib (STI571), a 2-phenylaminopyrimidine, specifically inhibits the tyrosine kinase activity of Abl, Kit, and platelet-derived growth factor receptor. Clinical trials in chronic myelogenous leukemia (CML), characterized by the constitutively active Bcr-Abl tyrosine kinase, and gastrointestinal stromal tumors, characterized by activating mutations of Kit, have shown excellent results. ⋯ Room will be given to problems and challenges that may be typical of molecularly targeted therapy in general, such as the emergence of resistance as a result of point mutations. Last, the question will be addressed, why imatinib is so successful, and whether its success might be reproducible in other malignant conditions.