Mechanisms of resistance imatinib (STI571) in preclinical models and in leukemia patients

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• 作者：Ellen Weisberg ; James D. Griffin
• 关键词：Cryptosporidum ; Drug resistance ; Chemotherapy
• 刊名：Drug Resistance Updates
• 出版年：2001
• 出版时间：February 2001
• 年：2001
• 卷：4
• 期：1
• 页码：22-28
• 全文大小：215 K

文摘

The tyrosine kinase inhibitor imatinib (ST1571, Glivec) blocks the activity of the BCR/ABL oncogene and induces hematologic remissions in the majority of patients with chronic myeloid leukemia (CML). Glivec is an aminopyrimidine derivative that interacts with the ATP-binding site within the kinase domain of ABL and several other tyrosine kinases, including c-KIT, PDGFβ receptor, and ARG. The compound is currently in phase III clinical trials. Although patients with chronic phase CML have been found to develop drug resistance only rarely so far, patients in more advanced phases of the leukemia develop resistance frequently. The available information on Glivec resistance will be reviewed.