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Imatinib: A Breakthrough of Targeted Therapy in Cancer

机译：伊马替尼：癌症靶向疗法的突破

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Deregulated protein tyrosine kinase activity is central to the pathogenesis of human cancers. Targeted therapy in the form of selective tyrosine kinase inhibitors (TKIs) has transformed the approach to management of various cancers and represents a therapeutic breakthrough. Imatinib was one of the first cancer therapies to show the potential for such targeted action. Imatinib, an oral targeted therapy, inhibits tyrosine kinases specifically BCR-ABL, c-KIT, and PDGFRA. Apart from its remarkable success in CML and GIST, Imatinib benefits various other tumors caused by Imatinib-specific abnormalities of PDGFR and c-KIT. Imatinib has also been proven to be effective in steroid-refractory chronic graft-versus-host disease because of its anti-PDGFR action. This paper is a comprehensive review of the role of Imatinib in oncology.
机译：失调的蛋白酪氨酸激酶活性对人类癌症的发病机制至关重要。选择性酪氨酸激酶抑制剂（TKIs）形式的靶向治疗已经改变了各种癌症的治疗方法，代表了治疗上的突破。伊马替尼是最早显示出这种靶向作用潜力的癌症疗法之一。伊马替尼是一种口服靶向疗法，可特异性抑制酪氨酸激酶BCR-ABL，c-KIT和PDGFRA。伊马替尼除了在CML和GIST中取得显著成功外，还有益于伊马替尼特有的PDGFR和c-KIT异常引起的其他多种肿瘤。伊马替尼还具有抗PDGFR的作用，因此已被证明可有效治疗类固醇难治的慢性移植物抗宿主病。本文是对伊马替尼在肿瘤学中的作用的全面综述。

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