伊马替尼：癌症靶向治疗的一项突破。
Imatinib: a breakthrough of targeted therapy in cancer.
作者信息
Iqbal Nida, Iqbal Naveed
机构信息
Department of Medical Oncology, Dr. B. R. A. Institute Rotary Cancer Hospital, All India Institute of Medical Sciences, New Delhi 110029, India.
Department of Anaesthesia and Intensive Care Unit, Indraprastha Apollo Hospital, New Delhi 110076, India.
出版信息
Chemother Res Pract. 2014;2014:357027. doi: 10.1155/2014/357027. Epub 2014 May 19.
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.
蛋白酪氨酸激酶活性失调是人类癌症发病机制的核心。选择性酪氨酸激酶抑制剂（TKIs）形式的靶向治疗改变了各种癌症的治疗方法，代表了一项治疗突破。伊马替尼是最早显示出这种靶向作用潜力的癌症治疗药物之一。伊马替尼是一种口服靶向治疗药物，特异性抑制酪氨酸激酶BCR-ABL、c-KIT和PDGFRA。除了在慢性粒细胞白血病（CML）和胃肠道间质瘤（GIST）方面取得显著成功外，伊马替尼还对由PDGFR和c-KIT的伊马替尼特异性异常引起的其他各种肿瘤有益。由于其抗PDGFR作用，伊马替尼在类固醇难治性慢性移植物抗宿主病中也被证明是有效的。本文是对伊马替尼在肿瘤学中作用的全面综述。
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