Imatinib: a breakthrough of targeted therapy in cancer.
Imatinib: a breakthrough of targeted therapy in cancer.
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伊马替尼：癌症靶向治疗的突破。
DOI：
10.1155/2014/357027
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Iqbal N
中科院分区：
文献类型：
--
作者：
Iqbal N;Iqbal N
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（TKI）形式的靶向治疗已经改变了各种癌症的管理方法，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治疗药物，可特异性抑制酪氨酸激酶BCR-ABL、c-KIT和PDGFRA。除了在CML和GIST中的显著成功外，伊马替尼还有益于由伊马替尼特异性PDGFR和c-KIT异常引起的各种其他肿瘤。伊马替尼也已被证明是有效的类固醇难治性慢性移植物抗宿主病，因为它的抗PDGFR的行动。本文就伊马替尼在肿瘤学中的作用作一综述。
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.