多靶点抗肿瘤酪氨酸激酶抑制剂的研究开发

Advances in the research of multi-target tyrosine kinase inhibitors

随着对肿瘤细胞信号转导途径研究的不断深入,人们发现单靶点酪氨酸激酶抑制剂(TKI)难以达到理想的阻断肿瘤细胞发生发展通路及选择性抗癌作用,且相关毒副作用很难避免,为此多靶点TKI引起高度关注。目前为止,该类化合物的研究已取得很大进展,有十几种药物先后进入临床研究并陆续有药物成功上市,其中最引人关注的是索拉非尼和舒尼替尼。本文从多靶点TKI作用靶点、上市状况及其临床应用效果,分析该类药物的研究概况。

Advances in the understanding of cancer at the signaling pathways have led to much progress in the development of antieplastic. The tyrosine kinase inhibitors has been one of the most studied and exploited targets for molecular cancer therapy. Up to date, progress on the research of this class of multi-target kinase inhibitors has being achieved. Sorafenib is the first oral, multi-target tyrosine kinase inhibitor. This article summarized the progress on targets of effect, latest trends of development, products marketed and clinical researches about multi-target tyrosine kinase inhibitors.