酪氨酸激酶抑制剂类新药的研发现状

周冰莹;安春娜;蒲小平

【期刊名称】《中国新药杂志》

【年(卷),期】2011(020)017

【摘要】蛋白激酶在多种疾病,特别是肿瘤发生发展过程中起重要作用,以其为药物靶点的激酶抑制剂则成为近年药物研发的热点.目前已有11个小分子激酶抑制剂上市,其中9个为酪氨酸激酶抑制剂.激酶抑制剂具有高选择性、副作用少的特点.已上市药物已经在慢性粒细胞白血病、非小细胞肺癌、肾细胞癌等多种疾病的治疗中显示出其较传统治疗药物的优越性,部分已成为治疗肿瘤的一线用药.本文对小分子酪氨酸激酶抑制剂类新药的研发现状进行综述.%Protein kinases are important in the pathogeneses and development of various diseases, especially tumor. Kinase inhibitors, targeting protein kinases, garner the attention of drug research and development ( R&D) in recent years. Currently, 11 small-molecule kinase inhibitors have been approved; among them 9 are the tyrosine kinase inhibitors. Kinase inhibitors have high selectivity and minimal side effects. Approved drugs have shown their superiority over traditional treatments in chronic myeloid leukemia (CML) , non-small cell lung cancer (NSCLC) and renal cell carcinoma (RCC) ; some of them already have become the first-line treatment of tumors. In the present paper, the current status of the new drug R&D of small-molecule tyrosine kinase inhibitors was reviewed.

【总页数】6页(1661-1666)