钠-葡萄糖协同转运蛋白2抑制剂类抗糖尿病新药的研发概况  

Survey on new drugs of sodium-glucose co-transporter 2 inhibitors for treatment of diabetes

作　　者：王玉丽[1] 王小彦[1,2] 赵桂龙[1] 邵华[1] 徐为人[1,2] 汤立达[1] 

机构地区：[1]天津药物研究院天津市新药设计与发现重点实验室,天津300193 [2]天津中医药大学研究生院,天津300193

出　　处：《现代药物与临床》2012年第2期138-142,共5页Drugs & Clinic

基　　金：国家重大新药创制专项(2011ZX09401-009);天津市科技支撑计划重点项目(10ZCKFSH01300)

摘　　要：目前,钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂通过抑制葡萄糖在肾脏近曲小管的重吸收,从而成为治疗糖尿病的新途径。按其结构,SGLT2抑制剂主要分为C-芳基抑制剂、O-芳基抑制剂、S-糖苷抑制剂和N-糖苷抑制剂,而C-芳基抑制剂和O-芳基抑制剂处于研究热点,其中几个新药(dapagliflozin、canagliflozin、ASP1941、BI10773和LX4211)显示出良好的控制血糖水平和减轻体质量的效果,且不良反应较小。综述两类结构中的主要药物研究概况,并分析其研发前景。For the present,sodium-glucose co-transporter 2（SGLT2） inhibitors have become a potentially new therapeutic approach for the treatment of type 2 diabetes,and they could lower the blood glucose levels by inhibiting glucose reabsorption in the renal proximal tubules.They conclude C-aryl inhibitor,O-aryl inhibitor,S-aryl inhibitor,and N-aryl inhibitor,but C-aryl inhibitor and O-aryl inhibitor are in the hot research.Several SGLT2 inhibitors in development（dapagliflozin,canagliflozin,ASP1941,BI10773,and LX4211） have demonstrated the improvement in glycemic control and weight loss,along with slight adverse effects.In this paper,the progress in study on drugs,from the two sorts of structure,is reviewed,and the development prospects of the SGLT2 is also analyzed.

关 键 词：SGLT2抑制剂 精眯病 DAPAGLIFLOZIN canagliflozin C-艿睦抑制剂 

分 类 号：R977[医药卫生—药品]