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新型SGLT1/2双靶点抑制剂sotagliflozin
引用本文:周植星,耿艳艳,崔艳丽,刘巍.新型SGLT1/2双靶点抑制剂sotagliflozin[J].现代药物与临床,2015,30(4):465-469.
作者姓名:周植星  耿艳艳  崔艳丽  刘巍
作者单位: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. 天津药物研究院天津市新药设计与发现重点实验室,天津 300193; 天津医科大学,天津 300070
3. 天津药物研究院医药信息中心,天津,300193
基金项目:天津市应用基础与前沿技术研究计划项目(14JCZDJC33500)
摘    要:钠-葡萄糖共转运蛋白2(SGLT2)抑制剂是一类新兴的治疗糖尿病的药物。近年来,遗传学和药理学研究发现,胃肠道SGLT1蛋白也可能成为一个有治疗前景的药物靶点。SGLT1/SGLT2双靶点抑制剂的开发将为糖尿病的治疗提供另一个非胰岛素依赖的途径。临床研究表明,sotagliflozin可以通过双重抑制SGLT1和SGLT2的作用来降低餐后血糖、升高GLP-1和促进尿糖排出。因此,这些特征使得sotagliflozin在对1型和2型糖尿病的治疗方面具有重要临床意义。

关 键 词:sotagliflozin  钠-葡萄糖共转运蛋白2  钠-葡萄糖共转运蛋白1  抑制剂  糖尿病
收稿时间:2015/3/25 0:00:00

A new dual sodium-dependent glucose transporter 1/2 inhibitor: sotagliflozin
ZHOU Zhi-xing,GENG Yan-yan,CUI Yan-li and LIU Wei.A new dual sodium-dependent glucose transporter 1/2 inhibitor: sotagliflozin[J].Drugs & Clinic,2015,30(4):465-469.
Authors:ZHOU Zhi-xing  GENG Yan-yan  CUI Yan-li and LIU Wei
Institution:Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Tianjin Medical University, Tianjin 300070, China;Drug Informatics Center, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Abstract:The sodium-dependent glucose transporter 2 (SGLT2) inhibitors is an important emerging class for the treatment of diabetes. In recent years, genetic and pharmacology researches have indicated that gastrointestinal SGLT1 inhibitors may also be an appropriate therapeutic target to treat diabetes. Combining SGLT1 and SGLT2 inhibitors in a single molecule would provide complementary insulin-independent mechanisms to treat diabetes. Therefore, sotagliflozin has been developed as a dual inhibitor of SGLT1 and SGLT2. The differentiating clinical features of dual inhibitor of SGLT1 and SGLT2 include a large postprandial glucose reduction, elevation of glucagon-like peptide 1 and modest urinary glucose excretion. These features may have clinical implications for the use of sotagliflozin in the treatment of both type 1 and type 2 diabetes.
Keywords:sotagliflozin  SGLT2  SGLT1  inhibitor  diabetes
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