| 引用本文: | 曾要富,姚亮元,钟爱军,朱颖熹,袁秀菊.SGLT2抑制剂Canagliflozin——Ⅱ型糖尿病治疗的新药[J].中国现代应用药学,2014,31(9):1154-1160. |
| ZENG Yaofu,YAO Liangyuan,ZHONG Aijun,ZHU Yingxi,YUAN Xiuju.SGLT2 Inhibitor Canagliflozin: A New Drug for the Treatment of Patients with Type 2 Diabetes Mellitus[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(9):1154-1160. |
|
| 摘要: |
| 钠依赖的葡萄糖转运蛋白2(sodium-dependent glucose transporters 2，SGLT2)是一种低亲和力、高容量的转运体，主要分布在肾脏近曲小管S1部位，负责肾脏中约90%葡萄糖的重吸收。因此，抑制SGLT2，阻止近曲小管对葡萄糖的重吸收，通过增加尿糖的排出来降低血糖已经成为糖尿病治疗的一种新的策略。文章简述了目前处于临床阶段的SGLT2抑制剂，重点阐述了第1个被FDA批准的SGLT2抑制剂——Canagliflozin，包括它的合成、药动学、药效学、临床研究及不良反应等。 |
| 关键词: SGLT2抑制剂 Canagliflozin Ⅱ型糖尿病 |
| DOI： |
| 分类号: |
| 基金项目: |
|
| SGLT2 Inhibitor Canagliflozin: A New Drug for the Treatment of Patients with Type 2 Diabetes Mellitus |
|
ZENG Yaofu, YAO Liangyuan, ZHONG Aijun, ZHU Yingxi, YUAN Xiuju
|
|
Hunan Qianjin Xiangjiang Pharmaceutical Industry Co., Ltd., Zhuzhou 412000, China
|
| Abstract: |
| Sodium-dependent glucose transporters 2 mainly found in the S1 segment of the proximal tubule of the nephron is a low-affinity, high-capacity transporter believed to account for 90% of the renal glucose reabsorption. Therefore, inhibiting the activity of SGLT2, blocking this reabsoption and increasing the amount of glucose excretion, has been proposed as a novel strategy for treating diabetes. The latest research progress on SGLT2 inhibitors was introduced. Additionally, Canagliflozin, the first SGLT2 inhibitor approved by FDA was described in detail, including its synthesis, pharmacokinetics, pharmacodynamics, clinical research and adverse effects and so on. |
| Key words: SGLT2 inhibitor Canagliflozin type 2 diabetes mellitus |
