Isaji Masayuki
Kissei Pharmaceutical Co. Ltd, Central Research Laboratory, Nagano, Japan.
Kidney Int Suppl. 2011 Mar(120):S14-9. doi: 10.1038/ki.2010.511.
The physiological and pathological handling of glucose via sodium-glucose cotransporter-2 (SGLT2) in the kidneys has been evolving, and SGLT2 inhibitors have been focused upon as a novel drug for treating diabetes. SGLT2 inhibitors enhance renal glucose excretion by inhibiting renal glucose reabsorption. Consequently, SGLT2 inhibitors reduce plasma glucose insulin independently and improve insulin resistance in diabetes. To date, various SGLT2 inhibitors have been developed and evaluated in clinical studies. The potency and positioning of SGLT2 inhibitors as an antidiabetic drug are dependent on their characteristic profile, which induces selectivity, efficacy, pharmacokinetics, and safety. This profile decides which SGLT2 inhibitors can be expected for application of the theoretical concept of reducing renal glucose reabsorption for the treatment of diabetes. I review the structure and advancing profile of various SGLT2 inhibitors, comparing their similarities and differences, and discuss the expected SGLT2 inhibitors for an emerging category of antidiabetic drugs.
肾脏中通过钠-葡萄糖协同转运蛋白2（SGLT2）对葡萄糖进行的生理和病理处理一直在不断演变，而SGLT2抑制剂已成为治疗糖尿病的一种新型药物。SGLT2抑制剂通过抑制肾脏对葡萄糖的重吸收来增加肾脏葡萄糖排泄。因此，SGLT2抑制剂可独立降低血浆葡萄糖和胰岛素水平，并改善糖尿病患者的胰岛素抵抗。迄今为止，已开发出多种SGLT2抑制剂并在临床研究中进行了评估。SGLT2抑制剂作为一种抗糖尿病药物的效力和定位取决于其特性，包括选择性、疗效、药代动力学和安全性。这一特性决定了哪些SGLT2抑制剂有望应用于减少肾脏葡萄糖重吸收以治疗糖尿病的理论概念。我回顾了各种SGLT2抑制剂的结构和发展概况，比较了它们的异同，并讨论了有望成为新型抗糖尿病药物的SGLT2抑制剂。
