钠-葡萄糖共转运蛋白2抑制剂的研究进展
作者：任悦;张路平;秦兰;杨加举;顾恩科;唐春雷;
Author：
收稿日期： 年卷（期）页码：2018,33(01):-101-106
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：Ⅱ型糖尿病;钠-葡萄糖共转运蛋白2;抑制剂;双重抑制剂;复方制剂;临床研究;研究进展;综述
Key words：
基金项目：国家自然科学基金资助项目(批准号:21305051);;
国家级大学生创新训练计划(编号:201510295051)
中文摘要
钠-葡萄糖共转运蛋白2(SGLT2)对肾脏葡萄糖的重吸收有重要作用。通过选择性地抑制SGLT2可减少近曲小管对葡萄糖的重吸收,使多余的葡萄糖通过尿液排出达到降低血糖的效果。SGLT2抑制剂在降低血糖的同时,还可减轻体重,改善胰岛素抵抗,成为治疗Ⅱ型糖尿病的新方向。现综述了已上市的和正在研究中的部分SGLT2抑制剂,并展望该类药物的发展。
参考文献
[1]刘建民,赵咏桔.糖尿病酮症酸中毒和高血糖高渗状态[J].中华内分泌代谢杂志,2003,19(6):505-508.
[2]曾要富,姚亮元,钟爱军,等.SGLT2抑制剂Canagliflozin—Ⅱ型糖尿病治疗的新药[J].中国现代应用药学,2014,9:1154-1160.
[3]Xu Y,Wang L,He J,et al.Prevalence and control of diabetes in Chinese adults[J].JAMA,2013,310(9):948-959.
[4]Wright EM,Loo DD,Hirayama BA.Biology of human sodium glucose transporters[J].Physiol Rev,2011,91(2):733-794.
[5]Nisly SA,Kolanczyk DM,Walton AM.Canagliflozin,a new sodium-glucose cotransporter 2 inhibitor,in the treatment of diabetes[J].Am J Health Syst Pharm,2013,70(4):311-319.
[6]朱路,李华荣.SGLT2抑制剂:机制独特的降糖药物[J].新医学,2014,09:573-576.
[7]蔡茜.根皮苷对db/db小鼠糖尿病心肌病变保护机制的定量蛋白质组学研究[D].济南:山东大学硕士学位论文,2013.
[8]李莹,钱海,黄文龙.糖尿病治疗的新希望—SGLT2抑制剂[J].中国新药杂志,2011,20(21):2073-2079.
[9]Tsujihara K,Hongu M,Saito K,et al.Na+-glucose cotransporter(SGLT)inhibitors as antidiabetic agents.4.Synthesis and pharmacological properties of 4’-dehydroxyphlorizin derivatives substituted on the B ring[J].J Med Chem,1999,42(26):5311-5324.
[10]Oku A,Ueta K,Nawano M,et al.Antidiabetic effect of T-1095,an inhibitor of Na+-glucose cotransporter,in neonatallystreptozotocin-treated rats[J].Eur J Pharmacol,2000,391(1-2):183-192.
[11]Ueta K,Ishihara T,Matsumoto Y,et al.Long-term treatment with the Na+-glucose cotransporter inhibitor T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats[J].Life Sci,2005,76(23):2655-2668.
[12]Nomura S,Sakamaki S,Hongu M,et al.Discovery of Canagliflozin,a novel C-glucoside with thiophene ring,as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus(1)[J].J Med Chem,2010,53(17):6355-6360.
[13]Devineni D,Curtin CR,Polidori D,et al.Pharmacokinetics and pharmacodynamics of Canagliflozin,a sodium glucose co-transporter 2 inhibitor,in subjects with type 2 diabetes mellitus[J].J Clin Pharmacol,2013,53(6):601-610.
[14]Wilding JPH,Charpentier G,Hollander P,et al.Efficacy and safety of Canagliflozin in patients with type 2 diabetes mellitus inadequately controlled with metformin and sulphonylurea:A randomisedtrial[J].Int J Clin Pract,2013,67(12):1267-1282.
[15]Bailey CJ,Iqbal N,T'joen C,et al.Dapagliflozinmonotherapy in drug-na6ve patients with diabetes:A randomized-controlled trial of low-dose range[J].Diabetes Obes Metab,2012,14(10):951-959.
[16]石卫峰,李晓宇,刘皋林.治疗2型糖尿病新药达格列净[J].中国新药杂志,2013,22(16):1861.
[17]吕昕泽,孙波,杨微,等.治疗2型糖尿病新药Ipragliflozin[J].中国新药杂志,2015,24(3):241-244.
[18]Kashiwagi A,Takinami Y,Kazuta K,et al.Ipragliflozin improved glycaemic control with additional benefits of reductions of body weight and blood pressure in Japanese patients with type 2 diabetes mellitus:Brighten Study[C].Diabetologia.233 Spring ST,New York,NY 10013 USA:Springer,2011,54:S68-S69.
[19]Schwartz SL,Akinlade B,Klasen S,et al.Safety,pharmacokinetic,and pharmacodynamic profiles of ipragliflozin(ASP1941),a novel and selective inhibitor of sodium-dependent glucose co-transporter 2,in patients with type 2 diabetes mellitus[J].Diabetes Technol Ther,2011,13(12):1219-1227.
[20]Smulders RA,Zhang W,Veltkamp SA,et al.No pharmacokinetic interaction between ipragliflozin and sitagliptin,pioglitazone,or glimepiride in healthy subjects[J].Diabetes Obes Metab,2012,14(10):937-943.
[21]Anthony M,Shelley E.Luseogliflozin:First global approval[J].Drugs,2014,74(8):945-950.
[22]Sasaki T,Seino Y,Fukatsu A,et al.Safety,Pharmacokinetics,and pharmacodynamics of single and multiple luseogliflozin dosing in healthy japanese males:A Randomized,single-blind,placebocontrolled trial[J].Adv Ther,2014,31(3):345-361.
[23]刘文杰,陈林,李江红,等.2型糖尿病的克星—SGLT-2抑制剂[J].国外医药:抗生素分册,2015,3:121-125.
[24]Seino Y.Luseogliflozin for the treatment of type 2 diabetes[J].Expert Opin Pharmacother,2014,15(18):2741-2749.
[25]陈再新,刘雯,张明光,等.新型2型糖尿病治疗药物SGLT-2抑制剂的临床研究进展[J].常州大学学报:自然科学版,2014,26:37-44.
[26]Haneda M,Seino Y,Sasaki T,et al.Luseogliflozin,a SGLT2inhibitor,as add-on therapy to 5 types of oral antidiabetic drugs improves glycaemic control and reduces body weight in Japanese patients with type 2 diabetes mellitus[C].Diabetologia.233Spring ST,New York,NY 10013 USA:Springer,2013,56:S384-S384.
[27]Nagata T,Fukuzawa T,Takeda M,et al.Tofogliflozin,a novel sodium-glucose co-transporter 2 inhibitor,improves renal and pancreatic function in db/dbmice[J].Br J Pharmacol,2013,170(3):519-531.
[28]鄂一丹,许佑君.艾帕列净[J].中国药物化学杂志,2015,25(1):80.
[29]Kadowaki T,Haneda M,Inagaki N,et al.Efficacy and safety of Empagliflozin monotherapy for 52 weeks in Japanese patients with type 2 diabetes:A randomized,double-blind,parallel-group study[J].Ad Ther,2015,32(4):306-318.
[30]Hring HU,Merker L,Seewaldt-Becker E,et al.Empagliflozin as add-on to metformin plus sulfonylurea in patients with type 2diabetes:A 24-week,randomized,double-blind,placebocontrolled trial[J].Diabetes Care,2013,36(11):3396-3404.
[31]Kovacs CS,Seshiah V,Swallow R,et al.Empagliflozin improves glycaemic and weight control as add-on therapy to pioglitazone or pioglitazone plus metformin in patients with type 2 diabetes:A24-week,randomized,placebo-controlled trial[J].Diabetes Obes Metab,2014,16(2):147-158.
[32]Julio R,Ante J,Guillaume F,et al.Improved glucose control with weight loss,lower insulin doses,and no increased hypoglycemia with Empagliflozin added to titrated multiple daily injections of insulin in obese inadequately controlled type 2 diabetes[J].Diabetes Care,2014,37(7):1815-1823.
[33]刘莲,封宇飞.SGLT2抑制剂依帕列净的药理作用与临床评价[J].中国新药杂志,2015,11:1201-1203.
[34]Fujimori Y,Katsuno K,Ojima K,et al.Sergliflozinetabonate,a selective SGLT2 inhibitor,improves glycemic control in streptozotocin-induced diabetic rats and Zucker fatty rats[J].Eur J Pharmacol,2009,609(1-3):148-154.
[35]Thaddanee R,Khilnani AK,Khilnani G.SGLT-2 inhibitors:The glucosuricantidiabetics[J].Int J Basic Clin Pharmacol,2013,2(4):347-352.
[36]段娟慧,巫冠中.SGLT1/SGLT2双重抑制剂—Sotagliflozin的研究概况[J].中南药学,2015,9:947-950.
[37]Zambrowicz B,Freiman J,Brown P M,et al.LX4211,a Dual SGLT1/SGLT2 Inhibitor,improved Glycemic control in patients with type 2 diabetes in a randomized,placebo-controlled trial open[J].Clin Pharmacol Ther,2012,92(2):158-169.
[38]Powell DR,Dacosta CM,Smith M,et al.Effect of LX4211 on glucose homeostasis and body composition in preclinical models[J].J Pharmacol Exp Therapeutics,2014,350(2):232-242.
[39]周植星,耿艳艳,崔艳丽,等.新型SGLT1/2双靶点抑制剂Sotagliflozin[J].现代药物与临床,2015,04:465-469.
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