SGLT2抑制剂治疗糖尿病研究进展

丁海峰; 曹永兵; 安毛毛; 贾鑫明; 姜远英

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SGLT2抑制剂治疗糖尿病研究进展

丁海峰, 曹永兵, 安毛毛, 贾鑫明, 姜远英

文章导航 > 药学实践与服务 > 2011 > 29(2): 89-92,116

丁海峰, 曹永兵, 安毛毛, 贾鑫明, 姜远英. SGLT2抑制剂治疗糖尿病研究进展[J]. 药学实践与服务, 2011, 29(2): 89-92,116.

引用本文:

丁海峰, 曹永兵, 安毛毛, 贾鑫明, 姜远英. SGLT2抑制剂治疗糖尿病研究进展[J]. 药学实践与服务, 2011, 29(2): 89-92,116.

DING Hai-feng, CAO Yong-bing, AN Mao-mao, JIA Xin-ming, JIANG Yuan-ying. Research on type 2 sodium glucose co-transporters in diabetes treatment[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(2): 89-92,116.

Citation:

DING Hai-feng, CAO Yong-bing, AN Mao-mao, JIA Xin-ming, JIANG Yuan-ying. Research on type 2 sodium glucose co-transporters in diabetes treatment[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(2): 89-92,116.

SGLT2抑制剂治疗糖尿病研究进展

第二军医大学药学院新药研究中心,上海 200433

Research on type 2 sodium glucose co-transporters in diabetes treatment

The center of new drug development, second military medical university, Shanghai 200433, China

摘要: 近年来,钠-葡萄糖协同转运蛋白2(type 2 sodium glucose co-transporters,SGLT2)抑制剂作为一种新型的治疗糖尿病药物成为研究热点。SGLT2在肾近端小管葡萄糖重吸收中起着非常重要的作用;抑制肾脏SGLT2可以促进Ⅱ型糖尿病人尿糖的排泄,使其血糖恢复正常而不会有低血糖的风险。临床实验表明,SGLT2抑制剂对Ⅱ型糖尿病的治疗效果明显,且具有降低体重、无低血糖风险等优点,目前,许多SGLT2抑制剂已经进入临床评价后期。
- Ⅱ型糖尿病 /
- 钠-葡萄糖协同转运蛋白 /
- 抑制剂
Abstract: In the last few years, inhibitors of the type 2 sodium glucose co-transporters (SGLT2) had been the subject of novel approach to treating diabetes. SGLT2 played a major role in physiology of glucose reabsorption from proximal part of kidney. The blockade of SGLT2 in the kidney had the potential to prompts urinary excretion of glucose and promotes normalization of blood glucose without hypoglycemia in the setting of type 2 diabetes. Clinical trails showed that their efficacy in the treatment of type 2 diabetes was promising; Weight loss and very low risk of hypoglycemia were the potential benefits of these inhibitors. Some of these inhibitors had been developed and advanced to late phase clinical testing.
- type 2 diabetes /
- sodium-glucose co-transporters (SGLT) /
- inhibitor

[1]	Wright EM,Hirayama BA,Loo DF.Active sugar transport in health and disease[J].Intern Med,2007,261:32.
[2]	Kanai Y,Lee WS,You G,et al.The human kidney low affinity Na/glucose cotransporter SGLT2: delineation of the major renal reabsorptive mechanism for D-glucose[J].Clin Investig,1994,93:397.
[3]	Van den Heuvel LP,Assink K,Willemsen M,et al.Autosomal recessive renal glucosuria attributable to a mutation in the sodium glucose cotransporter (SGLT2) [J].Hum Genet,2002,111:544.
[4]	Calado J,Soto K,Clemente C,et al.Novel compound heterozygous mutations in SLC5A2 are responsible for autosomal recessive renal glucosuria[J].Hum Genet,2004, 114:314.
[5]	Pajor A,Wright EM.Cloning and functional expression of a mammalian Na⁺/nucleoside cotransporter. A member of the SGLT family[J].Biol Chem,1992,267:3557.
[6]	Wright EM.Renal Na⁺-glucose cotransporters[J].Am J Physiol,2001,280:F10.
[7]	Turk E,Zabel B,Mundlos S,et al.Glucose/galactose malabsorption caused by a defect in the Na⁺/glucose cotransporter[J].Nature,1991,350:354.
[8]	Pajor AM,Randolph KM,Kerner SA,et al.Inhibitor binding in the human renal low-and high-affinity Na⁺/glucose cotransporters[J].J Pharmacol Exp Ther,2008,324:985.
[9]	Ehrenkranz JRL,Lewis NG,Kahn CR,et al.Phlorizin: a review[J].Diabetes Metab Res Rev,2005,21:31.
[10]	Oku A,Ueta K,Arakawa K,et al.T-1095, an inhibitor of renal Na⁺- glucose cotransporters, may provide a novel approach to treating diabetes[J].Diabetes,1999, 48:1794.
[11]	Adachi T,Yasuda K,Okamoto Y,et al.T-1095, renal Na⁺-glucose transporter inhibitor, improves hyperglycemia in streptozotocin induced diabetic rats[J].Metabolism,2000,49:990.
[12]	Katsuno K,Fujimori Y,Takemura Y,et al.Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level[J].Pharmacol Exp Ther,2007,320:323.
[13]	Hussey EK,Clark RV,Amin DM,et al.Early clinical studies to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of single doses of sergliflozin, a novel inhibitor of renal glucose reabsorption, in healthy volunteers and subjects with type 2 diabetes mellitus[J].Diabetes,2007,56 (Suppl 1):189.
[14]	Fujimori Y,Katsuno K,Nakashima I,et al.Remogliflozin etabonate, in a novel category of selective low-affinity/high-capacity sodium glucose cotransporter (SGLT-2) inhibitors, exhibits antidiabetic efficacy in rodent models[J].Pharmacol Exp Ther,2008,327:268.
[15]	Wei M,Bruce AE,Alexandra AN,et al.Discovery of dapagliflozin: A potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes[J].J Med Chem,2008,51(5):1145.
[16]	Komoroski B,Vachharajani N,Boulton D,et al.Dapagliflozin, a Novel SGLT2 Inhibitor, Induces Dose-Dependent Glucosuria in Healthy Subjects[J].Clin Pharmacol Ther,2009,85:520.
[17]	Komoroski B,Vachharajani N,Feng Y,et al.Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus[J].Clin Pharmacol Ther,2009,85:513.
[18]	List JF,Woo V,Morales E,et al.Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes mellitus[J].Diabetes Care,2009,32:650.
[19]	Calado J,Loeffler J,Sakalliouglu O,et al.Familial renal glucosuria: SGLC5A2 mutation analysis and evidence of salt-wasting[J].Kidney Int,2006,69:852.

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SGLT2抑制剂治疗糖尿病研究进展

第二军医大学药学院新药研究中心,上海 200433

收稿日期: 2010-11-09
修回日期: 2011-02-22

关键词:

Ⅱ型糖尿病 /

钠-葡萄糖协同转运蛋白 /

抑制剂

摘要: 近年来,钠-葡萄糖协同转运蛋白2(type 2 sodium glucose co-transporters,SGLT2)抑制剂作为一种新型的治疗糖尿病药物成为研究热点。SGLT2在肾近端小管葡萄糖重吸收中起着非常重要的作用;抑制肾脏SGLT2可以促进Ⅱ型糖尿病人尿糖的排泄,使其血糖恢复正常而不会有低血糖的风险。临床实验表明,SGLT2抑制剂对Ⅱ型糖尿病的治疗效果明显,且具有降低体重、无低血糖风险等优点,目前,许多SGLT2抑制剂已经进入临床评价后期。