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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

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

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

  • 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。
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    [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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  • 收稿日期:  2010-11-09
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SGLT2抑制剂治疗糖尿病研究进展

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。

English Abstract

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.
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