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达格列净,首个用于治疗2型糖尿病的钠-葡萄糖协同转运蛋白2(SGLT-2)抑制剂

[Dapagliflozin, the first SGLT-2 inhibitor in the treatment of type 2 diabetes].

作者信息

Albarrán Olga González, Ampudia-Blasco F Javier

机构信息

Servicio de Endocrinología y Nutrición, Hospital Universitario Ramón y Cajal, Madrid, España.

Unidad de Referencia de Diabetes, Servicio de Endocrinología y Nutrición, Hospital Clínico Universitario de Valencia, Valencia, España.

出版信息

Med Clin (Barc). 2013 Sep;141 Suppl 2:36-43. doi: 10.1016/S0025-7753(13)70062-9.

Abstract

Dapagliflozin is the first novel sodium-glucose co-transporter-2 (SGLT2) inhibitor approved by the European Medicines Agency (EMA) for the treatment of type 2 diabetes. By inhibiting SGLT2, dapagliflozin blocks reabsorption of filtered glucose in the kidney, increasing urinary glucose excretion and reducing blood glucose levels. Its mechanism of action is independent of pancreatic β cell function and modulation of insulin sensitivity. The results of phase III clinical trials showed that dapagliflozin, at a dose of 5 or 10mg/day for 24 weeks as monotherapy in previously untreated patients, or as add-on combination therapy with metformin, glimepiride, pioglitazone or insulin-based therapy, significantly reduced both HbA1c and fasting plasma glucose levels compared with placebo. In addition, dapagliflozin was noninferior to glipizide, in terms of glycemic control after 52 weeks, when used as add-on therapy in patients with type 2 diabetes inadequately controlled with metformin. In most clinical trials, dapagliflozin reduced body weight. The combination of both effects (improved glycemic control and weight loss) is achieved to a greater extent in treatments that include dapaglifozin. Longer-term extension studies indicated that the efficacy of dapagliflozin on the glycemic control and weight reducción is maintained for up to 2 and 4 years. Dapagliflozin was well tolerated. Genital infections and urinary tract infections were more frequent in patients who received dapagliflozin than in placebo recipients. Hypoglycemic episodes were scarce with dapagliflozin. In conclusion, dapagliflozin is a novel option for the management of type 2 diabetes, particularly when used as add-on therapy.

摘要

达格列净是首个获欧洲药品管理局(EMA)批准用于治疗2型糖尿病的新型钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂。通过抑制SGLT2,达格列净可阻止肾脏中滤过葡萄糖的重吸收,增加尿糖排泄并降低血糖水平。其作用机制独立于胰腺β细胞功能和胰岛素敏感性调节。III期临床试验结果表明,对于既往未接受治疗的患者,达格列净以5或10mg/天的剂量单药治疗24周,或与二甲双胍、格列美脲、吡格列酮或胰岛素治疗联合使用作为附加联合治疗时,与安慰剂相比,均能显著降低糖化血红蛋白(HbA1c)和空腹血糖水平。此外,在二甲双胍控制不佳的2型糖尿病患者中,达格列净作为附加治疗使用52周后,在血糖控制方面不劣于格列吡嗪。在大多数临床试验中,达格列净可减轻体重。在包含达格列净的治疗中,能更大程度地实现血糖控制改善和体重减轻这两种效果的结合。长期扩展研究表明,达格列净在血糖控制和体重减轻方面的疗效可维持长达2年和4年。达格列净耐受性良好。接受达格列净治疗的患者发生生殖器感染和尿路感染的频率高于接受安慰剂的患者。使用达格列净时低血糖发作较少。总之,达格列净是管理2型糖尿病的一种新型选择,尤其是用作附加治疗时。

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