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达格列净和沙格列汀片用于成人2型糖尿病患者。

Dapagliflozin and saxagliptin tablets for adults with type 2 diabetes.

作者信息

Scheen André J

机构信息

a Division of Diabetes, Nutrition and Metabolic Disorders, Department of Medicine , CHU Liège , Liège , Belgium.

b Division of Clinical Pharmacology, Center for Interdisciplinary Research on Medicines (CIRM) , University of Liège , Liège , Belgium.

出版信息

Expert Rev Clin Pharmacol. 2017 Dec;10(12):1303-1316. doi: 10.1080/17512433.2017.1389645. Epub 2017 Oct 18.

Abstract

Saxagliptin (a dipeptidyl peptidase-4 inhibitor, DPP-4i) and dapagliflozin (a sodium-glucose cotransporter type 2 inhibitor, SGLT2i) improve glucose control in type 2 diabetes (T2D) through different potentially complementary mechanisms, thus offering the opportunity for a combined therapy. Area covered: The characteristics of the saxagliptin/dapagliflozin combination are analysed, focusing on: 1) pharmacokinetic and pharmacodynamic properties; 2) efficacy and safety in phase III trials with concurrent and sequential add-on therapy; and 3) potential use in clinical practice, including in special populations (cardiovascular disease, heart failure, chronic kidney disease, elderly). Expert commentary: Conclusions drawn from clinical trials investigating combination with the separate drugs are considered to apply to the fixed-dose combination (FDC) that demonstrates bioequivalence. Dual saxagliptin/dapagliflozin therapy is more potent than either monotherapy and can be used as an initial combination or a stepwise sequential approach. Dual therapy is generally well tolerated and may be used in special populations, with some limitations because of the presence of dapagliflozin. However, the latter may offer some advantages because of multiple effects attributed to SGLT2i. The best place of this dual combination for the management of T2D and the profile of patients who will make the most of this combined therapy remains to be defined.

摘要

沙格列汀(一种二肽基肽酶-4抑制剂,DPP-4i)和达格列净(一种钠-葡萄糖协同转运蛋白2抑制剂,SGLT2i)通过不同但可能互补的机制改善2型糖尿病(T2D)患者的血糖控制,从而为联合治疗提供了机会。涵盖领域:分析沙格列汀/达格列净联合用药的特点,重点关注:1)药代动力学和药效学特性;2)在III期试验中联合及序贯附加治疗的疗效和安全性;3)在临床实践中的潜在应用,包括特殊人群(心血管疾病、心力衰竭、慢性肾脏病、老年人)。专家评论:从单独药物联合用药的临床试验得出的结论被认为适用于具有生物等效性的固定剂量复方制剂(FDC)。沙格列汀/达格列净双重治疗比单一疗法更有效,可作为初始联合治疗或逐步序贯治疗方法。双重治疗通常耐受性良好,可用于特殊人群,但由于达格列净的存在有一些限制。然而,由于SGLT2i具有多种作用,达格列净可能具有一些优势。这种双重联合用药在T2D管理中的最佳地位以及最能从这种联合治疗中获益的患者特征仍有待确定。

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