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利司那肽——一种用于治疗2型糖尿病的新型胰高血糖素样肽-1受体激动剂。

Lixisenatide - A New Glucagon-like Peptide 1 Receptor Agonist in the Treatment of Type 2 Diabetes.

作者信息

Vidal Josep

机构信息

Head, Endocrinology and Nutrition Department, Hospital Clinic, Barcelona, Spain.

出版信息

Eur Endocrinol. 2013 Aug;9(2):76-81. doi: 10.17925/EE.2013.09.02.76. Epub 2013 Aug 23.

Abstract

Optimal glycaemic control is essential to managing risks in patients with type 2 diabetes. However, glycaemic control remains poor among type 2 diabetes patients, particularly the control of post-prandial glucose (PPG). Almost half of patients treated with basal insulin and oral anti-diabetic drugs (OADs) do not achieve their glycated haemoglobin (HbA1c) goals, despite achieving fasting plasma glucose (FPG) control. Glycaemic control targets have emphasised FPG targets, but PPG contributes significantly to overall glycaemic control in type 2 diabetes. Glucagon-like peptide 1 (GLP-1) receptor agonists have shown substantial efficacy in improving overall glycaemic control but have differing effects on PPG, which is a result of their different mechanisms of action. Lixisenatide is unique among existing GLP-1 receptor agonists in that it is short acting but given as a once daily dose, and exerts its main effects during the prandial period. It has demonstrated efficacy in an extensive clinical trial programme. In particular, it has shown a beneficial effect on PPG compared with existing GLP-1 receptor agonists, probably a result of its effect on slowing gastric emptying. This has provided a strong rationale for its use as add-on therapy to long-acting basal insulin analogues, in cases where the latter is not providing adequate glycaemic control. The additive effects on glycaemic control may lead to a new treatment approach to manage blood glucose and prevent long-term complications in patients with type 2 diabetes.

摘要

优化血糖控制对于管理2型糖尿病患者的风险至关重要。然而,2型糖尿病患者的血糖控制仍然较差,尤其是餐后血糖(PPG)的控制。几乎一半接受基础胰岛素和口服降糖药(OADs)治疗的患者尽管实现了空腹血糖(FPG)控制,但仍未达到糖化血红蛋白(HbA1c)目标。血糖控制目标一直强调FPG目标,但PPG在2型糖尿病的总体血糖控制中起着重要作用。胰高血糖素样肽1(GLP-1)受体激动剂在改善总体血糖控制方面已显示出显著疗效,但对PPG的影响各不相同,这是其不同作用机制的结果。利司那肽在现有GLP-1受体激动剂中独具特色,它作用时间短但每日给药一次,且在进餐期间发挥主要作用。它在广泛的临床试验项目中已证明具有疗效。特别是,与现有的GLP-1受体激动剂相比,它对PPG显示出有益作用,这可能是其对胃排空减慢作用的结果。在长效基础胰岛素类似物不能提供充分血糖控制的情况下,这为其作为附加疗法用于此类患者提供了有力的理论依据。对血糖控制的附加作用可能会带来一种新的治疗方法,用于管理2型糖尿病患者的血糖并预防长期并发症。

相似文献

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The design and discovery of lixisenatide for the treatment of type 2 diabetes mellitus.用于治疗2型糖尿病的利司那肽的设计与发现。
Expert Opin Drug Discov. 2014 Oct;9(10):1223-51. doi: 10.1517/17460441.2014.942638. Epub 2014 Aug 14.

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