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利拉鲁肽:它能在2型糖尿病治疗中发挥作用吗?

Liraglutide: can it make a difference in the treatment of type 2 diabetes?

作者信息

Unger J

机构信息

Catalina Research Institute, Chino, CA 91710, USA.

出版信息

Int J Clin Pract Suppl. 2010 Oct(167):1-3. doi: 10.1111/j.1742-1241.2010.02497.x.

Abstract

Despite advances in the management of type 2 diabetes, glycaemic control remains suboptimal for many patients because of the complexities of disease progression and the need to balance improved glycaemic control against adverse treatment effects, particularly weight gain and hypoglycaemia. Thus, the development of new antidiabetes therapies continues in earnest. Incretin hormones have been the recent focus of research, as they account for up to 70% of the insulin response following a meal. There is also a high concordance between the physiological actions of one hormone, glucagon-like peptide-1 (GLP-1), and the therapeutic needs of patients. As native human GLP-1 has a half life of only approximately 2 min, researchers have developed molecules that act as GLP-1 receptor agonists or inhibit the enzyme responsible for GLP-1 degradation (dipeptidyl peptidase-4). Liraglutide, a human GLP-1 analogue sharing 97% of its amino acid sequence identity with native GLP-1, has been approved for use as monotherapy (not in Europe) and in combination with selected oral agents. In this supplement, we summarise key liraglutide data, offer practical insight into what we might expect of liraglutide in clinical use and examine selected case studies. For reasons of the safety and efficacy of GLP-1 receptor agonists, many thought leaders believe that these will become background therapy for majority of patients in the coming years. This supplement will serve as a resource from which readers can extract information concerning the potential benefits for patients who are overweight, losing pancreatic beta-cell function and drifting towards the ravaging effects of chronic hyperglycaemia.

摘要

尽管2型糖尿病的管理取得了进展,但由于疾病进展的复杂性以及需要在改善血糖控制与不良治疗效果(尤其是体重增加和低血糖)之间取得平衡,许多患者的血糖控制仍未达到最佳状态。因此,新型抗糖尿病疗法的研发仍在积极进行。肠促胰岛素激素是近期的研究重点,因为它们在餐后胰岛素反应中占比高达70%。一种激素,即胰高血糖素样肽-1(GLP-1)的生理作用与患者的治疗需求之间也高度一致。由于天然人GLP-1的半衰期仅约2分钟,研究人员已开发出作为GLP-1受体激动剂或抑制负责GLP-1降解的酶(二肽基肽酶-4)的分子。利拉鲁肽是一种与人天然GLP-1氨基酸序列一致性达97%的人GLP-1类似物,已被批准用作单一疗法(欧洲除外)以及与某些口服药物联合使用。在本增刊中,我们总结了利拉鲁肽的关键数据,对其临床应用的预期提供实用见解,并审视了一些案例研究。出于GLP-1受体激动剂安全性和有效性的原因,许多思想领袖认为,在未来几年这些药物将成为大多数患者的基础治疗药物。本增刊将成为读者获取信息的资源,从中可以提取有关超重、胰腺β细胞功能丧失以及逐渐走向慢性高血糖破坏影响的患者潜在益处的信息。

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