Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics) - preclinical and clinical results
Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics) - preclinical and clinical results
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DOI：
10.1016/j.beem.2009.03.008
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发表时间：
2009-08-01
影响因子：
7.4
通讯作者：
Madsbad, Sten
中科院分区：
文献类型：
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作者：
Madsbad, Sten
GLP-1类似物依塞那肽和利拉鲁肽以葡萄糖依赖性方式刺激胰岛素分泌并抑制胰高血糖素输出，减缓胃排空并降低食欲。可注射的胰高血糖素样肽-1（GLP-1）受体激动剂艾塞那肽可显著改善血糖控制，治疗30周后，HbA 1c平均降低约1.0%，空腹血糖约为1.4 mmol l（-1），体重减轻约2-3 kg。副作用是短暂的恶心和呕吐。每日一次的长效人GLP-1受体激动剂利拉鲁肽可使HbA 1c降低约1.0-2.0%，体重降低1-3 kg，且胃肠道副作用似乎比艾塞那肽更少。GLP-1受体激动剂在糖尿病治疗方案中的最终地位将在我们有心血管终点的长期试验和说明对2型糖尿病进展影响的数据时阐明。(C)2009爱思唯尔有限公司版权所有。
The GLP-1 analogues exenatide and liraglutide stimulate insulin secretion and inhibit glucagon output in a glucose-dependent manner, slow gastric emptying and decrease appetite. The injectable glucagon-like peptide-1 (GLP-1) receptor agonist exenatide significantly improves glycaemic control, with average reductions in HbA1c of about 1.0% point, fasting plasma glucose of about 1.4 mmol l(-1), and causes a weight loss of approximately 2-3 kg after 30 weeks of treatment. The adverse effects are transient nausea and vomiting. The long-acting once-daily human GLP-1 receptor agonist liraglutide reduces HbA1c by about 1.0-2.0% point, weight by 1-3 kg and seems to have fewer gastrointestinal side effects than exenatide. The final place of the GLP-1 receptor agonists in the diabetes treatment algorithm will be clarified when we have long-term trials with cardiovascular end-points and data illustrating the effects on the progression of type 2 diabetes. (C) 2009 Elsevier Ltd. All rights reserved.