长效胰高血糖素样肽-1受体激动剂的研究进展

Advance in study of long-acting glucagon-like peptide-1 receptor agonists

胰高血糖素样肽（GLP-1）用于2型糖尿病的治疗正受到广泛关注。自2005年第1个GLP-1受体激动剂艾塞纳肽（exenatide,Byetta）获FDA批准上市至今,已有6种GLP-1受体激动剂相继获批上市。目前上市的GLP-1受体激动剂的体内半衰期相比于天然GLP-1虽然有所延长,但患者仍需每天注射1~2次,因此需开发更为长效化的GLP-1受体激动剂。2014年,两种新的长效GLP-1受体激动剂阿必鲁肽（albiglutide）和多拉鲁肽（dulaglutide）相继获批上市。本文将对长效GLP-1受体激动剂的研究进展进行综述。

Recently,great attention has been paid to research of glucagon-like peptide-1（ GLP-1） used in therapy of type 2 diabetes mellitus. Six GLP-1 receptor agonists have been approved since the first GLP-1 receptor agonist exenatide（ Byetta） was approved by FDA in 2005. The half-lives of marketed GLP-1 receptor agonists are longer than natural human GLP-1,but most of them still need to be injected once or twice daily. So the studies of GLP-1 receptor agonists mainly focus on long-acting GLP-1 receptor agonists. Two new long-acting GLP-1 receptor agonists,albiglutide and dulaglutide,were approved in 2014. The research advance of long-acting GLP-1 receptor agonists was reviewed in this paper.