GLP-1受體激動劑的臨床研究進展
發(fā)布時間:2018-05-15 04:05
本文選題:型糖尿病 + GLP-受體激動劑; 參考:《中國新藥雜志》2015年19期
【摘要】:當(dāng)前研究已經(jīng)顯示2型糖尿病同肥胖癥具有并發(fā)趨勢,臨床上也公認將控制患者體重列入到2型糖尿病治療指南中。目前在已經(jīng)過驗證的治療方案中,只有胰高血糖素樣肽受體激動劑(glucagon-like peptide-1 receptor agonists,GLP-1 RAs)可以實現(xiàn)對患者的體重和血糖水平同時調(diào)控。GLP-1作為GLP-1受體激動劑研究的基礎(chǔ),具有血糖依賴性的促進胰島素分泌作用。其可以通過抑制食欲和減緩胃排空來達到減輕體重的作用。天然的GLP-1由于受到二肽基肽酶(dipeptide peptidase,DPP-Ⅳ)的降解作用,半衰期僅為2 min。為了延長GLP-1 RAs的體內(nèi)半衰期,多種改造策略被應(yīng)用于新型GLP-1受體激動劑的研究開發(fā),目前此類GLP-1受體激動劑已部分進入臨床評估階段,給藥頻率將從每周1次延長到每月1次。本文將對近年來已進入臨床試驗研究的GLP-1受體激動劑進行綜述。
[Abstract]:Current studies have shown that type 2 diabetes has a tendency to be associated with obesity, and it is also recognized that weight control is included in the treatment guidelines for type 2 diabetes. At present, only glucagon-like peptide-1 receptor agonists, glucagon-like peptide-1 receptor agonistsGLP-1 RAsS, have been proven to be the basis for simultaneous regulation of body weight and blood glucose levels as GLP-1 receptor agonists. Promote insulin secretion in a glucose dependent manner. It can reduce weight by suppressing appetite and reducing gastric emptying. The natural GLP-1 was degraded by dipeptidyl peptidase (DPP- 鈪,
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