目前,许多以胰高血糖素样肽-1(GLP-1)为基础的、联合其他胃肠激素发挥促进或协同作用的单分子多重受体激动剂正处于临床前和临床开发阶段,且已表现出协同增效、提高耐受性和改善安全性等益处。以GLP-1为基础的单分子多重受体激动剂主要有五类,包括GLP-1/胃抑制肽(...
HRS9531作为GLP-1/GIP双受体激动剂,激活GIP受体和GLP-1受体信号通路,通过对胰岛β细胞的双重作用来增强胰岛素分泌,对大脑两种受体信号通路的激活产生更强烈的抑制食欲作用,同时GIP发挥对脂肪存储和脂肪组织功能的重要调控作用,表现为增加白...
与第一代GLP-1R激动剂相比,替尔泊肽作为GLP-1/GIP双受体激动剂,有三个关键的改进:首先,肽骨架中的许多残基被改变以获得GIPR激活活性;第二,艾塞那肽的C末端序列延长了C末端;第三,一个脂肪酸侧链是共轭的类似于semaglutide延长半衰期。通过研究每个位置采用的不同残基,可以定制双激动剂的活性。最初,主要关注的是...
4.Zhao L, et al. 1861-LB#Efficacy and Safety of HRS9531, a Novel Dual GLP-1/GIP Receptor Agonist, in Obese Adults: A Phase 2 Trial. Presented at ADA 2024.
[4]Müller TD,Finan B,Bloom SR,et al.Glucagon-like peptide 1(GLP-1).Mol Metab 2019;30:72-130. [5]Pelle MC,et al.Role of a Dual Glucose-Dependent Insulinotropic Peptide(GIP)/Glucagon-like Peptide-1 Receptor Agonist(Twincretin)in Glycemic Control:From Pathophysiology to Treatment.Life(Basel...
me/src/EventPilot/php/express/web/page.php?page=IntHtml&project=ADA23&id=789.3. Zhao J, et al.LBA 66Efficacy and safety of HRS9531, a novel dual GLP-1/GIP receptor agonist, in patients with type 2 diabetes mellitus (T2DM): a phase 2 trial. Presented at EASD annual meeting.
GIP-GLP-1 DUAL AGONIST COMPOUNDS AND METHODSThe present invention relates to the acylation GIP analog with GIP and GLP-1 double activities and its purposes in treatment metabolic disease.Anne Pernille Tofteng SHELTONPia NRREGAARDJacob Ulrik FOG...
1. Zhao L, et al. 1861-LB#Efficacy and Safety of HRS9531, a Novel Dual GLP-1/GIP Receptor Agonist, in Obese Adults: A Phase 2 Trial. Presented at ADA 2024. 2. Nauck, et al. Lancet Diabetes Endocrinol.2016; 4: 525-36.
4.Zhao L, et al. 1861-LB#Efficacy and Safety of HRS9531, a Novel Dual GLP-1/GIP Receptor Agonist, in Obese Adults: A Phase 2 Trial. Presented at ADA 2024. 声明: 1. 本新闻旨在分享研发前沿资讯,仅供医疗卫生专业人士基于学术目的参阅,非广告用途。
1. 吴霞, 等. 中华糖尿病杂志. 2022; 14(11): 1321-1326. 2. eppro02.ativ.me/src/Eve. 3. Zhao J, et al.LBA 66Efficacy and safety of HRS9531, a novel dual GLP-1/GIP receptor agonist, in patients with type 2 diabetes mellitus (T2DM): a phase 2 trial. Presented at EASD annual ...