胰高血糖素样肽1受体激动剂(GLP-1 receptor agonists, 简称GLP-1肽),通过增强β胰腺细胞分泌胰岛素和抑制α胰腺细胞释放胰高血糖素来改善血糖控制。[5] 此外,激动剂会减缓胃排空、增加饱腹感并降低食欲 ,导致体重减轻。GLP-1肽可以分为短效或长效药物。[6] 短效激动剂循环数小时,长效激动剂产生持久的药物浓度,...
2023年12月7日,美国凯斯西储大学医学院的研究人员在 JAMA 子刊 JAMA Oncology 上发表了一篇题为:GLP-1 Receptor Agonists and Colorectal Cancer Risk in Drug-Naive Patients With Type 2 Diabetes,With and Without Overweight/Obesity 的研究论文。 该研究发现,无论是否肥胖,与其他抗糖尿病药物相比,GLP-1受体激...
[5] McIntyre RS, Mansur RB, Rosenblat JD, Kwan ATH. The association between glucagon-like peptide-1 receptor agonists (GLP-1 RAs) and suicidality: reports to the Food and Drug Administration Adverse Event Reporting System (FAERS). Expert Opin Drug Saf. 2024 Jan;23(1):47-55. doi: 10.1080...
临床前数据表明,相较于单独GLP-1类似物或单独雌激素,GLP-1/雌激素结合产物可增强小鼠厌食、减重、促胰岛素和胰岛保存作用[83-85]。而这种GLP-1/雌激素结合物并没有雌激素独有的促子宫内膜增生的效应,仅体现GLP-1成分介导的治疗指标改善。GLP-1R靶向作用也...
[7] Bettge, K., Kahle, M., Abd El Aziz, M.S., Meier, J.J., Nauck, M.A. 2017. Occurrence of nausea, vomiting and diarrhoea reported as adverse events in clinical trials studying glucagon-like peptide-1 receptor agonists: A systematic analysis of published clinical trials. Diabetes Obe...
度拉糖肽由两个GLP-1分子通过甘氨酸和丝氨酸为基础的间隔基在其C-端融合到人免疫球蛋白G4(IgG4)的Fc片段。 天然GLP-1的化学修饰对提高GLP-1RA治疗T2DM和肥胖的药理学价值至关重要。G…
2023年12月7日,美国凯斯西储大学医学院的研究人员在JAMA子刊JAMA Oncology上发表了一篇题为:GLP-1 Receptor Agonists and Colorectal Cancer Risk in Drug-Naive Patients With Type 2 Diabetes,With and Without Overweight/Obesity的研究论文。 该研究发...
2023年12月7日,美国凯斯西储大学医学院的研究人员在JAMA子刊JAMA Oncology上发表了一篇题为:GLP-1 Receptor Agonists and Colorectal Cancer Risk in Drug-Naive Patients With Type 2 Diabetes,With and Without Overweight/Obesity 的研究论文。 该研究发现,无论是否肥胖,与其他抗糖尿病药物相比,GLP-1受体激动剂与...
[9] Zhang, Xiaolong, et al. "Discovery of novel OXM-based glucagon-like peptide 1 (GLP-1)/glucagon receptor dual agonists." Peptides 161 (2023): 170948.[10] Liu, Chunxia, Yuxing Zou, and Hai Qian. "GLP-1R agonists for the treatment of obesity: a patent review (2015-present)." ...
GLP-1具有葡萄糖浓度依赖性降糖作用,其受体激动剂(GLP-1RA)能模拟GLP-1的生理作用,是治疗糖尿病与肥胖症的重要药物。此外,GLP-1RA亦对心血管系统、肾脏、中枢神经系统等有保护作用。 来源:Anti-obesity drug discovery: advances and challenges.Nature Reviews....