PB-718 a dual agonist that activates both the GLP-1 receptor and the glucagon receptor

  • 产品概览
  • 作用机理
  • 产品特点与优势
  • 研究进展
  • PB-718 is a dual agonist that activates both the GLP-1 receptor and the glucagon receptor. The two activated receptors are associated with suppressed appetite, weight loss, and increased energy expenditure, creating a synergistic effect superior to that of either of the receptor agonist acting alone. In addition, PB-718 can reduce lipid accumulation in liver which prevents hepatic cell death and consequent liver fibrosis. Thus, PB-718 has the therapeutic potential for treating non-alcoholic fatty liver disease (NAFLD).

    PB-718 has been identified from screening multiple dual agonists to reach the optimal activation of both receptors, so as to pursue maximal weight loss and improvement in NAFLD while ensuring the drug safety.

    Moreover, PB-718 is PEGylated to prolong the drug half-life, which reduces the administration frequency to once per week. This will greatly increase the convenience of use of PB-718 in NASH/NAFLD patients. The phase I clinical trial of PB-718 is currently ongoing in US.
  • PB-718是GLP-1受体及胰高血糖素受体双激动剂,通过筛选和控制两种受体的激活程度,在确保药物安全性的同时,达到最优的减重和改善非酒精性脂肪肝病的效果。此外,PB-718通过聚乙二醇化修饰,延长药物的半衰期,实现一周一次给药,极大提高了非酒精性脂肪肝病患者的用药便利性及依从性。研究表明,GLP-1受体及胰高血糖素受体激活的程度是决定体重下降和非酒精性脂肪肝病改善程度的重要因素。
  • 1) 最优比例激活受体,双靶点协同达到最佳改善非酒精性脂肪肝病效果
    2) 显著降低体重,改善肝脏脂代谢并减轻肝脏病理组织变化和肝纤维化
    3) 一周一次给药,改善患者用药体验
  • PB-718目前正在美国开展针对非酒精性脂肪肝的临床I期研究,评估单次和多次给药,不同剂量下PB-718对健康受试者的安全性和耐受性以及药物代谢情况。