Xie Zhouling, Xin Jiwei, Huang Chuping, Liao Chenzhong
Department of Pharmaceutical Sciences and Engineering, School of Food and Biological Engineering, Hefei University of Technology, Hefei, China.
Department of Pharmaceutical Sciences and Engineering, School of Food and Biological Engineering, Hefei University of Technology, Hefei, China.
Drug Discov Today. 2025 Mar;30(3):104318. doi: 10.1016/j.drudis.2025.104318. Epub 2025 Feb 20.
The year 2024 witnessed the accelerated approvals of two peroxisome proliferator-activated receptor (PPAR) agonists for the treatment of primary biliary cholangitis (PBC). PPARs, including three isoforms (PPARα, PPARγ, and PPARδ), are therapeutic targets generating considerable debate yet also seeing significant advances in their successful targeting. Currently, selective PPAR agonists are used to manage hyperlipidemia, type 2 diabetes mellitus (T2DM), and PBC, and dual/pan-PPAR agonists have been developed to address various disorders. In this review, we summarize the PPAR agonists approved globally, and their pros and cons as therapeutic agents for various diseases, with a particular focus on those agonists marketed since 2010.
2024年，两种过氧化物酶体增殖物激活受体（PPAR）激动剂被加速批准用于治疗原发性胆汁性胆管炎（PBC）。PPAR包括三种亚型（PPARα、PPARγ和PPARδ），是治疗靶点，引发了大量争论，但在成功靶向方面也取得了重大进展。目前，选择性PPAR激动剂用于治疗高脂血症、2型糖尿病（T2DM）和PBC，并且已经开发出双/泛PPAR激动剂来治疗各种疾病。在本综述中，我们总结了全球范围内批准的PPAR激动剂，以及它们作为各种疾病治疗药物的优缺点，特别关注自2010年以来上市的那些激动剂。
