Drugs targeting peroxisome proliferator-activated receptors

Abstract

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.

Keywords: PPARα; PPARγ; PPARδ; drug development; dual PPAR agonists; metabolic syndrome; pan PPAR agonists; selective PPAR agonist.