Fig. 1: Literature FXR and PPAR agonists.

Obeticholic acid (OCA, 6α-ethylchenodeoxycholic acid, 1) and tropifexor (2) are FXR agonists that are currently undergoing clinical trials for NASH. Seladelpar (3), a selective PPARδ agonist, and the dual PPARα/δ agonist elafibranor (4) are additional investigational drugs for NASH. Phenylacetic acid 520 served as a lead structure for dual FXR/PPAR partial agonists.