Abstract: Peroxisome proliferator-activated receptor α(PPARα)is an important subtype in the PPARs family, which are a group of nuclear hormone receptors belonging to type II nuclear receptor super family. PPARα agonists, which used in the treatment of hyperlipemia in clinic, mainly include natural and synthetic types. According to the structure, the synthetic PPARα agonists can be divided into phenyl-heterocyclic derivatives, ureide derivatives, amide derivatives, phenyloxazole or phenylthiazole derivatives, etc. Up to now, many PPARα agonists have been approved or in clinical development, and a series of novel PPARα agonists with higher activity and selectivity are being developed. This review will summarized the progress in PPARα agonists according to their structural classification.