Pirinixic acid is a typical fatty acid mimetic and was developed as synthetic antihyperlipidemic agent. While its target remained unknown in the early development, it has later been characterized as dual PPARα/γ agonist. Based on this activity, pirinixic acid has served as a lead compound for several structure-activity relationship (SAR) studies addressing diverse targets for lipid mimetics. Many structural variants of pirinixic acid descendants have been developed and thereby potent agents on metabolic, inflammatory and neuroprotective targets were discovered of which some have proven in vivo efficacy. This article reviews pirinixic acid descendants along with their in vitro-pharmacological profiles, summarizes their in vivo data and finally gives a future perspective for this valuable class of fatty acid mimetics.