The fibrate class of hypolipidemic drugs such as clofibrate and fenofibrate elicit their effects by binding to and activating peroxisome proliferator-activated receptor α (PPARα). Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity, characterized by reduction in serum triglyceride and cholesterol concentrations in rats. In male wistar rats, cetaben increased the activity of all peroxisomal enzymes examined in liver and kidney, whereas clofibrate showed a varied regulatory pattern. In addition to its effects on peroxisomes, cetaben inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology. It also blocked triglyceride synthesis by 99% and reduced cholesterol ester synthesis by >70% at a concentration of 50 µM in these same cells.