Lifibrol is a hypocholesterolemic compound. The effect of lifibrol on serum cholesterol levels has been examined in several animal models and clinical trials. The efficacy of lifibrol in lowering total cholesterol, LDL cholesterol, and apo B is comparable to the 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, the most potent lipid-lowering drugs known so far. In addition, lifibrol reduces serum triglycerides, lipoprotein (a), and fibrinogen. lifibrol acts synergistically upon key regulatory processes of cholesterol homeostasis: it reduces cholesterol absorption from the intestine, moderately decreases hepatic cholesterol biosynthesis and stimulates the expression of low density lipoprotein receptors, presumably by a sterol-independent mechanism. Lifibrol had been in phase II clinical trials for the treatment of hypercholesterolaemia. However, this study was discontinued. It has the potential to accumulate in the liver and induce hepatic peroxisome proliferation.