Tocofibrate is a peroxisomotropic ester compound consisting of both clofibric acid and alpha-tocopherol. Tocofibrate is a hypocholesterolemic drug. Lowering activity of tocofibrate in cholesterol level in blood was no less than that of clofibrate in rats fed high-fat cholesterol diet. In view of the fact that only a fraction of tocofibrate is not hydrolyzed in the liver 24-hr following oral administration, it was reasonable to assume that tocofibrate exerts its effect in an unaltered state rather than as a result of hydrolysis to clofibric acid and alpha-tocopherol. The distribution of tocofibrate clearly differs from that of both clofibrate and alpha-tocofibrate is primarily associated with its effect upon liver peroxisomes. Tocofibrate acts upon peroxisomes to lower plasma lipid levels.