Recently, interest has increased in the hypothesis that low-density lipoprotein (LDL) modified by oxidation may lead to the initiation and to the development of atherosclerosis. In vitro studies of cellular interactions with LDL have revealed that various cells, including endothelial cells and smooth muscle cells, can oxidize LDL. The biochemical changes in LDL may further enhance its atherogenic potential. In addition to these in vitro studies, there is in vivo evidence for oxidized LDL in atherosclerotic lesions and for circulating antibodies against oxidized LDL. Probucol, 4,4'-(isopropylidenedithio)bis(2,6-di-tert-butylphenol), is a widely used cholesterol-lowering drug. Recently, there has been accumulating evidence for other mechanisms of probucol's antiatherogenic effects apart from cholesterol-lowering action. Attention has especially focused on probucol's antioxidant action in the mechanism of antiatherogenesis. In the present article, we will summarize the antiatherogenic and antioxidant actions of probucol.