Nowadays,cardio-cerebrovascular disease is a major cause of death in China.As a common pathogenic basis of coronary heart disease and stroke,atherosclerosis is a complex pathological process which is controlled by multiple factors.With its unique effects on anti-oxidation,anti-inflammation,cholesterol-lowering and improving endothelial function,probucol has been clinically used in preventing and treating atherosclerosis and coronary artery restenosis after angioplasty for decades.This review describes the situation and prospect in the research of probucol and its derivatives in treating atherosclerosis and restenosis from several aspects such as its mechanism,clinical application and the exploitation of its derivatives.