There are overwhelming epidemic evidences that both an elevated concentration of low-density lipoprotein cholesterol (LDLC) and a low concentration of high-density lipoprotein cholesterol (HDLC) are independent risk factors of atherosclerotic cardiovascular disease (CVD). Theoretically, the level of HDLC will rise when cholesteryl ester transfer protein (CETP) is inhibited, leading to treatment of CVD. To date, the results of basic and clinical studies on CETP are not consistent. Perhaps it is not an easy choice for drugs based on inhibition of CETP. The paper illustrates the physiological role of CETP in lipid metabolism, the relationship between CETP and atherosclerosis in some animal studies, and the phase Ⅲ clinical trial of the effects of CETP inhibitors on cardiovascular disease. It will review current status of CETP inhibitors in details.