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Epidemiological studies have shown that low-density lipoprotein cholesterol (LDL-C) is a strong risk factor for coronary heart disease (CHD), whilst high-density lipoprotein cholesterol (HDL-C) reduces the risk for CHD. Therefore, strategies to manage dyslipidemia in an effort to prevent or treat CHD have primarily attempted to decrease LDL-C and raise HDL-C levels. Cholesteryl ester transfer protein (CETP) inhibitors have proven to be effective in achieving both a reduction in LDL-C and an increase in HDL-C. This review will discuss the current status and future prospects of CETP inhibitors in the treatment of CHD.