For many years, studies on cholesteryl ester transfer protein inhibitors(CETP) have not been interrupted, intending to achieve further cardiovascular protection through increasing the level of HDL-C on the basis of statin-lowering LDL-C. However, the failure of large clinical studies of CETP inhibitors represented by torcetrapib has caused continuous controversy in this area of research. The 2017 European Society of Cardiology Annual Conference published the results of Phase 3 clinical trials on Anacetrapib, which regained significant attention to CETP inhibitors. Based on these, this article reviewed the development of the four major CETP inhibitors, and briefly discusses their clinical effects and differences.