This paper, from the perspective of small molecule drugs regulating reverse cholesterol transport mechanism, introduces the latest research progress in the role of RCT key proteins in the regulation of cholesterol efflux and lipid metabolism by small molecule drugs, and explore the role of small molecule drugs with different chemical structures in mediating the expression of different drug target proteins in RCT. The purpose of this study is, from a point of view of pharmacology, to provide a new thinking mode for RCT related research.