Abstract: Fatty acid-binding proteins (FABPs) are a group of intracellular lipid chaperones with low molecular weight that play important roles in regulating the metabolism of glucose and lipid and inflammatory responses. Studies have shown that simultaneous inhibition of both FABP4 and FABP5 can significantly improve metabolic stress-induced disorders of lipid metabolism, and attenuate chronic metabolic inflammation. In recent years, FABP4 and FABP5 have attracted much attention as potential targets for developing drugs for metabolic diseases (such as type 2 diabetes, atherosclerosis and fatty liver, et al). This article summarized the latest research progresses in dual inhibitors of FABP 4 and 5 with a focus on the correlation between FABP4/5 and diseases, structure-activity relationship of the inhibitors and the crystal structures of protein-inhibitor complexes, so as to provide reference for the design of novel FABP4/5 dual inhibitors.