Abstract: Carboxylesterase, arylacetamide deacetylase, butyrylcholinesterase, paraoxonase are important esterases in the human body, participating in the metabolism, activation and detoxification of drugs in the body, thus with a very important role in the design of prodrugs.This paper focuses on the esterases that are widely involved in drug metabolism in human body, and summarizes their tissue distribution in vivo, substrate and inhibitor and species differences, aiming to provide reference for preclinical selection of animal models, drugs design and development of new drugs.