Abstract: As a functional membrane protein, drug transporters play an important role in the absorption, distribution, metabolism and excretion of drugs. The functional omission or inhibition of drug transporters is believed to be involved in the drug-drug interaction and pathogenesis of certain diseases. Understanding the function of drug transporters is highly significant in terms of pharmacokinetics, pharmacodynamics and toxicity of drugs. This article summarized the methods for the study of drug transporters in vitro and in vivo.