There are many transporters in the blood-brain barrier with influence on the behavior of the drugs through acrossing the blood-brain barrier and different drug concentrations in the brain.Studying the signif- icant role of transporters in drug blood-brain bander can provide deep analysis of the drug kinetics in the blood- brain barrier transport with effective regulation and helpful for understanding the interaction between the trans- porters and substrate;and furthermore with guidance to the research and development of drugs including brain- targeting and nonbrain-targeting.This article comprehends the significant role of the transporters in drug blood- brain barrier.