Multidrug resistance，MDR is main limit for successful cancer chemotherapy. The etiology of MDR is complicated. However，among of them， ATP Binding Cassett（ABC）transporters， such as ABCB1， ABCG2， ABCC1， being capable of transporting anti-cancer drug out of tumor cells， down regulating an intracellular accumulation of anticancer drugand resulting in MDR phenotype， are the most common cause. It is the most urgent to conque rMDR in the field of cancer chemotherapy. Here we summarized the ABC transporters-mediated MDR and it sreversal.