Abstract: Glycyrrhetinic acid(GA) is belong to pentacyclic triterpene which is a major active ingredient in licorice, a famous traditional Chinese medicine. It has the effect of anti-inflammation, anti-virus, anti-ulcer and immune regulation. In recent years, it has been found that GA also has high broad spectrum anti-tumor activity, and its anti-tumor mechanism has attracted a great deal of attention. The mechanism of multidrug resistance(MDR) is very complex, and in current, MDR is still the obstacles and challenges of chemotherapy in clinical treatment of tumors. GA has the advantages of good pharmacological activity and low toxicity. The latest research shows that GA can reverse the multidrug resistance of tumor, but also can become a chemosensitizer in chemical resistance caused by various chemotherapy drugs. This paper discusses the mechanism of MDR, and the research progress of GA in reversing the multidrug resistance is reviewed in this paper.