Abstract: Antineoplastic drug-induced liver injury（DILI），one of the most common clinical problems，has been increasingly concerned. As multifunctional hepatoprotective drugs of anti-inflammatory class，glycyrrhizin，especially the latest glycyrrhizin magnesium isoglycyrrhizinate，has been used for the prevention and treatment of DILI recently. This paper reviewed the current situation and research progress of magnesium isoglycyrrhizinate in the prevention and treatment of DILI in the hematological malignancy，solid tumor，hepatic artery embolism chemotherapy and molecular target therapy，and discussed the future direction of development.