Abstract: As the first marketed epidermal growth factor receptor tyrosine kinase inhibitor, gefitinib plays an important role in the targeted therapy of malignant tumors such as non-small cell lung cancer, but this drug can cause serious adverse effects such as liver toxicity. If the reaction occurs, the drug must be stopped for liver protection treatment, which greatly affects the treatment process of cancer. However, the mechanism of gefitinib-induced hepatotoxicity is still unclear, and clinical treatment measures are very limited. This article aims to review the molecular mechanism of gefitinib-induced hepatotoxicity and the commonly used clinical therapeutic drugs, so as to provide scientific basis for clinical prevention and rational drug use.