Leptomeningeal metastasis（LM） is a common complication of advanced non-small cell lung cancer（NSCLC）. About 5%-10% of patients with advanced NSCLC may experience LM，and a lack of effective treatment leads to an extremely short survival time of these patients. Although there are various treatment methods for NSCLC patients such as platinum-based dual-drug chemotherapy，whole-brain radiotherapy，and intrathecal injection，they often have limited effects in improving patients’ survival time. In recent years，biologically targeted therapy has become one of the hot research fields. Epidermal growth factor receptor-tyrosine kinase in－hibitors，anaplastic lymphoma receptor tyrosine kinase inhibitor，and anti-angiogenic drugs have been used in the treatment of NSCLC patients with central nervous system metastasis. Previous studies have demonstrated that these biologically targeted drugs can effec－tively prolong the survival time of NSCLC patients. This article reviews the research advances in biologically targeted therapy for NSCLC patients with LM.