Abstract: Non-small cell lung cancer（NSCLC）is one of the most common malignant tumor and a major cause of death from cancer. NSCLC patients often poorly responds to chemotherapy and has a relatively poor prognosis，especially in those patients with brain metastases. NSCLC patients with brain metastases have poor prognosis and worse quality of life； the natural median survival time is only 1-2 months. To some extent，whole brain radiation therapy improves quality of life and prolongs the survival time in NSCLC patients with brain metastases； but the curative effects are still unsatisfactory.In recent years，some research around pemetrexed，temozolomide and epidermal growth factor receptortyrosine kinase inhibitors（EGFR-TKIs）are conducted and achieves certain results. In this paper，we review the progress of drugs in NSCLC with brain metastasis.