Abstract: Angiogenesis plays an important role in tumor genesis and development. Therefore， anti-angiogenic therapy has become an important part in cancer therapy and throughout the entire therapy process. Vascular endothelial growth factor receptor tyrosine kinase inhibitor （VEGFR-TKI） is small molecular anti-angiogenic drug. This article introduces the domestic and international listed and researching VEGFR-TKIs. The models of single-agent／combined with chemotherapy drugs／combined with targeted drugs can improve the objective response rates（ORR）of advanced non-small cell lung cancer （NSCLC）， lengthen progression-free survival（PFS）. But it was failed to lengthen overall survival（OS）. And the adverse effects of VEGFR-TKIs were greater. How to improve the efficacy and reduce adverse effects will be the direction of future research.