Abstract: Treatment of advanced malignant tumors after failure of multiple lines therapy has been a hotspot of clinical research, and there is no unified standard in multiple lines of therapy so far. Neovascularization plays a key role in the tumor development and metastasis. Vascular endothelial growth factor and its receptor (VEGF/VEGFR) signal pathway are of great importance in regulating and controlling angiogenesis. Inhibition of this signal pathway is a major target in anti-tumor therapy. Mesylate apatinib is a kind of novel small molecule inhibitors of VEGFR-2 tyrosine kinase. Studies have shown that in clinical trials and preclinical experiments, apatinib shows good antitumor effect and safety in treatment of a variety of malignant tumors such as gastrointestinal cancer, non-small cell lung cancer and breast cancer. These research findings are reviewed in this paper, which may provide evidence for clinical decision.