In physiological conditions, angiogenesis is a process responsible for the generation of new blood vessels in order to provide oxygen and nutrients to peripheral tissues and to maintain correct levels of perfusion. However, when the same process becomes uncontrolled such as in the case of cancer, the formation of new blood vessels becomes a pathological factor, which dramatically worsens patients’ clinical outcomes. The angiogenic process is majorly regulated by the interactions between tissue vascular endothelial growth factor (VEGF) and their soluble ligands (VEGFRs). Mesylate apatinib, as a domestically developed anti-angiogenesis drug, is a small-molecule tyrosine kinase (TK) inhibitor, which can exert its anti-angiogenesis effect and thereby achieve anti-tumor effect by specifically inhibiting VEGFR-2 pathway. It is now included in domestic guidelines, especially for the advanced gastric cancer. Clinical researches such as lung cancer, breast cancer, hepatocellular carcinoma (HCC) are under way.