Rivoceranib (Apatinib) is the first successful small-molecule tyrosine kinase inhibitor to be approved in gastric cancer (China, Dec 2014). It is important to note that in the United States and other jurisdictions, Rivoceranib is investigational and safety and efficacy have not been established. Orphan Drug designation has been granted in the US, Europe and South Korea. It has been clinically tested with over 1,000 patients worldwide. Rivoceranib has also shown potential to improve outcomes in combination treatment with chemotherapeutics and immunotherapy, as well as for maintenance therapy. Additional studies and research will need to be conducted to verify the clinical applications in this context.