The chemotherapy with cytotoxic drugs for gastric cancer has entered a platform. With the progress of molecular biology, the diagnosis and therapy for gastric cancer is at molecular level. Many clinical and basic studies have explored the molecular targets for gastric cancer, such as the human epidermal growth factor receptor 2, the human epidermal growth factor receptor 1, mammalian target of rapamycin, vascular endothelial growth factor, vascular endothelial growth factor receptor 2, fibroblast growth factor receptor 2, hepatocyte growth factor receptor, poly ADP-ribose polymerase, and so on. To date, trastuzumab (the HER2 monoclonal antibodies) and ramucirumab (the VEGFR2 monoclonal antibodies) are effective targeted drugs for advanced gastric cancer, which is confirmed by Phase III clinical study. More drugs against these targets are on the way.