Drug development in the treatment of malignant tumors over the last 50 years has focused on cytotoxic aggressive agents. Although many powerful chemotherapeutic drugs such as Tessoderm, Kepto, Platinum Oxalate, and Kenzei have been introduced and have played important roles in various different cancers, they are still of the nature that they cannot distinguish between tumor cells and normal cells, and their clinical applications are limited by many factors. Entering the twenty-first century, the strategy of antitumor drug research and development is to continue to develop cytotoxic drugs on the basis of in-depth development of cytotoxic drugs, and at the same time gradually introduce the development of molecular-targeted drugs. At present, many targeted drugs have played an extremely important and even miraculous role in clinical practice, and have entered into the standard therapeutic protocols and norms recognized by the international oncology community in accordance with the principles of evidence-based medicine. Tumor drug therapy is in a period of transition from pure cytotoxic attack to molecular targeted regulation, and its application has great prospects. Meanwhile, the combination of traditional Chinese medicine and molecular targeted therapy has also become one of the hot spots of research in recent years.