Chinese medicine has the earliest record of tumor in the world: it is called “ulcer disease”. It is believed that the cause of tumor is “the deficiency of evil and the deficiency of righteousness”, so the treatment method is based on “regulating qi and blood, helping righteousness and dispelling evil”. In the past, the development of Western medicine attributed the cause of tumor formation to “imbalance of body fluids”, so the treatment method was dominated by “regulating body fluids and correcting imbalance”. With the shift of medical research from macroscopic research to microscopic research under the microscope, there is a substantial change in the concept of anti-cancer, that is, the development of traditional cytotoxic chemotherapeutic drugs is driven by the cell killing mechanism. However, traditional cytotoxic chemotherapeutic agents are less selective in killing both tumor cells and normal cells, so the dose-limiting toxicity prevents them from “making their mark”. The development and refinement of the concept and theory of signal transduction pathways led to the birth of “targeted drugs” that target specific molecules to block the proliferation of tumor cells. The creation and design of targeted drugs are based on “pathway variation” as the cornerstone. “Pathway mutation” refers to the premise that tumor cells transform normal cell signaling pathways into abnormal tumor signaling pathways based on normal cell signaling pathways, so that abnormal mutated genes encode abnormal functional proteins to produce the effect of cell failure to differentiate and mature and unlimited cell proliferation. Targeted drugs work against specific molecules of abnormal tumor signaling pathways, especially because of their selectivity and low side effects, which become precision-guided anti-cancer “missiles”. The crossover and compatibility of cell signaling pathways form cell signaling networks, so the combination of targeted drugs for different target molecules or targeted drugs for multiple target molecules will become the trend of targeted therapy. Targeted drugs interpret “individualized” therapy based on “standardized” therapy, that is: targeted drugs target the common signal transduction pathway of normal cells and tumor cells, but act on the abnormal tumor signal transduction pathway different from the normal cell signal transduction pathway. In other words, the targeted drug targets the common signaling pathway of normal cells and tumor cells, but acts on the molecular target of abnormal tumor signaling pathway different from normal cell signaling pathway. The prerequisite for “individualized” therapy is the detection of individual molecular targets. Individual molecular target detection includes: 1) detection of individual gene mutation targets; 2) detection of individual gene amplification targets; 3) detection of individual gene fusion targets. It is believed that more and more assays will be available to detect more and more molecular targets as research at the molecular cellular level progresses. Targeted drugs as the “pioneer” of precision medicine, but still need traditional cytotoxic chemotherapy drugs. In the war against the tumor army: traditional cytotoxic chemotherapy drugs kill most of the common soldiers, while molecularly targeted drugs target a small number of key leaders to decapitate them, even tumor stem cells/pre-tumor cells. In the recurrence and metastasis caused by tumor evolution, the combination of targeted drugs with different target molecules or targeted drugs with multiple target molecules can play a multi-directional blocking role, and the drug resistance problem of tumor cells can be prevented and avoided to a certain extent. Finally, as the “pioneer” of precision medicine, it is expected that targeted drugs with the improvement of signaling pathways and drug design will be presented like a spring and will bring more epoch-making diagnostic and therapeutic significance.