Anti-tumor molecularly targeted drugs are currently emerging hot tumor treatment modalities. Common drugs include folic acid, various antibodies and porphyrins, among which porphyrins are the most common. Tumor molecularly targeted drugs take advantage of the molecular biological differences between tumor cells and normal cells, such as genes, enzymes, signal transduction and other different characteristics, targeting a specific site, and accumulating or releasing active ingredients in the target site to inhibit the growth and proliferation of tumor cells, and ultimately the death of tumor cells. The pathways of action mainly include the signal transduction pathway regulating cell proliferation, the transduction pathway regulating angiogenesis, and the transduction pathway of loss of function of tumor suppressor genes, etc. Through the above pathways, to achieve the inhibition of tumor cell proliferation or induction of apoptosis, or through the activation of the immune system, to directly identify and kill tumor cells, and so on. Although anti-tumor targeted drugs are the emerging and effective treatment for tumors nowadays, there are still certain risks, such as afatinib may lead to rash and diarrhea; bevacizumab may cause hemorrhage, high blood pressure and other toxic side effects. Therefore, patients should regularly check their liver and kidney functions when undergoing targeted therapy. Tumor molecular targeted drugs, is currently a promising direction for cancer treatment. Patients should not take the drugs on their own, patients need to pay attention to diet and test liver and kidney functions when taking the drugs. If discomfort occurs, it is recommended to consult a doctor as soon as possible, complete the examination and follow the doctor’s instructions for treatment.