With the improvement of people’s living standard and quality, the incidence of oral and maxillofacial tumors, like the whole body tumors, has been increasing year by year. For larger tumors or tumors with lymph node metastasis, traditional radiotherapy and chemotherapy have a lot of side effects. It is increasingly accepted by tumor therapists to select the specific target of tumor cells and apply drugs targeting that target for treatment, so as to avoid harming normal cells and achieve a treatment mode with high efficiency and low side effects. What is targeted therapy for tumors? In terms of molecular tumor therapy, it means targeting a certain cancer cell, or a certain protein or molecule of cancer cells for treatment. It is divided into three levels, the first one is to target a certain organ, for example, a certain drug is only effective for tumors in a certain organ, this is called organ targeting; the second one is called cell targeting, as the name implies, it refers to targeting only a certain type of tumor cells, the drug can selectively bind to such cells after entering the body, thus causing apoptosis; the third one is molecular targeting, it refers to targeting a certain part of molecules in a certain protein family in tumor cells. The third type is molecular targeting, which refers to the treatment of a certain part of a protein family of molecules, or a fragment of a nucleotide, or a gene product inside a tumor cell. Molecular targeted therapy is a “flash point” in tumor treatment, with its specificity and effectiveness, it has achieved great success and is a “hot spot” in domestic and international treatment. Traditional chemotherapy can be interpreted as “shooting the birds in the head”, which mainly targets the fast-growing tumor cells. However, besides tumor cells, some normal cells in normal human body also grow and multiply faster. While targeting tumor cells in the body, chemotherapy drugs will inevitably cause different degrees of damage to normal cells in the body that are growing vigorously. In this way, the tumor cells will be killed and many cells in the body will be buried with them, which will only cause “both losses” in the long run. However, as the immunity of the body is destroyed, the tumor cells are bound to “rise”. Therefore, the blindness of chemotherapy is not conducive to the long-term treatment of tumors, and is not targeted therapy in the true sense. Likewise, the so-called targeted chemotherapy, targeted radiotherapy, targeted surgery, argon helium targeted and radiofrequency targeted treatment inevitably also have the problem of greater damage to normal tissues or incomplete treatment. Cell-targeted therapy is also called “missile therapy”, which mainly takes advantage of the difference in biological characteristics between tumor cells and normal cells, and has high selectivity, and can strike tumor cells steadily, accurately and viciously. Molecular targeting is the highest level of specificity in targeted therapy. Molecular targeting is a new biological therapy that targets the links that may lead to cell cancer, such as cell signaling pathways, proto-oncogenes and oncogenes, cytokines and receptors, anti-tumor angiogenesis, suicide genes, etc., and reverses the malignant biological behavior from the molecular level, thus inhibiting the growth of tumor cells and even making them completely disappear. It is a new biological treatment mode. It is a treatment that targets a molecule of a protein, or a fragment of a nucleotide, or a gene product inside a tumor cell. It targets the difference between tumor cells and normal cells, and only attacks tumor cells, with very little effect on normal cells, so it is said to be “stable, accurate and hard”. The basic procedure of tumor molecular targeting treatment: firstly, we complete the sampling by means of surgical biopsy, puncture biopsy, microscopic sampling and fluid collection, and then we use conventional pathology, immunohistochemistry, gene mutation, Southern, PCR, ELISH, FISH, CISH, etc. to complete the histocytological examination and consultation, so as to determine the tumor type. At the same time, targeted molecular pathology indexes are completed. In conclusion, molecular targeted therapy has become the main direction and trend of tumor treatment in the 21st century. How to better combine molecular targeted therapy with other therapies to improve the therapeutic effect and survival quality will undoubtedly help biotherapy play a more important role in comprehensive tumor treatment and bring gospel to people’s health.