Angiogenesis plays an important role in the transformation of tumors from benign to malignant, the entry of cancer cells into the blood circulation, and the development and rupture of metastases, involving the whole process from tumor formation to metastasis. In recent years, the rapid development of anti-angiogenic drugs has provided new means and solutions for the treatment of malignant tumors. Since these drugs have the characteristics of targeting and non-cytotoxicity, and mainly play a regulatory and stabilizing role on tumor cells, they are very different from cytotoxic drugs, and their mechanism of action and clinical application are different from cytotoxic drugs. Endostar (YH-16) is a humanized broad-spectrum anti-angiogenic drug developed by Centrum Medizin Bioengineering Co. Compared with the natural vascular endothelial inhibitor, Endo has added 9 amino acid sequences at the N-terminal end, which prolongs the half-life, improves the biological activity and stability, and solves the protein compounding and purification technology; it adopts E. coli as the expression system, realizes large-scale industrial fermentation production, low cost, uniform product conformation, stable and reliable quality. In September 2005, Endo received the manufacturing approval and new drug certificate of the first class of therapeutic biological products issued by SFDA, and was marketed. Clinical trials have shown that the combination of Endo with anti-tumor drugs can significantly improve the clinical benefit rate (CRB) and extend the overall survival (OS) of patients. Endo was approved in combination with NP (vincristine + cisplatin) chemotherapy regimen for the treatment of patients with primary or relapsed stage III/IV non-small cell lung cancer. It has been included in NCCN’s clinical practice guidelines for non-small cell lung cancer (Chinese version) for 3 consecutive years. Endo is often used in combination with standard chemotherapy regimens in clinical practice. At present, many units in China have extended its scope of application for the treatment of head and neck, gastrointestinal and reproductive system tumors, as well as malignant thoracic and ascitic fluid, etc. It is generally not used alone. It is characterized by high efficiency, low toxicity, no drug resistance, clear therapeutic targeting, anti-tumor effect and no inhibition of normal cell growth, and can be used in combination with other chemotherapeutic drugs, which has good clinical application prospects. This paper reviews the clinical application of recombinant human vascular endothelial inhibitor (Endo), a new class I drug in China. Endo is generally easy to be tolerated, with less non-specific toxicity than chemotherapeutic drugs, and the degree of adverse reactions is mild, and the combination of Endo does not increase the toxic side effects of chemotherapy regimens. Common adverse reactions include cardiac reactions, gastrointestinal reactions, skin and adnexal reactions, etc. Endo has the characteristics of low toxicity, high efficiency and strong targeting, which can inhibit tumor proliferation, invasion, recurrence and metastasis by inhibiting the formation of new blood vessels. Endo is a great progress in molecularly targeted tumor therapy, and has achieved certain efficacy both in non-small cell lung cancer and solid tumors such as extra-pulmonary tumors, and will be applied to the treatment of more tumors as research progresses. Meanwhile, the efficacy evaluation system of angiogenesis inhibitors (TAI) such as Endo needs to be further improved, the combined application with radiotherapy and molecular targeted drugs needs to be studied in depth, and there is still a lot of work to be done to explore new molecular markers to predict and evaluate the efficacy of Endo using modern biological techniques.