Abstract: Malignant tumors′ growth and metastasis depend on tumor angiogenesis. Recent studies had found that the integrin αvβ3 had a high expression on the surface of tumor angiogenesis endothelial cells and parts of the tumor cells, it can regulate tumor angiogenesis by cell adhesion, but it does not express on the surface of normal blood vessels or the normal organizations, or only had a low level expression. Thus it can be used as a new target for the tumor angiogenesis imaging and treatment. Recent years, there is a great progress on the design of the integrin αvβ3 targeting agents, the selection of radionuclides, and the latest research on the agents at home and abroad. This article will made a review on how to better design the integrin αvβ3 agents, choose the appropriate radionuclides, and the research direction of these agents.