Abstract: Integrin αvβ3 are heterodimeric transmembrane glycoproteins, consisting of two noncovalently bound transmembrane subunits. It had a high expression on the tumor but it does not expression on the surface of normal blood vessels or the normal organizations or only had a low level expression. It can regulate tumor angiogenesis by cell adhesion. The integrin αvβ3 can specifically recognize and combine with the peptides which containing tripeptide Arg-Gly-Asp(RGD). These RGD peptides are labeled with appropriate nuclide. The PET/CT, SPECT/CT and PET/MRI multimode imaging can be used to examine the tumor integrin αvβ3 expression level. Thus it can be used as a new target for the tumor angiogenesis imaging and therapy. There is a summary on the design of the integrin αvβ3 agents, the choice of appropriate radionuclides and the research direction of these agents.