A review.As RGD can specifically bind to integrin αvβ3, which is up-regulated in both tumor and tumor-endothelial cells, this enables the targeting of diagnostics and therapeutics of tumor using the affinity between RGD and its receptor.Previous studies and data from clin. trials demonstrated RGD imaging agents can target tumor tissues.RGD-nano antitumor agents (RGD-liposome, RGD-micelle, RGD-nanoparticle) have greater cellular uptake and higher cytotoxic in vitro, make more effective in tumor growth inhibition and prolong survival times in xenograft models.Tumor incidence increases year by year, but therapeutics and efficacy are still very limited.The advantage of RGD-peptidomimetic agents in targeting of diagnostics and therapeutics deserve special attention.