Abstract: Integrin α_Ⅴβ₃ is significant to tumor angiogenesis, which is necessary for tumor growth and metastasis. So, it’s beneficial for us to make noninvasive visualizations and targeted treatments in tumor patients to detect malignant tumors and inhabit tumor metastasis early by using radiolabeled integrin α_Ⅴβ₃ antagonists which have high specificity and affinity to integrin α_Ⅴβ₃. This article will focus on the current researches on nonpeptide small molecular antagonists of integrin α_Ⅴβ₃ by computerassisted drug design(CADD) to review the nonpeptide antagonists of integrin α_Ⅴβ₃ in present progress. Also, it makes an analysis on the applications of radiolabeled small molecular antagonists as probes in tumor imaging.