Given their key roles in tumor progression, integrins are attractive targets for cancer therapy. Several integrin inhibitors, including monoclonal antibodies and small molecules, are currently being investigated in clinical trials. For example, cilengitide, an inhibitor of integrins αvβ3 and αvβ5, has shown promise in the treatment of glioblastoma. However, the efficacy of integrin-targeted therapies has been variable, and ongoing research aims to identify optimal strategies for their use.