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This paper discussed the impact of molecular imaging on clinical and preclinical medicine. Potential problems of delivering the effective therapeutic dose and the properties that can help contribute to the drug efficacy were presented. The rationale for the design of new antiangiogenic agents that can be used for imaging and therapy was presented. Finally, results from imaging and targeted nanoparticle-based therapies were presented. In vivo imaging of angiogenic tumors using anti-αvβ3-targeted polymerized vesicles composed of the murine antibody LM609 attached to nanoparticles labeled with the MR contrast agent gadolinium in the V2 carcinoma model in rabbits. MRI studies using this targeted contrast agent revealed large areas of αvβ3 integrin expression in tumor-associated vasculature that conventional MRIs failed to show. By modification of the nanoparticles this imaging agent was used as an antiangiogenic gene delivery system.