[68Ga]NS3-RGD and [68Ga] Oxo-DO3A-RGD for imaging αvβ3 integrin expression: synthesis, evaluation, and comparison

[68Ga]Oxo-DO3A-RGD and [68Ga]NS3-RGD have inferior characteristics compared to already existing 68Ga-labeled RGD peptides and thus, both are not suited to image αvβ3 integrin expression. Of all our tested RGD peptides, [68Ga]NODAGA-RGD still possesses the most favorable imaging properties. Moreover this study shows that the use of appropriate chelators to achieve good targeting properties of 68Ga-labeled biomolecules and careful in vitro and in vivo evaluation including comparative studies of different strategies are essential components in designing an effective imaging agent for PET.