Abstract: Receptor targeting therapy with radiolabeled peptides has become very important in oncology in the past few years. The most frequently used peptides in the clinic are analogs of somatostatin. Radiolabeled analogs of alpha-melanocyte-stimulating hormone, neurotensin, vasoactive intestinal peptide, bombesin, substance P, neuropeptide Y, gastrin and cholecystokinin are also being developed and evaluated in vitro and in vivo. This review focuses on the state of the art of the pre-clinical and clinical studies on ⁹⁰Y and ¹⁷⁷Lu radiolabeled somatostatin analogs for receptor-mediated radionuclide targeting therapy. Early clinical data of radiolabeled cholecystokinin and neuropeptide Y for internal radiopeptide therapy are also reviewed.