Tumor targeting with 99mTc radiolabeled peptides: Clinical application and recent development

Abstract Targeting overexpressed receptors on the cancer cells with radiolabeled peptides has become very important in nuclear oncology in the recent years. Peptides are small and have easy preparation and easy radiolabeling protocol with no side‐effect and toxicity. These properties made them a valuable tool for tumor targeting. Based on the successful imaging of neuroendocrine tumors with 111 In‐octreotide, other receptor‐targeting peptides such as bombesin ( BBN ), cholecystokinin/gastrin analogues, neurotensin analogues, glucagon‐like peptide‐1, and RGD peptides are currently under development or undergoing clinical trials. The most frequently used radionuclides for tumor imaging are 99m Tc and 111 In for single‐photon emission computed tomography and 68 Ga and 18 F for positron emission tomography imaging. This review presents some of the 99m Tc‐labeled peptides, with regard to their potential for radionuclide imaging of tumors in clinical and preclinical application.