Site-Directed Radiopeptides: Design and Applications in Medicine

Dear Colleagues,

The increasing importance of target-specific radiopetides in the clinical arena is demonstrated by the approval of the first β-emitting radiopharmaceutical for peptide receptor radionuclide therapy, lutetium-177 oxodotreotide (Lutathera^®), by the European Medicines Agency (2017) and U.S. Food and Drug Administration (2018) for the treatment of somatostatin receptor (SSTR)-positive gastroenteropancreatic neuroendocrine tumors. This recent accomplishment and the two-decade success story of the indium-111 pentetreotide (OctreoScan^®) radiotracer in the scintigraphic localization of SSTR-positive primary and metastatic neuroendocrine tumors continuously inspire scientists working in this area.

The design of novel site-directed radiopeptides, to address unmet needs in precision medicine, is currently being fueled by i) the identification of novel biomarkers of cancer; ii) the introduction of innovative chemical strategies to develop “smart drugs” (e.g., innovative bioconjugation techniques); iii) the availability of “new” generator-produced radionuclides (e.g., gallium-68 for PET imaging or bismuth-213 for ɑ therapy); iv) the emergence of new radionuclides for molecular imaging (e.g., copper-64 or terbium-152) or radionuclide therapy (e.g., lead-212 or actinium-211), and v) the increasing importance of theranostic approaches in clinical practice. This Special Issue of Molecules welcomes original research articles, communications, and review articles dealing with major breakthroughs and challenges that are still to be addressed in the design of target-specific radiopeptides for disease theranostics. Considering the multidisciplinary nature of this research area, contributions from frontier subjects are welcome. When relevant from a (radio)chemical point of view, manuscripts partially addressing translational or regulatory issues might also be considered for publication.

As an active researcher in the field, we would be delighted if you would be willing to contribute to this Special Issue.

We hope that you can contribute and look forward to hearing from you in the near future.

Dr. João D. G. Correia
Dr. Theodosia Maina
Guest Editors

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