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Updated: Sep 13, 2025

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Recent advances in theranostics and oncology PET: emerging radionuclides and targets
Tadashi Watabe1,2, Kenji Hirata3, Mami Iima4
1Department of Radiology, Graduate School of Medicine, The University of Osaka, 2-2 Yamadaoka, Suita, Osaka, 565-0871, Japan. watabe.tadashi.med@osaka-u.ac.jp.
Abstract:
Theranostics, a novel integrated approach that combines cancer diagnosis and therapy by switching the radionuclide, has attracted growing attention. Various oncology PET probes other than FDG have been developed for the highly sensitive and precise detection of many types of cancer with the advancements in PET scanners, supporting the innovative development in theranostics. In therapeutic applications, radioligand therapy targeting somatostatin receptors (SSTR) and prostate-specific membrane antigen (PSMA) has already demonstrated significant clinical benefits. Terbium-161 (161Tb) has emerged as a new beta and Auger electron emitter, showing greater therapeutic efficacy compared to 177Lu. Alpha emitters, such as astatine (211At), are currently being evaluated in investigator-initiated clinical trials, with preliminary efficacy data reported for [211At]NaAt in patients with radioiodine-refractory thyroid cancer. Novel pan-tumor targeting agents, such as TROP-2, Nectin-4, LAT1, GPC-1, and EphA2, are also under development, and clinical translation of radioligand therapy is anticipated. These innovations in theranostics are expected to further broaden the scope of precision medicine in oncology.
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