Metabolic studies of astatine- and radioiodine-labeled neopentyl derivatives

Astatine-211 (211At) is one of the most promising radionuclides for targeted α therapy of cancers and radioiodine such as iodine-123 is useful radionuclide for diagnosis. Because astatine and iodine are the same group, halogen, the same scaffolds could be used for astatination and radioiodination to prepare radiotheranostics compounds. However, the in vivo instability of 211At-labeling agents such as 211At-benzoate limits the application of 211At to various compounds. To overcome the problem and expand the application of 211At-labeled compounds to radiotheranostics, we developed neopentyl derivatives as a novel scaffold for astatination and radioiodination. The stability and biodistribution of 211At or 125I-labeled neopentyl derivatives were compared with reference compounds radiolabeled with 125I or 211At via a conventional method using benzamide.
SNMMI2020 Annual Meeting