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Preparation and evaluation of $$^{186/188}$$Re-labeled antibody (A7) for radioimmunotherapy with rhenium(I) tricarbonyl core as a chelate site

Ogawa, Kazuma*; Kawashima, Hidekazu*; Kinuya, Seigo*; Shiba, Kazuhiro*; Onoguchi, Masahisa*; Kimura, Hiroyuki*; Hashimoto, Kazuyuki; Odani, Akira*; Saji, Hideo*

Rhenium is one of the most valuable elements for internal radiotherapy because $$^{186/188}$$Re have favorable physical characteristics. However, there are problems when proteins such as antibodies are used as carriers of $$^{186/188}$$Re. Labeling methods require the complicated processes. Therefore, we planned the preparation by a simple method and evaluation of a stable $$^{186/188}$$Re-labeled antibody. For this purpose, we selected $$^{186/188}$$Re(I) tricarbonyl complex as a chelating site. A7 was used as a model protein. $$^{186/188}$$Re-labeled A7 was prepared by directly reacting a $$^{186/188}$$Re(I) tricarbonyl precursor with A7. $$^{186/188}$$Re-(CO)$$_{3}$$-A7 were prepared with radiochemical yields of 23-28%. After purification, $$^{186/188}$$Re-(CO)$$_{3}$$-A7 showed a radiochemical purity of over 95%. In biodistribution experiments, $$^{186/188}$$Re-labeled A7 showed high uptakes in the tumor.

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Category:Radiology, Nuclear Medicine & Medical Imaging

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