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Comparison of nuclear medicine therapeutics targeting PSMA among alpha-emitting nuclides

Kaneda-Nakashima, Kazuko*; Shirakami, Yoshifumi*; Kadonaga, Yuichiro*; Watabe, Tadashi*; Oe, Kazuhiro*; Yin, X.*; Haba, Hiromitsu*; Shirasaki, Kenji*; Kikunaga, Hidetoshi*; Tsukada, Kazuaki  ; Toyoshima, Atsushi*; Cardinale, J.*; Giesel, F. L.*; Fukase, Koichi*

Currently, targeted alpha therapy (TAT) is a new therapy involving the administration of a therapeutic drug that combines a substance of $$alpha$$-emitting nuclides that kill cancer cells and a drug that selectively accumulates in cancer cells. We labeled the compounds targeting prostate specific membrane antigen (PSMA) with $$^{211}$$At and $$^{225}$$Ac. PSMA is a molecule that has attracted attention as a theranostic target for prostate cancer, and several targeted radioligands have already shown therapeutic effects in patients. The results showed that $$^{211}$$At, which has a much shorter half-life, is no less cytotoxic than $$^{225}$$Ac. In $$^{211}$$At labeling, our group has also developed an original method (Shirakami Reaction). We have succeeded in obtaining a highly purified labeled product in a short timeframe using this method.

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Category:Biochemistry & Molecular Biology

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