Dispersion of Alpha-Nuclides during Animal Experiments

Kaneda-Nakashima, Kazuko; Zhang, Zijian; Nagata, Koji; Shirasaki, Kenji; Kikunaga, H.; Yamamura, Tomoo; Ooe, Kazuhiro; Watabe, Tadashi; Toyoshima, Atsushi; Yoshimura, Takashi; Shinohara, Atsushi

doi:10.12950/rsm.210519

Cited by 2 publications

(2 citation statements)

References 15 publications

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“…In addition, side effects can occur when the labeled nuclide is released from the compound. This is because 211 At behaves in a similar fashion to iodine and 225 Ac accumulates in the bones and liver [31]. Consideration is also required in order to ensure safety.…”

Section: Discussionmentioning

confidence: 99%

“…The intensity of the nuclides were measured using a germanium semiconductor detector (BE2020, Canberra, Mirion Technologies, Inc., Atlanta, GA. USA) and a γ-counter (Wizard 2 2480, PerkinElmer, Inc., Shelton, CT, USA). The samples treated with 225 Ac were maintained until radiative equilibrium was reached before the measurements were taken, according to a previous study [31]. The PSMA-selected chemicals were labeled with each nuclide using previously reported procedures.…”

Section: Methodsmentioning

confidence: 99%

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Comparison of Nuclear Medicine Therapeutics Targeting PSMA among Alpha-Emitting Nuclides

Kaneda-Nakashima,

Shirakami,

Kadonaga

et al. 2024

IJMS

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Currently, targeted alpha therapy (TAT) is a new therapy involving the administration of a therapeutic drug that combines a substance of α-emitting nuclides that kill cancer cells and a drug that selectively accumulates in cancer cells. It is known to be effective against cancers that are difficult to treat with existing methods, such as cancer cells that are widely spread throughout the whole body, and there are high expectations for its early clinical implementation. The nuclides for TAT, including 149Tb, 211At, 212/213Bi, 212Pb (for 212Bi), 223Ra, 225Ac, 226/227Th, and 230U, are known. However, some nuclides encounter problems with labeling methods and lack sufficient preclinical and clinical data. We labeled the compounds targeting prostate specific membrane antigen (PSMA) with 211At and 225Ac. 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 211At, which has a much shorter half-life, is no less cytotoxic than 225Ac. In 211At 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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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Comparison of Nuclear Medicine Therapeutics Targeting PSMA among Alpha-Emitting Nuclides

Kaneda-Nakashima,

Shirakami,

Kadonaga

et al. 2024

IJMS

Self Cite

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Development of LAT1-Selective Nuclear Medicine Therapeutics Using Astatine-211

Kaneda-Nakashima,

Shirakami,

Hisada

et al. 2024

IJMS

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We investigated nuclear medicine therapeutics targeting the L-type amino acid transporter 1 (LAT1). We previously reported that a nuclear medicine therapeutic drug using astatine 211 (211At), an alpha-emitting nuclide that can be produced in an accelerator and targets LAT1 as a molecular target, is effective. The seed compound was 3-[211At] Astato-α-methyl-L-tyrosine (211At-AAMT-OH-L). We used a unique labeling method. By changing the OH group of phenol to a methyl group, retention was successfully increased. It was also found that the amount of the L-isomer taken up by the D-isomer and L-isomer was clearly higher, and the L-isomer was superior as a therapeutic drug. Compounds in which the methyl group was replaced with an ethyl or propyl group were also examined, but their retention did not increase significantly. In fact, we observed increased non-specific accumulation and dynamics, suggesting that labeling may be off. In addition, 211At-AAMT-O-Me-L, which has a simple structure, was clearly superior in terms of uptake speed for several candidate compounds. As a result, we were able to develop a compound that can be easily labeled, has high specific radioactivity, is stable, and has a strong therapeutic effect.

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Dispersion of Alpha-Nuclides during Animal Experiments

Cited by 2 publications

References 15 publications

Comparison of Nuclear Medicine Therapeutics Targeting PSMA among Alpha-Emitting Nuclides

Comparison of Nuclear Medicine Therapeutics Targeting PSMA among Alpha-Emitting Nuclides

Development of LAT1-Selective Nuclear Medicine Therapeutics Using Astatine-211

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