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論文

Complexation of lutetium-177 with bifunctional chelators in the presence of Mg, Cu, and Yb

渡辺 智; 橋本 和幸; 石岡 典子

JAEA-Review 2014-050, JAEA Takasaki Annual Report 2013, P. 102, 2015/03

As part of basic studies for the production of $$^{177}$$Lu capable of labeling of $$^{177}$$Lu-1,4,7,10-tetraazacyclododecan-N,N',N'',N'''-tetraacetic acid (DOTA)-antibody, $$^{177}$$Lu complexation of DOTA and diethylenetriamine-N,N,N',N'',N''-pentaacetic acid (DTPA) was investigated in the presence of competing metals: Mg, Cu, and Yb in addition to Ca, Fe, and Zn. The inhibition of $$^{177}$$Lu complexation by the competing metals was in the order of Mg, Ca $$<$$ Fe $$<$$ Yb $$<$$ Cu, Zn and Mg, Ca $$<$$ Zn $$<$$ Fe $$<$$ Cu $$<$$ Yb with DOTA and DTPA, respectively. Consequently, the elimination of Mg and Ca from the $$^{177}$$Lu final solution produced was not found to be necessary, while the elimination of Cu, Fe, Zn and Yb from the $$^{177}$$Lu final solution was found to be necessary. On the basis of the knowledge obtained, the method of elimination of the competing metals will be developed.

論文

Production of highly purified no-carrier-added $$^{177}$$Lu for radioimmunotherapy

渡辺 智; 橋本 和幸; 渡辺 茂樹; 飯田 靖彦*; 花岡 宏史*; 遠藤 啓吾*; 石岡 典子

Journal of Radioanalytical and Nuclear Chemistry, 303(1), p.935 - 940, 2015/01

 被引用回数:16 パーセンタイル:75.78(Chemistry, Analytical)

No-carrier-added $$^{177}$$Lu produced via the $$^{176}$$Yb(n, $$gamma$$) $$^{177}$$Yb $$rightarrow$$$$^{177}$$Lu process was separated from the macroscopic amounts of the Yb target using reversed-phase ion-pair liquid chromatography. To produce a highly purified $$^{177}$$Lu solution capable of labeling antibodies, the metallic impurities were removed using cation, chelating ion, and anion exchange columns. After the elimination of metallic impurities, the concentrations of Ca, Fe, and Zn were reduced from 87, 340, and 77 ppb to 13, 18, and 9 ppb, respectively. Consequently, the labeling yield of the $$^{177}$$Lu -labeled antibody increased from less than 5% to 88%.

口頭

JRR-3を用いたLu-177製造に関する生成量評価

藤野 隼輔; 橋本 和幸; 佐伯 秀也*; 河内 幸正*; 川端 方子*; 千葉 悠介

no journal, , 

Lu-177は神経内分泌腫瘍の治療薬として、ルタテラが国内承認されており、さらなる治療薬開発が期待されている核種の1つである。しかし、Lu-177は海外からの輸入に依存しており、輸送トラブル等により国内流通及び薬剤開発等に影響を及ぼすことが懸念される。そのため、原子力機構でLu-177の一部を国内で製造可能かどうかを確認するため、JRR-3を用いたLu-177の生成量評価を実施した。

口頭

金属元素存在下における$$^{177}$$Luと二官能性キレート剤との錯形成

渡辺 智; 橋本 和幸; 石岡 典子

no journal, , 

$$^{177}$$Lu-1,4,7,10-tetraazacyclododecan-N,N',N'',N'''-tetraacetic acid(DOTA)-抗体の標識が可能な$$^{177}$$Luの製造研究の一環として、Ca, Fe, Znに加えてMg, Cu, Yb存在下での$$^{177}$$LuとDOTA及びdiethylenetriamine- N,N,N',N'',N''-pentaacetic acid (DTPA)との錯形成時の阻害について検討した。競合金属による$$^{177}$$Luの錯形成阻害の強さは、DOTA及びDTPAにおいて、それぞれMg, Ca $$<$$ Fe $$<$$ Yb $$<$$ Cu, Zn及びMg, Ca $$<$$ Zn $$<$$ Fe $$<$$ Cu $$<$$ Ybの順序であった。以上の結果から、製造した$$^{177}$$Lu最終溶液中のMg及びCaは除去する必要はないが、Cu, Fe, Zn及びYbは除去する必要があることが判明し、競合金属の除去方法の開発のための有用な知見を得ることができた。

口頭

The Current status and challenge for radioisotopes production by JRR-3

藤野 隼輔; 千葉 悠介

no journal, , 

In the past, JAEA used to manufacture radioisotopes for medicine and industry, but our radioisotope manufacturing projects has been downsized considering the decrease in the number of operating research reactors and the shutdown of reactors. Due to the reduction of radioisotope production, most of the radioisotopes used in Japan are dependent on imports from overseas, and there is concern that supply disruptions caused by external factors may hinder the use of radioisotopes. In particular, the production and stable supply of medical radioisotopes in Japan has become an issue due to the recent international situation and transportation troubles. Therefore, the Atomic Energy Commission formulated the "Action Plan for the Production and Utilization of Radioisotopes for Medical Use" on May 31, 2022. One of the goals of this action plan is to produce and supply approximately 30% of the domestic demand for Mo-99 using JRR-3. In addition to the above, the production for sealed radioactive sources in medical and industrial use has been restarted since the resumption of JRR-3 operation at 2021. And the production of Lu-177 has been developed in progress.

口頭

Production of Lu-177 Using JRR-3 and PWR

渡辺 杏*; 藤野 隼輔; 高木 直行*

no journal, , 

Targeted Radionuclide Therapy using Lu-177 is mainly used to treat prostate cancer and is attracting attention as a new treatment method that can also treat transition cancer cells. Although Lu-177 is being produced by research reactor around the world, Lu-177 production has not yet taken place in Japan. There are two ways to produce Lu-177 in reactors: direct production by the Lu-176(n,$$gamma$$) reaction and indirect production by the Yb-176(n,$$gamma$$ $$beta$$$$^{-}$$) reaction. The former method of enriched Lu-176 yields a large amount of Lu-177, but the specific activity is as small as about 0.5 TBq/mg-Lu at the neutron flux level of commercial light water reactors. On the other hand, the indirect method using enriched Yb-176 yields less Lu-177 than direct production, but it has a high specific activity of about 4 TBq/mg-Lu and enables the production of no carrier added (nca) Lu-177 without the waste problem of Lu-177m (half-life: 160 days). The objective of this study is to produce Lu-177 using a nuclear reactor, with the goal of supplying 15,000 castration-resistant prostate cancer patients in Japan. To achieve mass production in commercial light water reactors in the future, we first conducted experiments and analysis on JRR-3.

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