2021 Fiscal Year Final Research Report

PD-ECGF targeted tumor treatment with new At-211 radiolabeled uracil derivatives

Research Project

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Project/Area Number	19K08180
Research Category	Grant-in-Aid for Scientific Research (C)
Allocation Type	Multi-year Fund
Section	一般
Review Section	Basic Section 52040:Radiological sciences-related
Research Institution	Fukushima Medical University
Principal Investigator	NISHIJIMA Ken-ichi 福島県立医科大学, 公私立大学の部局等, 講師 (60364254)
Co-Investigator(Kenkyū-buntansha)	東川桂北海道大学, アイソトープ総合センター, 助教 (10756878) 粟生木美穂福島県立医科大学, 公私立大学の部局等, 助手 (10783227) 久下裕司北海道大学, アイソトープ総合センター, 教授 (70321958) 趙松吉福島県立医科大学, 公私立大学の部局等, 教授 (80374239)
Project Period (FY)	2019-04-01 – 2022-03-31
Keywords	核医学治療 / チミジンホスホリラーゼ
Outline of Final Research Achievements	Platelet-derived endothelial cell growth factor (PD-ECGF) is expressed at higher levels in a variety of solid tumors than in normal tissue. The aim of this study was to develop therapeutic radiopharmaceuticals based on a newly developed 5-haloylmidazolyluracil derivative targeting PD-ECGF using At-211, an alpha-ray emitting radionuclide. We succeeded for the first time in obtaining the target At-211-labeled imidazolyluracil derivative by mixing At-211 produced by a cyclotron with an oxidant and a labeling precursor under basic conditions and reacting the mixture at 50°C or room temperature. In the future, we plan to conduct cellular and animal experiments to fundamentally evaluate the usefulness of the product as a therapeutic radiopharmaceutical. The results of this study provide important insights into the development of novel radiopharmaceuticals using At-211, an alpha-ray emitting radionuclide.
Free Research Field	放射性薬剤
Academic Significance and Societal Importance of the Research Achievements	固形腫瘍において高レベルで発現するPD-ECGFを標的としたα線放出核種At-211を用いた治療用放射性薬剤の開発を行い、At-211標識化合物を得ることに初めて成功した。今後、細胞および動物実験による有用性の評価を基礎的に検討することにより、新しい治療法の開発に寄与するものと考える。