Pretargeting system for targeted alpha therapy using 211At

2018 Fiscal Year Final Research Report

• Project/Area Number: 17K16426
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: Chiba University
• Principal Investigator: Suzuki Hiroyuki 千葉大学, 大学院薬学研究院, 助教 (00707648)
• Research Collaborator: Watanabe Shigeki
• Project Period (FY): 2017-04-01 – 2019-03-31
• Keywords: 標的α線治療 / アスタチン-211 / プレターゲティング / 放射性ヨウ素 / テトラジン / ネオペンチル / ヨウ素-125

Outline of Final Research Achievements

211At is an alpha-emitting radionuclide appropriate for medical use. To expand the application of 211At-labeled compounds to targeted alpha therapy, we developed neopentyl derivatives as a novel scaffold for astatination. The model neopentyl derivative radiolabeled with 211At was stable both in vitro and in vivo. The results showed that the neopentyl derivatives would serve as a useful scaffold to develop 211At-labeled compounds. Thus, we designed a tetrazine derivative including neopentyl astatide structure. In the preliminary study using 125I, the tetrazine derivative showed biodistribution appropriate for pretargeting system. These findings indicate that the novel tetrazine derivative would be useful for pretargeting system using 211At.

Free Research Field

放射性医薬品

Academic Significance and Societal Importance of the Research Achievements

現在α線治療の有用性が世界的にも認知され、骨転移以外の癌へのα線治療の応用が強く望まれている。本研究は、211Atによるα線治療に有用な戦略の一つであるプレターゲティングの実現への貢献が期待される。プレターゲティング法は多様な抗体に対して使用可能な基盤技術であり、本研究成果は様々な癌治療につながることが期待できる。