Development of At-211 labeled peptides for the targeted alpha therapy

• Project/Area Number: 26461872
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Institutes for Quantum and Radiological Science and Technology (2016); Japan Atomic Energy Agency (2014-2015)
• Principal Investigator: Watanabe Shigeki 国立研究開発法人量子科学技術研究開発機構, 高崎量子応用研究所 放射線生物応用研究部, 主幹研究員(定常) (10450305)
• Co-Investigator(Kenkyū-buntansha): 鷲山 幸信 金沢大学, 保健学系, 助教 (80313675)
• Co-Investigator(Renkei-kenkyūsha): Ohshima Yasuhiro 国立研究開発法人量子科学技術研究開発機構, 高崎量子応用研究所 放射線生物応用研究部, 主任研究員 (00588676)
• Research Collaborator: Sasaki Ichiro 国立研究開発法人量子科学技術研究開発機構, 高崎量子応用研究所 放射線生物応用研究部, 任期制技術員
• Project Period (FY): 2014-04-01 – 2017-03-31
• Project Status: Completed (Fiscal Year 2016)
• Budget Amount: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000); Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000); Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000); Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
• Keywords: At-211 / 内用放射線治療 / アルファ線 / ペプチド / アスタチン-211 / 湿式分離 / 標識実験 / ハロゲン―スズ交換反応 / アミノ酸 / ホウ素ケージ

Outline of Final Research Achievements

The use of alpha emitting radionuclides has been promising for development of targeted radionuclide therapy (TRT) because alpha particles give heavier damage to the cell by smaller dose than beta particles which has been employed for the TRT. In this study, we have successfully developed a novel isolation method of alpha emitting astatine-211 from an irradiated Bi target, and At-211 labeled peptides which have high affinity to HER2 overexpressing in some cancer cells such as breast cancer.

Research Products

• [Presentation] Isolation of At-211 using wet chemistry approach based on a column method (2017)
  • Author(s): Shigeki Watanabe
  • Organizer: 第３回核医学国際シンポジウム
  • Place of Presentation: 東京コンベンションホール（東京都中央区）
  • Year and Date: 2017-02-11
  • Int'l Joint Research / Invited
• [Presentation] Isolation of At-211 using an anion-exchange column method (2017)
  • Author(s): Shigeki Watanabe, Akihiko Shimada, Tetsuya Sakashita, Yasuhiro Ohshima, Noriko S. Ishioka
  • Organizer: 10th Synmpsium on Targeted Alpha Therapy
  • Place of Presentation: 石川県音楽堂（石川県金沢市）
  • Int'l Joint Research
• [Presentation] TIARAにおけるAt-211新規大量製造法の開発 (2016)
  • Author(s): 渡辺茂樹、渡辺智、島田明彦、石岡典子
  • Organizer: 第16回放射線プロセスシンポジウム
  • Place of Presentation: 東京大学（東京都文京区）
  • Year and Date: 2016-11-08
• [Presentation] Isolation of At-211 using a solid phase anion exchange method (2015)
  • Author(s): Sh. Watanabe, Sa. Watanabe, I. Sasaki, Y. Oｈshima, D.K. Hamlin, E.R. Balkin, M.K. Chyan, D.S. Wilbur, and N.S. Ishioka
  • Organizer: Pacifichem 2015
  • Place of Presentation: 米国ハワイ州ホノルル
  • Year and Date: 2015-12-16
  • Int'l Joint Research
• [Presentation] 乾式法および湿式法によるAt-211の分離 (2015)
  • Author(s): 渡辺茂樹・渡辺智・D.K.Hamlin, M.-K. Chyan, K. Gagnon, 鈴木博元, E.R. Balkin, 大島康宏, D.S.Wilbur, 石岡典子
  • Organizer: 第15回放射性医薬品・画像診断薬研究会
  • Place of Presentation: 京都勧業館 みやこメッセ（京都府京都市）
  • Year and Date: 2015-09-12
• [Presentation] 湿式分離法を用いたBiターゲットからのAt-211の分離 (2014)
  • Author(s): 渡辺 茂樹
  • Organizer: 第58回放射化学討論会
  • Place of Presentation: 愛知県名古屋市 名古屋大学
  • Year and Date: 2014-09-12
• [Presentation] Evaluation of Column Separation Methods for Simplification of the Wet Chemistry Approach to Isolation of At-211 (2014)
  • Author(s): Shigeki Watanabe
  • Organizer: 15th International Workshop on Targetry and Target Chemistry
  • Place of Presentation: チェコ共和国プラハ Hotel Diplomat
  • Year and Date: 2014-08-21