BNCT as Theranostics, development of boron-containing drugs for diagnostics and therapy

• Project/Area Number: 18K07624
• 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: University of Tsukuba
• Principal Investigator: Hatano Kentaro 筑波大学, 医学医療系, 准教授 (50228475)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Project Status: Completed (Fiscal Year 2020)
• Budget Amount: ¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000); Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000); Fiscal Year 2019: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000); Fiscal Year 2018: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
• Keywords: 中性子補足療法 / BNCT / PET / 腫瘍選択的ペプチド / フッ素-18 / 放射線治療 / 中性子捕捉療法

Outline of Final Research Achievements

(1)Production of 18F-F2 was optimized and synthesis of o-carborane using the reagent was examined. 18F-o-Carborane was obtained in 21% radiochemical yield. (2)According to peptide formation using 125I-DABI reaction of peptide and phenyl isothiocyanate was examined as model reaction. As DABI was obtained by oxidative iodination, similar preparation will be possible using 18F-F2 shown above. (3)BSH was successfully labeled with 18F-FBAM which indicates possibility of construction of BNCT-PET reagent using multi functional cross linking reagents.

Academic Significance and Societal Importance of the Research Achievements

本研究よりポジトロン標識ＢＮＣＴ製剤のドラッグデザインについていくつかの可能性を指し示すことが出来た。得られた化合物を用い、ＰＥＴによる生体内動態の最適化を通じ、ＢＮＣＴ製剤の開発を加速することができ、さらにその適用を判断するコンパニオン診断が実現されると考える。様々な生理活性ペプチドをＢＮＣＴ製剤デザインに持ち込むことで、この治療法の適用拡大が期待される。

Research Products

• [Journal Article] Peripheral benzodiazepine receptor/18?kDa translocator protein positron emission tomography imaging in a rat model of acute brain injury (2020)
  • Author(s): Nomura Masahiko、Toyama Hiroshi、Suzuki Hiromi、Yamada Takashi、Hatano Kentaro、Wilson Alan A.、Ito Kengo、Sawada Makoto
  • Journal Title: Annals of Nuclear Medicine Volume: 35 Issue: 1 Pages: 8-16
  • DOI: 10.1007/s12149-020-01530-2
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] Biomolecule‐Assisted Synthesis of Hierarchical Multilayered Boehmite and Alumina Nanosheets for Enhanced Molybdenum Adsorption (2019)
  • Author(s): Saptiama Indra、Kaneti Yusuf Valentino、Yuliarto Brian、Kumada Hiroaki、Tsuchiya Kunihiko、Fujita Yoshitaka、Malgras Victor、Fukumitsu Nobuyoshi、Sakae Takeji、Hatano Kentaro、Ariga Katsuhiko、Sugahara Yoshiyuki、Yamauchi Yusuke
  • Journal Title: Chemistry A European Journal Volume: 25 Issue: 18 Pages: 4843-4855
  • DOI: 10.1002/chem.201900177
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Journal Article] メソポーラス加工を応用した新規アルミナ吸着剤の開発 (2018)
  • Author(s): 福光 延吉; 山内悠輔; Saptiama, I; 有賀 克彦; 籏野 健太郎; 熊田 博明; 藤田 善貴; 土谷 邦彦
  • Journal Title: Isotope News Volume: 760 Pages: 15-18
• [Journal Article] Potential use of prostate specific membrane antigen (PSMA) for detecting the tumor neovasculature of brain tumors by PET imaging with 89Zr-Df-IAB2M anti-PSMA minibody (2018)
  • Author(s): Matsuda Masahide、Ishikawa Eiichi、Yamamoto Tetsuya、Hatano Kentaro、Joraku Akira、Iizumi Yuichi、Masuda Yosuke、Nishiyama Hiroyuki、Matsumura Akira
  • Journal Title: Journal of Neuro-Oncology Volume: in print Issue: 3 Pages: 581-589
  • DOI: 10.1007/s11060-018-2825-5
  • Peer Reviewed
• [Presentation] Zr-89 標識PSMA minibody PETによる前立腺がん等のイメージング (2020)
  • Author(s): 籏野健太郎
  • Organizer: PETサマーセミナー2019 in 福島
  • Invited
• [Book] 新核医学技術総論 技術編 (2020)
  • Author(s): 日本核医学技術学会編集委員会
  • Total Pages: 386
  • Publisher: 山代印刷株式会社出版部
  • ISBN: 9784991020124
• [Book] 小動物用PET、SPECTによる分子イメージング研究ガイド (2020)
  • Author(s): 西弘大、 籏野健太郎、 間賀田泰寛、 渡部浩司、 津國浩之
  • Total Pages: 24
  • Publisher: 公益社団法人日本アイソトープ協会