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

2020 Fiscal Year Final Research Report

• 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
• 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

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.

Free Research Field

放射性医薬品化学

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。