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Basic investigation on radionuclide therapy with auger electron by using Br-77 labeled MBBG

Research Project

Project/Area Number 23791464
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionJapan Atomic Energy Agency

Principal Investigator

WATANABE Shigeki  独立行政法人日本原子力研究開発機構, 量子ビーム応用研究部門, 研究員 (10450305)

Co-Investigator(Renkei-kenkyūsha) HANAOKA Hirofumi  千葉大学, 大学院・薬学研究府, 助教 (50361390)
Project Period (FY) 2011 – 2012
Project Status Completed (Fiscal Year 2012)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2012: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords核医学(PET を含む) / Br-77 / オージェ電子 / 内用放射線治療 / 褐色細胞腫 / RI内用療法
Research Abstract

β-emitting radiopharmaceutical, I-131 labeled m-iodobenzylguanidine (I-131 MIBG) has been used for radionuclide therapy of malignant pheochromocytoma. Therapeutic effect of this approach is however less than expected. As auger electron possesses higher toxicity against tumor cells than β-emitting radionuclide therapy, we challenged to reveal efficacy of auger electron by using auger emitting radionuclide Br-77 labeled m-bromobenzylguanidne. First of all, we tried to prepare Br-77 labeled MBBG via boron-bromine exchange reaction which is expected to obtain enough amount of radioactivity to radionuclide therapy. Although desired boronate compound, 3-Pinacolateboryl-benzyl(N,N’,N’’-triBoc)guanidine, was synthesized, following radiobromination was not proceeded at all. We then successfully synthesized Br-77 labeled MBBG by iodine-bromine exchange reaction which is conventional route of MBBG synthesis. We conducted cellular uptake studies, and the results showed that MBBG was taken up into PC-12 cells at 3 hours after incubation. However, we don’t revealed localization of Br-77 MBBG in PC-12 cells.

Report

(3 results)
  • 2012 Annual Research Report   Final Research Report ( PDF )
  • 2011 Research-status Report
  • Research Products

    (6 results)

All 2013 2012 Other

All Presentation (6 results) (of which Invited: 3 results)

  • [Presentation] Recent Advances of Radio-bromine chemistry2013

    • Author(s)
      Shigeki Watanabe
    • Organizer
      20^<th> International Symposium on Radiopharmaceutical Science (ISRS2013)
    • Place of Presentation
      Jeju, Korea
    • Year and Date
      2013-05-12
    • Related Report
      2012 Final Research Report
  • [Presentation] 原子力機構における新規PET 核種の製造と標識薬剤の開発研究2013

    • Author(s)
      渡辺 茂樹
    • Organizer
      薬物動態・個体差要因可視化による個別化EBM の推進 学術講演会
    • Place of Presentation
      金沢大学
    • Year and Date
      2013-02-08
    • Related Report
      2012 Final Research Report
  • [Presentation] Synthesis and Biological Evaluations of Radiobrominated Compounds for Tumor Imaging2012

    • Author(s)
      Shigeki Watanabe
    • Organizer
      7^<th> International Symposium on Radiohalogens
    • Place of Presentation
      Whistler, BC, Canada
    • Year and Date
      2012-09-18
    • Related Report
      2012 Final Research Report
  • [Presentation] Synthesis of Biological Evaluations of Radiobrominated Compounds for Tumor Imaging

    • Author(s)
      渡辺 茂樹
    • Organizer
      7th International Symposium on Radiohalogen
    • Place of Presentation
      ウィスラーコンベンションセンター(カナダ、ウィスラー)
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] 原子力機構における新規PET核種の製造と標識薬剤の開発研究

    • Author(s)
      渡辺 茂樹
    • Organizer
      薬物動態・個体差要因可視化による個別化EBMの推進 学術講演会
    • Place of Presentation
      金沢大学(金沢市)
    • Related Report
      2012 Annual Research Report
    • Invited
  • [Presentation] Recent Advances of Radio-bromine Chemistry

    • Author(s)
      渡辺 茂樹
    • Organizer
      20th International Symposium on Radiopharmaceutical Science
    • Place of Presentation
      済州国際コンベンションセンター(韓国、済州)
    • Related Report
      2012 Annual Research Report
    • Invited

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Published: 2011-08-05   Modified: 2019-07-29  

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