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Development of a new radioisotope-labeled peptide with accomplished low nephrotoxicity and effectiveness in cancer therapy

Research Project

Project/Area Number 24791329
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Radiation science
Research InstitutionHealth Sciences University of Hokkaido

Principal Investigator

OSHIMA Nobuhiro  北海道医療大学, 薬学部, 助教 (80508648)

Project Period (FY) 2012-04-01 – 2015-03-31
Project Status Completed (Fiscal Year 2014)
Budget Amount *help
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Keywordsがん / アイソトープ内用療法 / オクトレオチド / 薬物体内動態制御 / 放射性医薬品 / 腎臓 / ペプチド / インジウム-111 / 体内動態制御 / 負電荷導入 / 薬物動態制御 / 副作用低減
Outline of Final Research Achievements

Radioisotope (RI)-labeled peptides have been studied as agents for cancer radiotherapy. However, their clinical application is difficult because of the high accumulation in the kidney, which results in unnecessary radiation exposure. Our previous study revealed that introducing negative charge into RI-labeled peptide could reduce the accumulation of renal radioactivity. In addition, to maintain the residence time of peptide in tumor cells, it is important to introduce negative charge into a suitable position on the molecule. The present study aimed to develop RI-labeled peptides both reducing radioactivity levels in kidney and maintaining the accumulation in tumor by the introduction of negative charge. As a result, I synthesized a new RI-labeled peptide derivative, achieving not only the reduction of renal radioactivity but also augmented tumor radioactivity. An application for radiotherapy using this RI-labeled peptide will be evaluated in tumor-bearing animals in the near future.

Report

(4 results)
  • 2014 Annual Research Report   Final Research Report ( PDF )
  • 2013 Research-status Report
  • 2012 Research-status Report
  • Research Products

    (6 results)

All 2015 2014 2013 Other

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (4 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] Design, synthesis and biological evaluation of negatively charged 111In-DTPA-octreotide derivatives2014

    • Author(s)
      Oshima N, Akizawa H, Zhao S, Nishijima K, Kitamura Y, Arano Y, Kuge Y, Ohkura K
    • Journal Title

      Bioorgan Med Chem

      Volume: 22 Issue: 4 Pages: 1377-1382

    • DOI

      10.1016/j.bmc.2013.12.063

    • Related Report
      2013 Research-status Report
    • Peer Reviewed
  • [Presentation] [111In-DTPA-D-Phe-1-Asp0-D-Phe1]-オクトレオチドの体内動態評価: 放射能の腎集積性 低減と腫瘍集積性の向上2015

    • Author(s)
      大島 伸宏, 秋澤 宏行, 河嶋 秀和, 趙 松吉, 趙 芫, 西嶋 剣一, 北村 陽二, 荒野 泰, 久下 裕司, 大倉 一枝
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      神戸学院大学
    • Year and Date
      2015-03-25 – 2015-03-28
    • Related Report
      2014 Annual Research Report
  • [Presentation] テガフールとメトキシナフタレンとの光反応による新規付加体の生成2014

    • Author(s)
      大倉一枝、秋澤宏行、菅生辰之、大島伸宏、関興一
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 90Y標識のための2-(p-aminobenzyl)-6-methyl-DTPA-結合オクトレオチド誘導体の合成2013

    • Author(s)
      大島伸宏、秋澤宏行、大倉一枝
    • Organizer
      日本薬学会 第133年会
    • Place of Presentation
      パシフィコ横浜
    • Related Report
      2012 Research-status Report
  • [Presentation] アスパラギン酸で負電荷を導入した111In-DTPA-D-Phe1-オクトレオチド誘導体の in vitro 腫瘍集積性および体内動態の評価

    • Author(s)
      大島伸宏、秋澤宏行、趙松吉、趙芫、西嶋剣一、北村陽二、荒野泰、久下裕司、大倉一枝
    • Organizer
      日本薬学会北海道支部 139回例会
    • Place of Presentation
      北海道大学学術交流会館
    • Related Report
      2012 Research-status Report
  • [Patent(Industrial Property Rights)] オクトレオチド類似体及びそれを用いた放射性画像診断剤2013

    • Inventor(s)
      大島伸宏、秋澤宏行、大倉一枝、他4名
    • Industrial Property Rights Holder
      大島伸宏、秋澤宏行、大倉一枝、他4名
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2013-194032
    • Filing Date
      2013-09-19
    • Related Report
      2013 Research-status Report

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Published: 2013-05-31   Modified: 2019-07-29  

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