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Precise evaluation and optimization of the THK probe for tau imaging

Research Project

Project/Area Number 25293259
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypePartial Multi-year Fund
Section一般
Research Field Radiation science
Research InstitutionTohoku University

Principal Investigator

FURUMOTO SHOZO  東北大学, サイクロトロン・ラジオアイソトープセンター, 教授 (00375198)

Co-Investigator(Renkei-kenkyūsha) OKAMURA Nobuyuki  東北大学, 大学院医学系研究科, 准教授 (40361076)
SHIDAHARA Miho  東北大学, 大学院医学系研究科, 講師 (20443070)
Project Period (FY) 2013-04-01 – 2016-03-31
Project Status Completed (Fiscal Year 2015)
Budget Amount *help
¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Fiscal Year 2015: ¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2014: ¥6,110,000 (Direct Cost: ¥4,700,000、Indirect Cost: ¥1,410,000)
Fiscal Year 2013: ¥8,060,000 (Direct Cost: ¥6,200,000、Indirect Cost: ¥1,860,000)
Keywordsタウ / PET / イメージング / 18F
Outline of Final Research Achievements

Alzheimer's disease (AD) is the most common form of dementia in the elderly. Abnormal deposition of phosphorylated tau is one of the key pathological changes in the AD brain. The purpose of this study is to optimize the chemical structure of THK tau PET probes that have been developed by us for imaging tau pathology in the AD brain with PET. One modification of the probe structure was replacement of the benzene ring to pyridinyl one. Another change was conformational optimization of the fluoropropanol side chain. S-enantiomer of the pyridinyl derivative showed better brain pharmacokinetics in normal mice. The optimized derivative indicated lower non-specific binding to white matter of the AD brain tissue samples. Clinical PET study using the optimized probe demonstrated that higher radioactivity uptakes were observed in the parahippocampal gyrus and inferior temporal gyrus. These results suggest the potential utility of the optimized THK tau probe.

Report

(4 results)
  • 2015 Annual Research Report   Final Research Report ( PDF )
  • 2014 Annual Research Report
  • 2013 Annual Research Report
  • Research Products

    (21 results)

All 2016 2015 2014 2013

All Journal Article (8 results) (of which Peer Reviewed: 7 results,  Acknowledgement Compliant: 1 results,  Open Access: 1 results) Presentation (13 results) (of which Int'l Joint Research: 1 results,  Invited: 1 results)

  • [Journal Article] Structure-Activity Relationship of 2-Arylquinolines as PET Imaging Tracers for Tau Pathology in Alzheimer’s Disease2016

    • Author(s)
      Tetsuro Tago, Shozo Furumoto, Nobuyuki Okamura, Ryuichi Harada, Hajime Adachi, Yoichi Ishikawa, Kazuhiko Yanai, Ren Iwata, and Yukitsuka Kudo
    • Journal Title

      Journal of Nuclear Medicine

      Volume: 57(4) Issue: 4 Pages: 608-614

    • DOI

      10.2967/jnumed.115.166652

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] 18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease2016

    • Author(s)
      Harada R, Okamura N, Furumoto S, Furukawa K, Ishiki A, Tomita N, Tago T, Hiraoka K, Watanuki S, Shidahara M, Miyake M, Ishikawa Y, Matsuda R, Inami A, Yoshikawa T, Funaki Y, Iwata R, Tashiro M, Yanai K, Arai H, Kudo Y
    • Journal Title

      J Nucl Med

      Volume: 57 Issue: 2 Pages: 208-214

    • DOI

      10.2967/jnumed.115.164848

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Preclinical evaluation of [18F]THK-5015 enantiomers: effects of chirality on its effectiveness as a tau imaging radiotracer.2015

    • Author(s)
      Tago T., Furumoto S., Okamura N., Harada R., Adachi H., Ishikawa Y., Yanai K., Iwata R., Kudo Y.
    • Journal Title

      Mol. Imaging Biol.

      Volume: 未定 Issue: 2 Pages: 258-266

    • DOI

      10.1007/s11307-015-0879-8

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] タウプローブ開発の最先端2014

    • Author(s)
      古本 祥三, 岡村 信行, 原田 龍一, 多胡 哲朗, 工藤 幸司
    • Journal Title

      JSMI Report

      Volume: 8 Pages: 3-7

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed
  • [Journal Article] 18F標識PETプローブの現状と展望2014

    • Author(s)
      古本祥三
    • Journal Title

      INNERVISION

      Volume: 29 Pages: 11-14

    • Related Report
      2014 Annual Research Report
  • [Journal Article] Non-invasive assessment of Alzheimer's disease neurofibrillary pathology using 18F-THK5105 PET.2014

    • Author(s)
      Nobuyuki Okamura, Shozo Furumoto, Michelle T. Fodero-Tavoletti, Rachel S. Mulligan, Ryuichi Harada, Paul Yates, Svetlana Pejoska, Yukitsuka Kudo, Colin L. Masters, Kazuhiko Yanai, Christopher C. Rowe, Victor L. Villemagne
    • Journal Title

      Brain

      Volume: 137 Pages: 1762-1771

    • Related Report
      2014 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] In vivo evaluation of a novel tau imaging tracer for Alzheimer's disease2014

    • Author(s)
      Villemagne L. Victor, Shozo Furumoto, Michelle T. Fodero-Tavoletti, Rachel S. Mulligan, John Hodges, Ryuichi Harada, Paul Yates, Oliver Piguet, Svetlana Pejoska, Vincent Doré, Kazuhiko Yanai, Colin L. Masters, Yukitsuka Kudo, Christopher C. Rowe, Nobuyuki Okamura.
    • Journal Title

      European Journal of Nuclear Medicine and Molecular Imaging

      Volume: 41 Issue: 5 Pages: 816-826

    • DOI

      10.1007/s00259-013-2681-7

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Non-invasive assessment of Alzheimer's disease neurofibrillary pathology using 18F-THK5105 PET.2014

    • Author(s)
      Okamura N, Furumoto S, Fodero-Tavoletti MT, Mulligan RS, Harada R, Yates P, Pejoska S, Kudo Y, Masters CL, Yanai K, Rowe CC, Villemagne VL.
    • Journal Title

      Brain

      Volume: 印刷中

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed
  • [Presentation] PETによるアルツハイマー病タウイメージングのための2-アリールキノリン誘導体開発2015

    • Author(s)
      多胡哲郎,古本祥三,岡村信行,原田龍一,安立創,石川洋一,谷内一彦,工藤幸司,岩田錬
    • Organizer
      第 55 回日本核医学会学術総会
    • Place of Presentation
      東京
    • Year and Date
      2015-11-05
    • Related Report
      2015 Annual Research Report
  • [Presentation] タウイメージングトレーサー[18F]THK-5351 の代謝解析2015

    • Author(s)
      原田龍一,岡村信行,古本祥三,多胡哲郎,岩田錬,谷内一彦,工藤幸司
    • Organizer
      第 55 回日本核医学会学術総会
    • Place of Presentation
      東京
    • Year and Date
      2015-11-05
    • Related Report
      2015 Annual Research Report
  • [Presentation] PETプローブの創製研究 ~分子設計から橋渡し研究まで~2015

    • Author(s)
      古本祥三
    • Organizer
      平成27年度日本薬学会東北支部総会・学術講演会
    • Place of Presentation
      仙台
    • Year and Date
      2015-06-13
    • Related Report
      2015 Annual Research Report
    • Invited
  • [Presentation] Preclinical characterization of [18F]THK-5117 enantiomers as a PET tau probe for tau pathology in Alzheimer’s disease2015

    • Author(s)
      T. Tago, S. Furumoto, N. Okamura, R. Harada, H. Adachi, Y. Ishikawa, K. Yanai, R. Iwata, Y. Kudo.
    • Organizer
      21st International Symposium on Radiopharmaceutical Sciences
    • Place of Presentation
      Columbia, Missouri
    • Year and Date
      2015-05-26
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 2-アリールキノリン PET タウイメージング剤の構造活性相関研究2015

    • Author(s)
      多胡哲郎,古本祥三,岡村信行,原田龍一,石川洋一,谷内一彦,岩田錬,工藤幸司
    • Organizer
      日本分子イメージング学会第 10 回総会・学術集会
    • Place of Presentation
      東京
    • Year and Date
      2015-05-20
    • Related Report
      2015 Annual Research Report
  • [Presentation] Chirality of [18F]THK-5105 Affects its Preclinical Characteristics as a PET Tau Imaging Probe2015

    • Author(s)
      Tago T, Furumoto S, Okamura N, Harada R, Adachi H, Ishikawa Y, Yanai K, Iwata R, Kudo Y
    • Organizer
      9th Human Amyloid Imaging 2015
    • Place of Presentation
      米国マイアミ
    • Year and Date
      2015-01-14 – 2015-01-16
    • Related Report
      2014 Annual Research Report
  • [Presentation] PET用タウイメージング剤[18F]THK-5105のエナンチオマー体の詳細評価2014

    • Author(s)
      多胡 哲郎, 古本 祥三, 岡村 信行, 原田 龍一, 安立 創, 石川 洋一, 谷内 一彦, 工藤 幸司, 岩田 錬
    • Organizer
      第54回日本核医学会学術総会
    • Place of Presentation
      大阪
    • Year and Date
      2014-11-06 – 2014-11-08
    • Related Report
      2014 Annual Research Report
  • [Presentation] Accumulation of the novel tau imaging tracer, 18F-5117 is associated with brain atrophy in Alzheimer's disease.2014

    • Author(s)
      Ishiki A, Furumoto S, Harada R, Furukawa K, Okamura N, Tashiro M, Yanai K, Kudo Y, Arai H
    • Organizer
      Alzheimer's Association International Conference 2014
    • Place of Presentation
      コペンハーゲン
    • Year and Date
      2014-07-12 – 2014-07-17
    • Related Report
      2014 Annual Research Report
  • [Presentation] In vivo selective imaging of tau pathology in Alzheimer's disease with 18F-THK51172014

    • Author(s)
      Okamura N, Furumoto S, Harada R, Furukawa K, Ishiki A, Iwata R, Tashiro M, Yanai K, Arai H, Kudo Y.
    • Organizer
      Society of Nuclear Medicine and Molecular Imaging 2014
    • Place of Presentation
      米国セントルイス
    • Year and Date
      2014-06-07 – 2014-06-11
    • Related Report
      2014 Annual Research Report
  • [Presentation] Tau Probe Development: From A Molecular Design To A Clinical Research.2014

    • Author(s)
      Furumoto S., Okamura N., Kudo Y.
    • Organizer
      第9回日本分子イメージング学会総会・学術集会
    • Place of Presentation
      大阪千里
    • Year and Date
      2014-05-22 – 2014-05-23
    • Related Report
      2014 Annual Research Report
  • [Presentation] PET用タウイメージング剤[18F]THK-5105エナンチオマー体の評価2014

    • Author(s)
      多胡 哲郎, 古本 祥三, 岡村 信行, 原田 龍一, 安立 創, 石川 洋一, 谷内 一彦, 工藤 幸司, 岩田 錬
    • Organizer
      第9回日本分子イメージング学会総会・学術集会
    • Place of Presentation
      大阪千里
    • Year and Date
      2014-05-22 – 2014-05-23
    • Related Report
      2014 Annual Research Report
  • [Presentation] PET用タウイメージング剤[18F]THK5105のエナンチオマー体の合成と評価2013

    • Author(s)
      多胡哲朗、古本祥三、岡村信行、原田龍一、石川洋一、谷内一彦、工藤幸司、岩田錬
    • Organizer
      第53回日本核医学会学術総会
    • Place of Presentation
      福岡
    • Related Report
      2013 Annual Research Report
  • [Presentation] アルツハイマー病患者における[18F]THK5105の臨床評価2013

    • Author(s)
      岡村信行、古本祥三、原田龍一、多胡哲朗、谷内一彦、レイチェルマリガン、クリストファーロウ、ビクタービルマーニ
    • Organizer
      第53回日本核医学会学術総会
    • Place of Presentation
      福岡
    • Related Report
      2013 Annual Research Report

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Published: 2013-05-21   Modified: 2019-07-29  

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