Development of new radiopharmaceuticals for support system of anti-tumor drug therapy.

• Project/Area Number: 23591828
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: Osaka University of Pharmaceutical Sciences
• Principal Investigator: HIRATA masahiko 大阪薬科大学, 薬学部, 講師 (00268301)
• Project Period (FY): 2011-04-28 – 2015-03-31
• Project Status: Completed (Fiscal Year 2014)
• Budget Amount: ¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000); Fiscal Year 2014: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2013: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2012: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2011: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
• Keywords: 放射性医薬品 / EGF / チロシンキナーゼ / SPECT / 核医学 / 診断 / 放射性ヨウ素 / 抗癌剤 / 治療効果予測 / 核医学診断 / EGFR / tyrosine kinase / radiopharmacrtical / tumor / シグナル伝達 / ピペリジン誘導体 / 分子イメージング / T790

Outline of Final Research Achievements

New radiopharmaceticals which could support a cancer treatment plan.were developed The affinity of new radiopharmacruticals to EGFR-TK wrere weak as imaging probe.Form these result, a side chain greatly influenced activity.From some examination,the prediction of the curative effect of the anticancer drug was got using our new compounds.

Research Products

• [Journal Article] Monitoring of gefitinib sensitivity with radioiodinated PHY based on EGFR expression. (2014)
  • Author(s): Yoshimoto M, Hirata M, Kanai Y, Naka S, Nishii R, Kagawa S, Kawai K, Ohmomo Y.
  • Journal Title: Biol Pharm Bull Volume: 37 Pages: 355-60
  • NAID: 130003390939
  • Peer Reviewed / Open Access / Acknowledgement Compliant
• [Journal Article] Relationship between uptake of a radioiodinated quinazoline derivative and radiosensitivity in non-small cell lung cancer. (2014)
  • Author(s): Zhu HJ, Ogawa M, Magata Y, Hirata M, Ohmomo Y, Sakahara H.
  • Journal Title: Am J Nucl Med Mol Volume: 7 Pages: 293-302
  • Peer Reviewed / Open Access / Acknowledgement Compliant
• [Journal Article] Assessment of epidermal growth factor receptor status in glioblastomas (2014)
  • Author(s): Hui‐Jun Zhu, Mikako Ogawa, Yasuhiro Magata, Masahiko Hirata, Yoshiro Ohmomo, Hiroki Namba, Harumi Sakahara
  • Journal Title: Asia Oceania J Nucl Med Biol Volume: 1 Pages: 47-52
  • Open Access / Acknowledgement Compliant
• [Journal Article] Monitoring of gefitinib sensitivity with radioiodinated PHY based on EGFR expression (2014)
  • Author(s): Yoshimoto M, Hirata M, Kanai Y, Naka S, Nishii R, Kagawa S, Kawai K, Ohmomo Y.
  • Journal Title: Biol Pharm Bull. Volume: 37 Pages: 355-360
  • NAID: 130003390939
  • Peer Reviewed
• [Journal Article] A useful EGFR-TK ligand for tumor diagnosis with SPECT: development of radioiodinated 6-(3-morpholinopropoxy)-7-ethoxy-4-(3'-iodophenoxy)quinazoline. (2013)
  • Author(s): Hirata M, Kanai Y, Naka S, Yoshimoto M, Kagawa S, Matsumuro K, Katsuma H, Yamaguchi H, Magata Y, Ohmomo Y.
  • Journal Title: Ann Nucl Med. Volume: 27 Issue: 5 Pages: 431-443
  • DOI: 10.1007/s12149-013-0703-y
  • NAID: 10031183404
  • Peer Reviewed
• [Journal Article] Assessment of epidermal growth factor receptor status in glioblastomas (2013)
  • Author(s): Hui‐Jun Zhu, Mikako Ogawa, Yasuhiro Magata, Masahiko Hirata, Yoshiro Ohmomo, Hiroki Namba, Harumi Sakahara.
  • Journal Title: Asia Oceania J Nucl Med Biol. Volume: 1 Pages: 47-52
  • Peer Reviewed
• [Presentation] HER2イメージング薬剤p-LSYを用いたラパチニブ感受性の予測 (2014)
  • Author(s): 平田雅彦, 吉本光喜, 小川美香子, 間賀田泰寛, 大桃善朗
  • Organizer: 第５４回日本核医学会総会
  • Place of Presentation: 大阪
  • Year and Date: 2014-11-06 – 2014-11-08
• [Presentation] Development of a novel PET tracer targeting phosphatidylinositol 3-kinase (PI3K) in tumor (2014)
  • Author(s): Akira Makino, Takahiro Arai, Takashi Temma, Masahiko Hirata, Masahiro Ono, Yoshiro Ohmomo, Hideo Saji
  • Organizer: 27th Annual European Association of Nuclear Medicine Congress
  • Place of Presentation: Sweden
  • Year and Date: 2014-10-18 – 2014-10-22
• [Presentation] Development of a novel SPECT radiopharmaceutical targeting human epidermal growth factor type2 in tumor (2014)
  • Author(s): Masahiko Hirata, Mitsuyoshi Yoshimoto, Mikako Ogawa,Yasuhiro Magata, Yoshiro Ohmomo,
  • Organizer: World Fedration of Nuclear Medicine and Biology
  • Place of Presentation: Mexico
  • Year and Date: 2014-08-27 – 2014-08-31
• [Presentation] Pharmacokinetics and anti-tumor activity of AY002 with high affinity to EGFR-TK (2014)
  • Author(s): Mitsuyoshi Yoshimoto, Sadaaki Kimura, Masahiko Hirata, Yoshiro Ohmomo, Keiichi Kawai, and Hirofumi Fujii
  • Organizer: Society of Nuclear Medicine and Molecular Imaging
  • Place of Presentation: ST. Luise
  • Year and Date: 2014-06-07 – 2014-06-11
• [Presentation] 肺がん細胞の放射線治療とゲフィチニブ治療における[125I]PYK による効果予測 (2013)
  • Author(s): 朱蕙君、小川美香子、間賀田泰寛、平田雅彦、大桃善朗 、阪原晴海
  • Organizer: 日本分子イメージング学会
  • Place of Presentation: 横浜
• [Presentation] 新規HER2 受容体チロシンキナーゼ分子イメージング薬剤の合成と基礎評価 (2013)
  • Author(s): 平田雅彦、吉本光喜、小川美香子、間賀田泰寛、大桃善朗
  • Organizer: 日本分子イメージング学会
  • Place of Presentation: 横浜
• [Presentation] アニリノピリミジンを基本骨格とするEGFR-TK 阻害剤の開発 (2013)
  • Author(s): 吉本光喜、木村禎亮、平田雅彦、大桃善朗、川井恵一、藤井博史
  • Organizer: 日本分子イメージング学会
  • Place of Presentation: 横浜
• [Presentation] Synthesis and evaluation of iodinated cyclopropanecarboxylic acid {3-[6-(phenylamino)-pyrimidin-4-ylamino]-phenyl}-amides as EGFR-TK imaging agents. (2013)
  • Author(s): Yoshimoto M, Kimura S, Yamada K, Hirata M, Ohmomo Y, Kunishima M, Kawai K, Fujii H.
  • Organizer: The 20th International Symposium on Radiopharmaceutical Sciences,
  • Place of Presentation: Jeju (Korea)
• [Presentation] Development of novel EGFR-TK imaging agents based on anilinopyrimidine structure. (2013)
  • Author(s): Yoshimoto M, Kimura S, Hirata M, Ohmomo Y, Kawai K, Fujii H.
  • Organizer: The 60th Annual Meeting of the Society of Nuclear Medicine
  • Place of Presentation: Vancouver
• [Presentation] シグマレセプターを標的とする99mTc 標識ピペラジン誘導体の合成と基礎評価 (2013)
  • Author(s): 平田雅彦、大桃善朗
  • Organizer: 第53回 日本核医学会総会
  • Place of Presentation: 福岡
• [Presentation] 放射性ヨウ素標識アニリノピリミジン誘導体の合成と基礎的検討 (2013)
  • Author(s): 吉本光喜、木村禎亮、平田雅彦、大桃善朗、川井恵一、藤井博史
  • Organizer: 第53回 日本核医学会総会
  • Place of Presentation: 福岡