Development of F-18 fluorodeoxymannose (FDM) as a PET probe for cancer imaging

• Project/Area Number: 19390312
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Radiation science
• Research Institution: Tohoku University
• Principal Investigator: FUKUDA Hiroshi Tohoku University, 加齢医学研究所, 教授 (30125645)
• Co-Investigator(Kenkyū-buntansha): IWATA Ren 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 (60143038) ; YOSHIOKA Takashi 山形大学, 医学部, 教授 (90271981)
• Co-Investigator(Renkei-kenkyūsha): FURUMOTO Shozo 東北大学, 大学院・医学系研究科, 講師 (00375198)
• Project Period (FY): 2007 – 2009
• Project Status: Completed (Fiscal Year 2009)
• Budget Amount: ¥11,960,000 (Direct Cost: ¥9,200,000、Indirect Cost: ¥2,760,000); Fiscal Year 2009: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000); Fiscal Year 2008: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000); Fiscal Year 2007: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
• Keywords: 画像診断学(含放射線診断学、核医学) / 腫瘍イメージンダ / PET / ^<18>F-フルオロデオキシマンノース / 標識合成法 / 求核置換反応 / ^<18>F-フルオロデオキシグルコース / がん画像診断 / デオキシマンノース / デオキシグルコース

Research Abstract

We attempted to develop a method for radio-synthesis of ^<18>F-fluorodeoxymannose (^<18>F-FDM) by nucleofilic substituted reaction. We synthesized 3 precursors for ^<18>F-FDM radio-synthesis and ^<18>F-FDM was successfully synthesized using precursor 3 with high radiochemical yield (43-67%) and purity (94-98%). Bio-distribution and imaging studies of tumor bearing rat revealed high tumor uptake, relatively low uptake in the brain and rapid clearance from the kidney and blood. No acute toxicity was found in mice administered with 0.1および1.0mg/kg of cold FDM.

Research Products

• [Journal Article] Electrochemical concentration of no-carrier-added [^<18>F]fluoride from [^<18>O]water in a disposable microfluidic cell for radiosynthesis of ^<18>F-labeled radiopharmaceuticals (2010)
  • Author(s): Saiki H, Iwata R, 9人, 2番目
  • Journal Title: Appl Radiat Isot (In press)
  • Peer Reviewed
• [Journal Article] Clinical evaluation of whole-body FDG PET for recurrent gastric cancer : A multicenter study (2009)
  • Author(s): Nakamoto Y, Fukuda H (12人, 4番目)
  • Journal Title: Jpn J Clin Oncol 39 Pages: 297-302
  • Peer Reviewed
• [Journal Article] A bone marrow F-18 FDG uptake exceeding the liver uptake may indicate bone marrow hyperactivity (2009)
  • Author(s): Inoue K, Fukuda H(4人, 4番目)
  • Journal Title: Ann Nucl Med 23 Pages: 643-649
  • NAID: 10026098997
  • Peer Reviewed
• [Journal Article] Clinical significance of performing ^<18>F-FDG PET on patients with gastrointestinal stromal tumors : a summary of a Japanese multicenter study (2009)
  • Author(s): Kaneta T, Fukuda H(14人, 3番目)
  • Journal Title: Ann Nucl Med 23 Pages: 459-464
  • NAID: 10025136699
  • Peer Reviewed
• [Journal Article] 18FDG uptake associated with CT density on PET/CT in lungs with and without chronic interstitial lung diseases (2009)
  • Author(s): Inoue K, Fukuda H(6人, 6番目)
  • Journal Title: Ann Nucl Med 23 Pages: 277-281
  • NAID: 10025136113
  • Peer Reviewed
• [Journal Article] ^<18>FDG uptake associated with CT density on PET/CT in lungs with and without chronic interstitial lung diseases (2009)
  • Author(s): Inoue K, Fukuda H, 6人6番目
  • Journal Title: Ann Nucl Med 23 Pages: 277-281
  • NAID: 10025136113
  • Peer Reviewed
• [Journal Article] Clinical significance of performing ^<18>F-FDG PET on patients with gastrointestinal stromal tumors : a summary of a Japanese multicenter study (2009)
  • Author(s): Kaneta T, Fukuda H, 14人, 3番目
  • Journal Title: Ann Nucl Med 23 Pages: 459-464
  • NAID: 10025136699
  • Peer Reviewed
• [Journal Article] A bone marrow F-18 FDG uptake exceeding the liver uptake may indicate bone marrow hyperactivity (2009)
  • Author(s): Inoue K, Okada K, Kinomura S, Fukuda H
  • Journal Title: Ann Nucl Med 23 Pages: 449-643
  • NAID: 10026098997
  • Peer Reviewed
• [Journal Article] Clinical value of whole-body FDG-PET for recurrent gastric cancer : A multicenter study (2009)
  • Author(s): Nakamoto Y, Fukuda H, 12人, 4番目
  • Journal Title: Jpn J Clin Oncol 39 Pages: 297-302
  • Peer Reviewed
• [Journal Article] FDG PET for esophargeal cancer complicated by sarcoidosis mimicking mediastinal and hilar lymphnode metastases : two case reports (2008)
  • Author(s): Takanami K, Fukuda H(7人, 6番目)
  • Journal Title: Clin Nucl Med 33 Pages: 258-261
  • Peer Reviewed
• [Journal Article] Whole-body tumor imaging : O-[^<11>C]methyl-L-tyrosine/positron emission tomography (2008)
  • Author(s): Ishiwata K, Iwata R(4人, 4番目)
  • Journal Title: Cancer Imaging 2 Pages: 175-179
  • Peer Reviewed
• [Journal Article] Q fever with lymphadenopathy on F-18 FDG PET (2008)
  • Author(s): Takanami K, Fukuda H (8人, 7番目)
  • Journal Title: Clin Nucl Med 33 Pages: 436-437
  • Peer Reviewed
• [Journal Article] Increase of serum CA19-9 level without an evident lesion on conventional imaging is insufficient for justification of 18FDG PET examination (2008)
  • Author(s): Inoue K, Fukuda H(7人, 7番目)
  • Journal Title: Hepato-Gastroenterology 55 Pages: 46-49
  • Peer Reviewed
• [Journal Article] Increase of serum CA19-9 level without an evident lesion on conventional imaging is insufficient for justification of ^<18>FDG-PET examination (2008)
  • Author(s): Inoue K, Fukuda H(7人7番目)
  • Journal Title: Hepato-Gastroenterology 55 Pages: 46-49
  • Peer Reviewed
• [Journal Article] Molecular Imaging at Tohoku University : From Cancer to Neuroreceptors (2008)
  • Author(s): Tashiro M, Fukuda H, Itoh M, Matsuzawa T, Yanai K.
  • Journal Title: Medical Imaging Reviews 4 Pages: 8-13
  • Peer Reviewed
• [Journal Article] Q fever with lymphadenopathy on F-18 FDG PET (2008)
  • Author(s): Takanami K, Fukuda H(8人7番目)
  • Journal Title: Clinical Nuclear Medicine 33 Pages: 436-437
  • Peer Reviewed
• [Journal Article] FDG PET for esophageal cancer complicated by sarcoidosis mimicking mediastinal and hilar lymph node metastases : two case reports (2008)
  • Author(s): Takanami K, Fukuda H(7人6番目)
  • Journal Title: Clinical Nuclear Medicine 33 Pages: 258-261
  • Peer Reviewed
• [Journal Article] 私が歩んできた学際的医工学研究の道-PET, BNCT (2008)
  • Author(s): 福田寛
  • Journal Title: 医学物理 28 Pages: 3-6
  • NAID: 10026092258
• [Journal Article] ポジトロン断層法(PET)によるがんの生物特性イメージング (2008)
  • Author(s): 福田寛
  • Journal Title: 癌と化学療法 35 Pages: 1281-1285
• [Journal Article] がん薬物療法におけるポジトロンCTの役割 (2008)
  • Author(s): 吉岡 孝志
  • Journal Title: 山形医学 26 Pages: 1-9
  • NAID: 110006537359
  • Peer Reviewed
• [Journal Article] Diagnosing active inflammation in the SAPHO syndrome using ^<18>FDG PET/CT in suspected metastatic vertebral one tumor (2007)
  • Author(s): Inoue K, Fukuda H(9人, 9番目)
  • Journal Title: Ann Nucl Med 21 Pages: 477-480
  • Peer Reviewed
• [Journal Article] Initial evaluation of dynamic human imaging using 18F-FRP170 as a new PET tracer form imaging hypoxia (2007)
  • Author(s): Kaneta T, Fukuda H(17人, 15番目)
  • Journal Title: Ann Nucl Med 21 Pages: 101-107
  • Peer Reviewed
• [Journal Article] Initial evaluation of dynamic human imaging using 18F-FRP170 as a new PET tracer for imaging hypoxia. (2007)
  • Author(s): Kaneta T
  • Journal Title: Annals of Nuclear Medicine 21 Pages: 101-107
  • Peer Reviewed
• [Journal Article] Performance profile of FDG-PET and PET/CT for cancer screening on the basis of a Japanese nationwide survey. (2007)
  • Author(s): Minamimoto R
  • Journal Title: Annals of Nuclear Medicine 21 Pages: 481-498
  • Peer Reviewed
• [Journal Article] Diagnosing active inflammation in the SAPHO syndrome using 18FDG-PET/CT in suspected metastatic vertebral bone tumors. (2007)
  • Author(s): Inoue K
  • Journal Title: Annals of Nuclear Medicine 21 Pages: 477-480
  • Peer Reviewed
• [Journal Article] 2-(2-[2-Dimethylaminothiazol-5-yl]ethy1)-6-(2-[fluoro]ethoxy]benzoxazole: anovel PET agent for in vivo detection of dense amyloid plaques in Alzhymer's disease patients. (2007)
  • Author(s): Kudo Y
  • Journal Title: J. Nucl. Med. 48 Pages: 553-561
  • Peer Reviewed
• [Journal Article] First achievement of less than 1 mm FWHM resolution in practical semiconductor animal PET scanner. (2007)
  • Author(s): Ishii K
  • Journal Title: Nucl. Instr. Meth. Phys. Res. A576 Pages: 435-440
  • Peer Reviewed
• [Journal Article] Evaluation of the binding characteristics of [18F]fluoroproxyfan in the rat brain for in vivo visualization of histamine H_3 receptor. (2007)
  • Author(s): Funaki Y
  • Journal Title: Nucl. Med. Biol. 34 Pages: 981-987
  • Peer Reviewed
• [Journal Article] Electrochemical concentration of no-carrier added [^<18>F]fluoride from [^<18>O]water in a disposable microfluidic cell for radiosynthesis of ^<18>F-labereld radiopharmaceuticlas
  • Author(s): Saiki H, Iwata R (9人, 2番目)
  • Journal Title: Appl Radiat Isot (in press)
  • Peer Reviewed
• [Presentation] 求核置換反応を利用したフルオロデオキシマンノース合成法の確立と腫瘍集積性の評価 (2010)
  • Author(s): 新保亮, 岩田錬, 福田寛 (8人, 7,8番目)
  • Organizer: 日本薬学会第130回年会
  • Place of Presentation: 岡山
  • Year and Date: 2010-03-30
• [Presentation] 2-フロロピリジン誘導体化による代謝安定性の向上を目指した^<18>F標識MMP-2画像化プローブの開発 (2009)
  • Author(s): 古本祥三, 岩田錬, 福田寛, (6人, 5,6番目)
  • Organizer: 第49回日本核医学会学術総会
  • Place of Presentation: 旭川
  • Year and Date: 2009-10-01
• [Presentation] 新規前駆体による[^<18>F]FDM合成とその生物学的評価 (2009)
  • Author(s): 新保亮, 岩田錬, 福田寛, (8人, 7,8番目)
  • Organizer: 第49回日本核医学会学術総会
  • Place of Presentation: 旭川
  • Year and Date: 2009-10-01
• [Presentation] Synthesis and preliminary evaluation of [^<18>F] FDM for tumor imaging (2009)
  • Author(s): Furumoto S, Iwata R, Fukuda H(6人, 5,6番目)
  • Organizer: 18^<th> Int Symp Radiopharm Sci
  • Place of Presentation: Edmonton, Canada
• [Presentation] Managegment of physiologically increased FDG uptake in the myocardium for the diagnosis of the mediastinal and lung diseases nearby heart and the myocardial disease (2009)
  • Author(s): Takanami K, Fukuda H(4人, 3番目)
  • Organizer: 56^<th> SNM Annual Meeting
  • Place of Presentation: Toronto, Canada
• [Presentation] Combination of multimodality imaging for evaluationg cardiac involvement of sarcoidosis (2009)
  • Author(s): Takanami K, Fukuda H, (6人, 4番目)
  • Organizer: Annual Meeting of RSNA
  • Place of Presentation: Chicago, USA
• [Presentation] Synthesis and preliminary evaluation of [^<18>F]FDM for tumor imaging (2009)
  • Author(s): 古本祥三, 福田寛, 6人, 6番目
  • Organizer: ^<18>th Int Symp Radiopharm Sci
  • Place of Presentation: Edmonton, Canada
• [Presentation] Management of physiologically increased FDG uptake in the myocardium for the diagnosis of the mediastinal and lung diseases nearby heart and the myocardial disease (2009)
  • Author(s): Takanami K, Kaneta K, Fukuda H, Takahashi S
  • Organizer: 56^<th> SNM Annual Meeting
  • Place of Presentation: Toronto, Canada
• [Presentation] Intraductal papillary mucinous neoplasm of the pancreas : a comparison of the likelihood of invasiveness between ^<18>F-FDG PET/CT and contrast enhanced MDCT findings (2009)
  • Author(s): Takanami K, Kaneta K, Fukuda H, Takahashi S
  • Organizer: 56^<th> SNM Annual Meeting
  • Place of Presentation: Toronto, Canada
• [Presentation] Combination of multimodality imaging for evaluating cardiac involvement of sarcoidosis (2009)
  • Author(s): Takanami K, Fukuda H, 6人、4番目
  • Organizer: Annual Meeting of Radiological Society of North America 2009
  • Place of Presentation: Chicago, USA
• [Presentation] Intraductal papillary mucinous neoplasm of the bile ducts : Multimodality assessment with pathologic correlation (2009)
  • Author(s): Takanami K, Fukuda H, 6人、5番目
  • Organizer: Annual Meeting of Radiological Society of North America 2009
  • Place of Presentation: Chicago, USA
• [Presentation] F18-FDG PET/CT findings of Uncommon hepatobiliary/liver tumors (2009)
  • Author(s): Takanami K, Fukuda H, 7人、6番目
  • Organizer: Annual Meeting of Radiological Society of North America 2009
  • Place of Presentation: Chicago, USA
• [Presentation] Association of ^<18>FDG uptake by bone marrow and spleen with hematological parameters in patients with and without malignancy (2008)
  • Author(s): Inoue K, Fukuda H (7人, 7番目)
  • Organizer: Annual Congress of the European Association of Nuclear Medicine 2008, Munich, Germany
  • Place of Presentation: Munich, Germany
• [Presentation] Correlation of lung FDG uptake and CT density in dependent regions with and without interstitial lung disease on 18FDG-PET/CT. (2007)
  • Author(s): Inoue K
  • Organizer: 54th SNM Annual Meeting
  • Place of Presentation: ワシントンDC, USA
  • Year and Date: 2007-06-05
• [Presentation] Assessment of tumor hypoxia induced by vascular targeting therapy. (2007)
  • Author(s): Furumoto S
  • Organizer: 54th SNM Annual Meeting
  • Place of Presentation: ワシントンDC, USA
  • Year and Date: 2007-06-04
• [Presentation] Assessement of hypoxia induced by vascular targeting therapy (2007)
  • Author(s): Furumoto S, Iwata R, Fukuda H(10人, 8, 10番目)
  • Organizer: 54^<th> SNM Annual Meeting
  • Place of Presentation: Washington DC, USA
• [Presentation] Influences of nitrogylcelin treatment on tumor uptake of hypoxia marker, [F-18]FRP170 (2007)
  • Author(s): Kaneta T, Iwata R, Fukuda H(11人, 3,10番目)
  • Organizer: 54^<th> SNM Annual Meeting
  • Place of Presentation: Washington DC, USA
• [Presentation] Influence of nitrogycerin treatment on tumor uptake of hypoxia marker, [F18]FRP170. (2007)
  • Author(s): Kaneta T
  • Organizer: 54th SNM Annual Meeting
  • Place of Presentation: ワシントンDC, USA
• [Presentation] Correlation of lung FDG uptake and CT dependent density regions with and without interstitial lung diseases on ^<18>FDG-PET/CT (2006)
  • Author(s): Inoue K, Fukuda H (7人, 7番目)
  • Organizer: 54^<th> SNM Annual Meeting
  • Place of Presentation: Washington DC, USA
• [Book] PET-CT診断マニュアル (2008)
  • Author(s): 岡田 賢, 福田 寛, 井上健太郎
  • Publisher: 中外医学社
• [Book] PET-CT画像診断マニュアル (2008)
  • Author(s): 岡田賢、井上健太郎、福田寛(村上康二編)
  • Total Pages: 256
  • Publisher: 中外医学社
• [Book] PET-CT 画像診断マニュアル (2008)
  • Author(s): 岡田 賢
  • Publisher: 中外医学社
• [Book] ますます広がる分子イメージング技術 (2008)
  • Author(s): 福田 寛
  • Publisher: メディカルドゥ
• [Book] 非侵襲的・可視化ハンドブック-ナノ・バイオ・医療から情報システムまで (2007)
  • Author(s): 小川誠二, 上野照剛監修, 編集委員, 福田 寛(編集委員10人, 順序なし)
  • Total Pages: 1080
  • Publisher: エヌ・ティー・エス社
• [Book] 生体イメージング法におけるPETの位置づけ (小川誠二, 上野照剛監修), 「非侵襲的・可視化ハンドブック-ナノ・バイオ・医療から情報システムまで」 (2007)
  • Author(s): 福田 寛
  • Publisher: エヌ・ティー・エス社
• [Book] 非侵襲的・可視化ハンドブック-ナノ・バイオ・医療から情報システムまで (2007)
  • Author(s): 福田 寛, 窪田和雄, 小川誠二, 上野照剛監修
  • Publisher: エヌ・ティー・エス社
• [Book] 非侵襲的・可視化ハンドブック-ナノ・バイオ・医療から情報システムまで (2007)
  • Author(s): 岩田 錬, 小川誠二, 上野照剛監修
  • Publisher: エヌ・ティー・エス社
• [Book] 非侵襲・可視化技術ハンドブック (2007)
  • Author(s): 福田 寛
  • Publisher: エヌ・ティー・エス
• [Book] Future medical engineering based on bionanotechnology (2007)
  • Author(s): Suzuki M
  • Publisher: Imperial College Press
• [Book] クリニカルPETの最前線 (2007)
  • Author(s): 吉岡 孝志
  • Publisher: 先端医療技術研究所