Synthesis of 11C-Radiolabeled Eribulin as a Companion Diagnostics PET Tracer for Brain Glioblastoma

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  • Takashi Niwa
    Laboratory for Chemical Biology, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Tsuyoshi Tahara
    Laboratory for Biofunction Dynamics Imaging, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Charles E Chase
    Eisai Inc., 35 Cambridgepark Drive Suite 200, Cambridge, MA 02140 , USA
  • Francis G Fang
    Eisai Inc., 35 Cambridgepark Drive Suite 200, Cambridge, MA 02140 , USA
  • Takayoshi Nakaoka
    Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Satsuki Irie
    Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Emi Hayashinaka
    Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Yasuhiro Wada
    Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Hidefumi Mukai
    Laboratory for Molecular Delivery and Imaging Technology, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Kenkichi Masutomi
    Division of Cancer Stem Cell, National Cancer Center Research Institute, 5-1-1 Tsukiji, Chuo-ku, Tokyo 104-0045 , Japan
  • Yasuyoshi Watanabe
    Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Yilong Cui
    Laboratory for Biofunction Dynamics Imaging, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan
  • Takamitsu Hosoya
    Laboratory for Chemical Biology, RIKEN Center for Biosystems Dynamics Research (BDR), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo 650-0047 , Japan

Description

<jats:title>Abstract</jats:title> <jats:p>The successful 11C-radiolabeling of eribulin, an analog of the marine natural product halichondrin B, and an approved anticancer drug for the treatment of breast cancer and liposarcoma, is reported. A rapid sequence involving a nitroaldol reaction with [11C]nitromethane and subsequent reduction of the nitro group enabled the introduction of a carbon-11 atom at the C35-position of eribulin. Optimization of the reaction and purification conditions led to a reproducible synthetic method for [35-11C]eribulin with 248 ± 104 MBq of radioactivity, 88.2 ± 5.8% radiochemical purity, and 132 ± 32 MBq/nmol molar activity. The total synthetic time was 38.0 ± 1.3 min (n = 12). PET imaging using mice bearing brain tumors revealed a specific accumulation of [35-11C]eribulin in tumors without any significant metabolic changes. These results indicate the applicability of [35-11C]eribulin for the quantitative measurement of eribulin migration into tumor tissue, which would be beneficial for exploring the application of eribulin for glioblastoma treatment and estimating the appropriate dosage for each patient.</jats:p>

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