[Updated on Apr. 18] Integration of CiNii Articles into CiNii Research

Preliminary Evaluation of Astatine-211-Labeled Bombesin Derivatives for Targeted Alpha Therapy

  • Aoki Miho
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University Graduate School of Medical Sciences, Kanazawa University
  • Zhao Songji
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Takahashi Kazuhiro
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Washiyama Kohshin
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Ukon Naoyuki
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Tan Chengbo
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Shimoyama Saki
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Nishijima Ken-ichi
    Advanced Clinical Research Center, Fukushima Global Medical Science Center, Fukushima Medical University
  • Ogawa Kazuma
    Graduate School of Medical Sciences, Kanazawa University Institute for Frontier Science Initiative, Kanazawa University

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Abstract

<p>There are various diagnostic and therapeutic agents for prostate cancer using bombesin (BBN) derivatives, but astatine-211 (211At)-labeled BBN derivatives have yet to be studied. This study presented a preliminary evaluation of 211At-labeled BBN derivative. Several nonradioactive iodine-introduced BBN derivatives (IB-BBNs) with different linkers were synthesized and their binding affinities measured. Because IB-3 exhibited a comparable affinity to native BBN, [211At]AB-3 was synthesized and the radiochemical yields of [211At]AB-3 was 28.2 ± 2.4%, with a radiochemical purity of >90%. The stability studies and cell internalization/externalization experiments were performed. [211At]AB-3 was taken up by cells and internalized; however, radioactivity effluxed from cells over time. In addition, the biodistribution of [211At]AB-3, with and without excess amounts of BBN, were evaluated in PC-3 tumor-bearing mice. Despite poor stability in murine plasma, [211At]AB-3 accumulated in tumor tissue (4.05 ± 0.73%ID/g) in PC-3 tumor-bearing mice, which was inhibited by excess native BBN (2.56 ± 0.24%ID/g). Accumulated radioactivity in various organs is probably due to free 211At. Peptide degradation in murine plasma and radioactivity efflux from cells are areas of improvement. The development of 211At-labeled BBN derivatives requires modifying the BBN sequence and preventing deastatination.</p>

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