{
  "abstract": "Prostate cancer remains a leading cause of cancer-related mortality. Targeted alpha therapy using 211At is a promising treatment, although the low tumor-to-kidney ratios of 211At-labeled agents pose a persistent challenge. In this study, we designed prostate-specific membrane antigen (PSMA)-targeted radioligands incorporating 125I-labeled p-iodophenyl (IP) or 211At-labeled p-astatophenyl (AP) derivatives with different carbon-chain lengths and evaluated their impact on pharmacokinetics. In biodistribution studies, while [125I]IP-Cn-PSMA (n = 1, 2, or 4) exhibited low blood retention or high renal uptake, [125I]IP-C3-PSMA showed marked blood retention and low renal uptake, resulting in a higher tumor-to-kidney ratio compared with [125I]IP-C1-PSMA. [211At]AP-C1-PSMA and [211At]AP-C3-PSMA showed pharmacokinetic trends in the blood and kidneys comparable to those of the corresponding 125I-labeled compounds, despite partial deastatination. These results suggest that C3-chain-based IP and AP derivatives are effective for improving the tumor-to-kidney ratio, although the C1-chain-based derivatives retain advantages in early pharmacokinetics. Further comprehensive evaluations in tumor-bearing mice are required to determine the optimal candidate for PSMA-targeted 211At-labeled agents, potentially involving additional pharmacokinetic fine-tuning.",
  "abstract_shown": true,
  "affiliations": [],
  "article_type": null,
  "arxiv": null,
  "author_total": 9,
  "authors": [
    {
      "name": "Kazuma Nakashima"
    },
    {
      "name": "Honoka Asahina"
    },
    {
      "name": "Takuma Hasegawa"
    },
    {
      "name": "Hiroyuki Fujimoto"
    },
    {
      "name": "Masashi Murakami"
    },
    {
      "name": "Kazuhiro Ooe"
    },
    {
      "name": "Atsushi Toyoshima"
    },
    {
      "name": "Hiroyuki Watanabe"
    },
    {
      "name": "Masahiro Ono"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/4har9dsbjnwzj.bib",
  "cited_by": 0,
  "doi": "10.1248/cpb.c26-00140",
  "fulltext_url": "https://www.jstage.jst.go.jp/article/cpb/74/9/74_c26-00140/_article",
  "id": "4har9dsbjnwzj",
  "issns": [
    "1347-5223",
    "0009-2363"
  ],
  "landing_url": "https://www.jstage.jst.go.jp/article/cpb/74/9/74_c26-00140/_article",
  "language": null,
  "licence": "CC-BY-NC",
  "licence_label": "CC BY-NC",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by-nc/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "jstage-journal",
      "chemistry/medicinal"
    ],
    [
      "openalex",
      "2741|Radiopharmaceutical Chemistry and Applications"
    ]
  ],
  "openalex": "W7204783840",
  "pdf_url": "https://www.jstage.jst.go.jp/article/cpb/74/9/74_c26-00140/_pdf",
  "pmcid": null,
  "pmid": null,
  "published": "2026-09-01",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/4har9dsbjnwzj.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:17:34Z",
      "native_id": "10.1248/cpb.c26-00140",
      "source": "jstage",
      "url": "https://www.jstage.jst.go.jp/article/cpb/74/9/74_c26-00140/_article"
    }
  ],
  "subjects": [
    {
      "field": "medicine",
      "origin": "openalex:2741|Radiopharmaceutical Chemistry and Applications",
      "subfield": "imaging"
    }
  ],
  "title": "Effect of Carbon-Chain Length in [¹²⁵I]iodophenyl and [²¹¹At]astatophenyl Derivatives on Prostate-Specific Membrane Antigen-Targeted Radioligands",
  "title_text": "Effect of Carbon-Chain Length in [¹²⁵I]iodophenyl and [²¹¹At]astatophenyl Derivatives on Prostate-Specific Membrane Antigen-Targeted Radioligands",
  "type": "peer-reviewed",
  "updated_at": "2026-10-30T12:17:34Z",
  "url": "https://research.draconitic.com/paper/4har9dsbjnwzj",
  "venue": "Chemical and Pharmaceutical Bulletin",
  "versions": []
}