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<p>In recent years, ²¹¹At, a targeted α-emitting radionuclide, has demonstrated significant potential in cancer therapy. Its distinctive physical properties—including a moderate half-life, high linear energy transfer, short tissue penetration range, and a simplified decay pattern—enable maximal tumor cell eradication while sparing healthy tissues, particularly in micrometastases and small tumor foci. Multiple preclinical studies have shown that ²¹¹At-labeled radiopharmaceuticals exhibit strong tumor specificity, high therapeutic efficacy, and manageable safety profiles across both solid and hematologic malignancies. Strategic chemical modifications and the incorporation of nanomaterials have been reported to enhance the in vivo stability of ²¹¹At-labeled compounds. Nevertheless, widespread clinical translation remains limited by radionuclide availability, chemical instability, and the lack of rapid labeling technologies. Future investigations should focus on optimizing ²¹¹At production, labeling strategies, and targeting vector design to facilitate its clinical application in micrometastatic disease and personalized cancer therapy.</p>

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Advances in tumor-targeted ²¹¹At radiopharmaceuticals: preclinical investigations, challenges, and future perspectives

  • 期刊论文

  • 发表日期：

    2025年12月28日

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  • Min Wang,
  • Yuqin Li,
  • Bin Liu

摘要

In recent years, ²¹¹At, a targeted α-emitting radionuclide, has demonstrated significant potential in cancer therapy. Its distinctive physical properties—including a moderate half-life, high linear energy transfer, short tissue penetration range, and a simplified decay pattern—enable maximal tumor cell eradication while sparing healthy tissues, particularly in micrometastases and small tumor foci. Multiple preclinical studies have shown that ²¹¹At-labeled radiopharmaceuticals exhibit strong tumor specificity, high therapeutic efficacy, and manageable safety profiles across both solid and hematologic malignancies. Strategic chemical modifications and the incorporation of nanomaterials have been reported to enhance the in vivo stability of ²¹¹At-labeled compounds. Nevertheless, widespread clinical translation remains limited by radionuclide availability, chemical instability, and the lack of rapid labeling technologies. Future investigations should focus on optimizing ²¹¹At production, labeling strategies, and targeting vector design to facilitate its clinical application in micrometastatic disease and personalized cancer therapy.