61 针对前列腺癌的Cu-PSMA向PET:从放射性追踪器发展到首次在人体内进行成像
Tais Basaco Bernabeu1, Rosalba Mansi1, Luigi Del Pozzo1
1Division of Radiopharmaceutical Chemistry, University Hospital Basel, Basel, Switzerland.
概括
循环仪生产的标记铜-61 (61Cu) 的PSMA标记剂为广泛的前列腺癌成像提供了解决方案. [61Cu]Cu-NODAGA-PSMA-I&T显示了与现有的追踪剂相比有希望的结果,使得延迟成像成为可能.
科学领域:
- 核医学就是核医学.
- 放射化学 放射化学是指辐射化学.
- 在瘤学瘤学.
背景情况:
- 对前列腺特异性膜抗原 (PSMA) PET 标记物的需求不断增加.
- 由于半衰期短,目前-68 (68Ga) 和-18 (18F) PSMA 追踪剂的局限性限制了主要中心以外的使用.
- 需要可访问的PSMA PET成像解决方案.
研究的目的:
- 评估循环仪生产的-61铜 (61Cu) 用于标记PSMA PET标记剂,作为68Ga和18F的替代品.
- 评估61Cu标记的PSMA标记剂,特别是[61Cu]Cu-NODAGA-PSMA-I&T的潜力,以提高可访问性和治疗应用.
- 为了比较[61Cu]Cu-NODAGA-PSMA-I&T与已建立的PSMA追踪器的性能.
主要方法:
- 用61Cu合成和放射性标记PSMA-I&T和NODAGA-PSMA-I&T,使用61Cu.
- 在体外研究:脂性,亲和力,细胞吸收和分布.
- 在体内研究:PET/CT成像,生物分布和稳定性在临床前模型和第一次在人体成像.
- 与68Ga标记的PSMA跟踪器和18F-PSMA-1007.7进行比较.
主要成果:
- [61Cu]Cu-DOTAGA-PSMA-I&T和[61Cu]Cu-NODAGA-PSMA-I&T的高放射化学纯度 (>97%) 已经实现.
- 在体内研究表明,对[61Cu]Cu-NODAGA-PSMA-I&T的瘤吸收率和瘤与非瘤的比率是有利的,与参考痕迹剂相当或优于.
- 首次在人体成像成功可视化转移性前列腺癌病变.
结论:
- [61Cu]Cu-NODAGA-PSMA-I&T是一种有前途的PSMA放射追踪剂,在前列腺癌成像中具有有利的特性.
- 61Cu的更长半衰期允许更广泛的分布和延迟成像的潜力.
- 这种标记器提供了一个可行的替代方案,以克服68Ga和18FPSMA标记器的后勤挑战.
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