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合成和临床前评估针对PET和光学成像的FAP准放射追踪器
Jürgen Kogler1,2, Cornelius K Donat1, Johanna Trommer1,2
1Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), 01328, Dresden, Germany.
EJNMMI radiopharmacy and chemistry
|December 5, 2025
概括
针对纤维细胞激活蛋白α (FAP) 的新双模成像追踪器对固体瘤具有很高的特异性. 这些标记物使得术前确切的诊断和术后可视化成为可能,从而有可能改善癌症治疗的结果.
科学领域:
- 在瘤学瘤学.
- 医疗成像医学成像
- 分子生物学分子生物学
背景情况:
- 精确的癌症诊断对于有效的治疗至关重要,但手术内成像工具有限,导致瘤不完全去除.
- 纤维细胞激活蛋白α (FAP) 是癌症成像和治疗的目标.
- 开发用于双模成像的多功能追踪器可以增强手术前诊断和手术内指导.
研究的目的:
- 开发用于双模成像的新型纤维细胞激活蛋白α (FAP) 向标志物.
- 为了使手术前的正子发射断层扫描 (PET) 和手术内的光导向手术.
主要方法:
- 用 (R) -NODAGA合剂和光剂合成两个双模标记物 (NODAGA-FAP647和NODAGA-FAP800).
- 在体外评估使用FAP表达和野生类型细胞和异种移植组织的结合亲和力和动力学.
- 在体内评估药理动力学和瘤吸收使用PET和光成像在小鼠.
主要成果:
- 这两种标志物都在体外显示出与人类FAP (hFAP) 的皮科莫尔结合亲缘关系.
- 在体内,在10-20分钟内,在hFAP表达瘤中迅速积累的标记物具有高选择性.
- 选择性瘤吸收得到维持,与注射后24小时观察到的正常组织形成良好对比.
结论:
- 两种新的针对FAP的双模联体被成功合成和评估.
- 标记物具有高特异性,迅速瘤积累,并长时间保留瘤.
- 这些特性使它们成为癌症成像和手术中临床翻译的有希望的候选人.
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