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使用Cu- 61标记的FAP抑制剂对FAP向PET成像进行增强对比:开发和临床前评估新型[Cu- 61]PET放射连接体
Jacopo Millul1, Tais Basaco Bernabeu1, Raghuvir H Gaonkar1
1Division of Radiopharmaceutical Chemistry, University Hospital Basel, Basel, Switzerland.
EJNMMI radiopharmacy and chemistry
|August 21, 2025
概括
这项研究介绍了Kalios,一种用于纤维细胞激活蛋白 (FAP) 成像的新型Copper-61标记放射体. 它的半衰期更长,可以延迟成像,改善瘤可视化和治疗潜力.
科学领域:
- 放射化学
- 核医学
- 癌症学
背景情况:
- 纤维细胞激活蛋白 (FAP) 成像对于各种癌症至关重要.
- 当前的FAP向型放射体 (例如68Ga,18F) 的半衰期很短,限制了成像窗口.
- 需要具有扩展分布和成像范围的放射性体.
研究的目的:
- 开发和特征Kalios,一个新的类型的FAP准无线电连体.
- 评估Copper-61 (Cu) 对于针对FAP的成像的有用性.
- 评估使用61和67的测量应用潜力.
主要方法:
- 合成四个NODAGA结合的卡利奥斯配体.
- 使用61CuCl的放射性标记可以快速 (5分钟) 达到高产量和纯度.
- 在体外评估放射性链体的亲和力,内化和细胞吸收.
- 在瘤模型中的PET/CT成像和生物分布研究.
主要成果:
- 用61Cu有效标记卡利奥斯配体,显示出高水友性和FAP亲和力.
- 放射性链体被FAP阳性细胞内化
- 在注射后1小时和4小时,PET/ CT成像显示瘤累积.
- 由于正常的组织洗,Cu-Kalios-02在4小时后显示出稳定的瘤吸收率和改善的瘤背景比率.
结论:
- 卡利奥斯代表了一种新型的 Cu-标记的 FAP 向型放射性链体.
- 的更长的半衰期使得有效的延迟成像 (每日4小时) 通过增强的瘤可视化.
- 当与Cu67配对时,这些标记为Cu61的放射性质体具有显著的临床转化和治疗潜力.
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