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以结构为导向的设计和Ga-GP01的临床评估,用于固体瘤中针对FAP的PET成像
Xingyu Mu1, Zihao Chen2, Hoi Yee Chow3
1Department of Nuclear Medicine, The First Affiliated Hospital, Guilin Medical University, Guilin 541001, China.
概括
一种新型的放射性追踪剂68Ga-GP01在表达纤维细胞激活蛋白 (FAP) 的癌症中,与68Ga-FAPI-46相比,显示出更高的稳定性和瘤检测能力. 临床试验显示了针对FAP的PET成像的有希望的结果.
科学领域:
- 核医学是一种核医学.
- 在瘤学瘤学.
- 放射化学 放射化学是指辐射化学.
背景情况:
- 纤维细胞激活蛋白 (FAP) 向的放射性连接体对检测表达FAP的癌症有效.
- 基诺林制剂68Ga-FAPI-46在体内稳定性和药理动力学上有局限性.
研究的目的:
- 设计和评估一种新的针对FAP的放射性连体68Ga-GP01,其性能比68Ga-FAPI-46.6有所改善.
- 评估68Ga-GP01在临床前瘤模型和固体瘤临床试验中的诊断性能.
主要方法:
- 通过修改FAPI-46以N-甲基-硫酸侧链合成GP01.
- 进行了体外测定,瘤模型中的体内PET/CT成像和35名患者的临床评估.
- 与18F-FDG进行了直接比较.
主要成果:
- 68Ga-GP01具有高放射性化学纯度,在体外稳定性优异,并且与FAP有特定的结合.
- 临床前研究表明,与68Ga-FAPI-46相比,瘤与背景比率有所改善,吸收,内化和流出速度较慢.
- 临床评估表明了最佳的药理动力学,持续的目标参与,有前途的病变检测和低有效剂量.
- 68Ga-GP01检测到比18F-FDG更多的病变,吸收率和瘤与背景比率更高.
结论:
- 68Ga-GP01是一种临床翻译的FAP向PET追踪器,其性能优于68Ga-FAPI-46.
- 它增强或超越代谢成像的能力,需要在肌肉成像应用中进一步研究.
- 68Ga-GP01显示出作为FAP阳性固体瘤瘤学中的一个有价值的工具的潜力.
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