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加-68标记的正子发射计算机断层扫描标记器准高对比度的Glypican-3,用于肝细胞癌成像

Zhongjing Li¹, Chunwei Mo², Chengzhe Li¹

¹Department of Nuclear Medicine, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital & Shenzhen Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Shenzhen 518116, China.

ACS pharmacology & translational science

|December 19, 2024

概括

针对Glypican-3 (GPC3) 的新型Gallium-68标记探针显示,它有望用于检测肝细胞癌 (HCC). 该探针68Ga-ALB-GBP,与目前的方法相比,提供了改进的瘤可视化.

科学领域:

核医学就是核医学.
在瘤学瘤学.
放射化学放射化学是指辐射化学.

背景情况:

由于早期,非侵入性诊断方法的局限性,肝细胞癌 (HCC) 的检测仍然具有挑战性.
Glypican-3 (GPC3) 在HCC中显著过度表达,使其成为向成像的有希望的生物标志物.
开发有效的成像探针对于改善HCC诊断和患者治疗结果至关重要.

研究的目的:

开发和评估新的68Ga标记正子发射断层扫描 (PET) 探针,针对GPC3检测HCC.
为了比较GPC3向探针与蛋白结合部分 (68Ga-ALB-GBP) 的有效性,与用聚乙烯糖醇 (PEG) (68Ga-PEG2-GBP) 的探针进行比较.
在临床前的HCC模型中评估68Ga-ALB-GBP的诊断潜力.

主要方法:

两个68Ga标记的GPC3向PET探针的合成和特征:68Ga-PEG2-GBP和68Ga-ALB-GBP.
在皮下和正体HCC小鼠模型中使用微PET/计算机断层扫描 (CT) 进行体内评估.
对探针稳定性,瘤吸收,瘤与肝脏的比率以及瘤与肌肉的比率进行比较分析.

主要成果:

与68Ga-PEG2-GBP相比,68Ga-ALB-GBP在体内表现出更好的稳定性,更高的瘤吸收率,以及改善的瘤-肝脏比率.
在 орто型HCC模型中,68Ga-ALB-GBP在注射后3小时实现了2.29的瘤与肝脏的比率和13.03的瘤与肌肉的比率.
在临床前环境中,68Ga-ALB-GBP的性能超过了临床使用的18F-氧糖 (FDG) PET成像.

结论:

68Ga-ALB-GBP是一种非常有前途的PET追踪器,用于非侵入性HCC检测,显示增强的瘤可视化.
加入一个结合白蛋白的部分显著改善了标记剂的药理动力学,导致高对比度成像.
68Ga-ALB-GBP具有作为诊断工具的临床转化潜力,并可能用于HCC的治疗应用.

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