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探索两种代谢稳定的GRPR向的酸标记Ga-68用于PET成像的治疗潜力

Karim Obeid¹, Ekaterina Bezverkhniaia¹, Vladimir Tolmachev²

¹Department of Medicinal Chemistry, Uppsala University, 751 83, Uppsala, Sweden.

EJNMMI radiopharmacy and chemistry

|February 17, 2026

概括

新的PET标记物[68Ga]Ga-PKB2和[68Ga]Ga-PKB3对胃素释放受体 (GRPR) 具有很高的亲和力,并能够清晰地对GRPR阳性瘤进行成像. 这些标记物是针对性放射性核素治疗的有前途的诊断工具.

科学领域:

核医学是一种核医学.
放射性药物化学放射性药物化学
在瘤学瘤学.

背景情况:

胃释放受体 (GRPR) 是放射性应用的关键标.
之前开发的以177Lu标记的代谢稳定的GRPR向 (PKB2,PKB3) 显示了治疗潜力.

研究的目的:

为了评估PKB2和PKB3的诊断对应物,使用68Ga进行PET成像.
为了评估177Lu/68Ga对对GRPR向应用的theranostic潜力.

主要方法:

用68Ga.标记PKB2和PKB3的放射性标记.
在体外评估GRPR亲和力和PC-3细胞中的细胞吸收.
在PC-3异种移植和PET/CT成像中的体内生物分布研究.

主要成果:

[68Ga]Ga-PKB2和[68Ga]Ga-PKB3的放射性化学产量 (>99%) 和纯度 (>97%) 高.
这两种标记物都表现出低纳米GRPR亲和力和PC-3细胞中GRPR介导的吸收.
快速的血液清除 (下午2小时<0.5%IA/g) 在PC-3异种移植中具有高瘤吸收率 (16-17%IA/g).
与[68Ga]Ga-PKB2.2相比,[68Ga]Ga-PKB3显示胰腺和下脏吸收率更高.
PET/CT成像清楚地划分了瘤,并与生物分布相关联.

结论:

[68Ga]Ga-PKB2和[68Ga]Ga-PKB3是用于成像GRPR阳性瘤的有效PET追踪剂.
这些标记剂作为有前途的诊断对象,他们的177Lu标记的同类.
177Lu/68Ga对支持GRPR向癌症管理的治疗应用.

关键词:

68GaGa 68GaGaGa 68GaGa 68GaGa 68GaGa 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 68Ga 炸弹中的炸弹这就是为什么GRPR是GRPR.图像成像是一种成像.在这里,PET是PET.前列腺癌是什么意思前列腺癌是什么意思放射性药物放射性药物放射性药物

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