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Updated: Jun 29, 2025

An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use

An Automated Radiosynthesis of [⁶⁸Ga]Ga-FAPI-46 for Routine Clinical Use

Published on: May 24, 2024

一种新型FAPI二元体的临床翻译 [⁶⁸Ga]Ga-LNC1013

Yue Tan¹, Jian Li², Tianzhi Zhao^1,3,4

¹Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore.

European journal of nuclear medicine and molecular imaging

|April 1, 2024

概括

纤维细胞激活蛋白抑制剂 (FAPI) 被二元化以增强瘤吸收和保留用于癌症成像. 化合物Ga-LNC1013在试验性临床研究中显示出卓越的诊断潜力.

科学领域:

在瘤学瘤学.
放射化学放射化学是指辐射化学.
核医学就是核医学.

背景情况:

纤维细胞激活蛋白 (FAP) 是癌症成像和治疗的关键目标.
目前正在开发FAPI抑制剂 (FAPI) 用于诊断和治疗应用.
FAPI二极体为改善瘤向和保留提供了潜力.

研究的目的:

设计和合成新的FAPI二次元.
为了评估FAPI二元体的体外和体内性能.
在一项试点临床PET成像研究中,评估领先的FAPI二聚体,Ga-LNC1013.

主要方法:

合成了三种具有不同链接器的新型FAPI同分体.
在体外结合亲和度测试和临床前小动物PET成像.
在七名胃肠道癌症患者中进行试点临床PET成像研究.

主要成果:

合成的FAPI二元体表现出高的结合亲和力和特异性.
[⁶⁸Ga]Ga-LNC1013与单体和其他二元体相比,显示出优异的瘤吸收和保留.
临床PET成像显示了突出的瘤吸收和Ga-LNC1013的良好对比,在特定癌症中表现优于F-FDG.

结论:

FAPI二分化是一种有效的策略,可以增强瘤向和保留.
与单体FAPI和F-FDG相比,Ga-LNC1013显示出更高的诊断潜力.
在未来,LNC1013对FAP阳性癌症的放射性连接体治疗具有前途.

关键词:

68GaGa 68GaGa 的时间变质化变质化 (Dimerization Dimerization) 是一种变质化的过程.纤维细胞激活蛋白 (FAP) 是一种激活蛋白.在PET成像中使用PET成像.皮佩拉津 (Piperazine) 是一种药物.

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