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链接器驱动的突破:设计一种新的链接器,以提高FAPI剪切器的升级性能

Hua Cheng^1,2, Liyan Bai^1,3,4, Xuwei Liu^1,3,4

¹Department of Nuclear Medicine, Fudan University Shanghai Cancer Center, Shanghai 200032, P. R. China.

Journal of medicinal chemistry

|December 5, 2025

概括

一种新的纤维细胞激活蛋白抑制剂 (FAPI) 三分剂,Ga/177Lu-DOTA-FAPI-FUSCC-Tri,增强瘤向和保留,以改善癌症成像和治疗.

科学领域:

在瘤学瘤学.
放射化学放射化学是指辐射化学.
分子成像学分子成像学

背景情况:

放射性标记的纤维细胞激活蛋白抑制剂 (FAPI) 对癌症诊断至关重要.
FAP剪切剂策略为提高FAPI疗效提供了潜在的可能性.
现有的FAPI探针在药理动力学概况方面存在局限性.

研究的目的:

为FAPI探测器设计和合成一种新型的三链接器.
开发和评估Lu-DOTA-FAPI-FUSCC-Tri用于诊断和治疗应用.
为了改善瘤向,吸收和保留基于FAPI的药物.

主要方法:

设计和合成一个新的三元链接器.
68 Ga/177 探测器的开发.Lu-DOTA-FAPI-FUSCC-Tri探测器的开发.
在临床前模型中系统评估探针的结合亲和力,瘤吸收和保留.

主要成果:

这种新型的FAP剪切剂表现出强烈的FAP结合亲和力 (0.621对3.5nM).
与单体相比,Lu-DOTA-FAPI-FUSCC-Tri证明了瘤吸收能力提高了3.5倍.
显著延长的瘤保留时间被观察到与三重体探针.

结论:

一个新的FAP剪切器连接器被确定并成功开发成一个高性能探测器.
⁶⁸Ga/¹⁷⁷Lu-DOTA-FAPI-FUSCC-Tri显示出作为FAP表达瘤的双重用途剂的承诺.
开发的FAP剪切剂比单体FAPI提供了更好的诊断和治疗潜力.

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