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一个新的基于的PD-L1PET追踪器:设计,合成和临床前成像验证

Meilian Zhang^1,2, Ye Dong¹, Chunwei Mo¹

¹GDMPA Key Laboratory for Quality Control and Evaluation of Radiopharmaceuticals, Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, Guangdong 510515, China.

ACS medicinal chemistry letters

|January 14, 2026

概括

研究人员开发了一种新的PET成像探针,[18F]-AlF-Asp2-TPP-1,以可视化瘤中的编程死亡联体1 (PD-L1) 表达. 这种新型药物通过使PD-L1的非侵入性检测成为指导免疫治疗的前景.

科学领域:

核医学是一种核医学.
放射化学放射化学是指辐射化学.
在瘤学瘤学.

背景情况:

编程死亡连接体1 (PD-L1) 是一种关键的免疫检查点蛋白,在各种瘤细胞上表达.
准确评估PD-L1表达对于预测PD-1/PD-L1向免疫疗法的反应至关重要.

研究的目的:

开发和评估一种新的正子发射断层扫描 (PET) 成像探针[18F]-AlF-Asp2-TPP-1,用于非侵入性可视化PD-L1表达.
评估使用该探针指导PD-L1向癌症免疫治疗的可行性.

主要方法:

新型PET探头[18F]-AlF-Asp2-TPP-1的合成和特征.
放射性追踪物的体外和体内稳定性研究.
在携带瘤的模型中进行动态PET成像,以评估标志物吸收和生物分布.

主要成果:

探测器[18F]-AlF-Asp2-TPP-1的合成具有高放射性化学产量 (13.7%) 和纯度 (>95%).
证实了出色的体外和体内稳定性.
在瘤中观察到快速的标记剂积累,在注射后的30,60和90分钟内显著的瘤吸收.

结论:

[18F]-AlF-Asp2-TPP-1作为PD-L1表达的PET成像剂表现出有利的特性.
这种新型探测器有可能用于对瘤中PD-L1水平的非侵入性监测.
它可以作为一个有价值的工具来指导患者选择PD-L1向免疫治疗.

关键词:

在PD-L1中.聚乙烯/聚乙烯/聚乙烯太阳能发电厂-1 的建设.瘤成像成像瘤成像 [18F]AlF标签的使用

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