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临床前评估和首次对人体PET研究Al18F-标记双基二二烯基PSMA标记剂

Yimin Chen¹, Ming Ni², Xiaojun Zhang³

¹Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.

Journal of medicinal chemistry

|March 10, 2025

概括

一种新的[18F]AlF-PSMA-N5标记物显示出前列腺癌 (PCa) 成像的前景. 这种二维PSMA标记器提供了更好的成像质量和减少非目标组织的吸收,有助于准确的诊断和分期.

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:

前列腺特异性膜抗原 (PSMA) 是前列腺癌 (PCa) 诊断和治疗的关键目标.
开发新型放射性追踪剂对于提高PCa成像效率至关重要.

研究的目的:

开发和评估一种新的[18F]AlF标记的二维PSMA追踪器,[18F]AlF-PSMA-N5,用于增强PCa成像.
评估[18F]AlF-PSMA-N5.5的结合亲和力,体外和体内表现.

主要方法:

合成和评估七个基于双基的联体,用于PSMA结合亲和力.
在22Rv1瘤携带小鼠体内研究,以评估瘤吸收和向.
在PCa患者中进行初步首次人体研究,以评估诊断性能.

主要成果:

[18F]AlF-PSMA-N5表现出高的PSMA亲和力 (Ki = 0.31 ± 0.06nM) 和良好的放射性化学产量 (25.6% ± 6.6%).
在体内研究显示高瘤吸收率 (SUVmax = 3.15) 和瘤与肌肉的比率 (T/M = 22.57).
人类研究证实了PCa病变的成功识别,与[68Ga]Ga-PSMA-11相比,具有优异的对比度和T/M比率,与[18F]DCFPyL相比,结果相似.

结论:

[18F]AlF-PSMA-N5是PCa成像中的一个有前途的PET放射追踪器.
追踪器提供更好的成像质量和减少非特异性吸收,提高诊断准确度.

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