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一个基于TCO-Tetrazine的生物直角预定向PET/NIRF平台,可实现高对比度瘤成像

Mingxing Huang¹, Weichen Wang¹, Qiao Yu¹

¹Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu 610017, China.

Pharmaceuticals (Basel, Switzerland)

|December 31, 2025

概括

使用DZ-Lys-TCO和68Ga-DOTA-H-Tz的基于DZ-1的新型预定目标系统展示了高对比度瘤成像. 这种优化的48小时预定位间隔为精确和安全的放射性药物应用提供了一个有前途的平台.

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.
分子成像学分子成像学

背景情况:

预向策略通过将瘤向与放射性核素输送脱,提高放射性药物特异性和安全性.
直接标记的小分子面临着快速清除和全身暴露的挑战.
开发了一个基于DZ-1的预定向系统,以利用广谱瘤定向能力.

研究的目的:

合成和评估用于预定向成像的新型DZ-TCO前体.
为预定目标应用开发和评估68Ga标记的四素探针.
使用PET成像优化预定向间隔,以增强使用PET成像的瘤可视化.

主要方法:

三种DZ-TCO前体 (DZ-1-TCO,DZ-Lys-TCO,DZ-Lys-PEG4-TCO) 的合成 .
使用近红外光成像对具有瘤的小鼠进行前体的评估.
用68Ga对四素探针进行放射标记,并评估其稳定性.
预定向PET成像使用各种前体/探头组合和预定向间隔 (24,48,72小时).

主要成果:

所有前体都显示瘤积累和信号保留.
68Ga标记的氨酸探针表现出高放射性化学稳定性 (>4小时后85%).
在48小时间隔内与68Ga-DOTA-H-Tz结合的DZ-Lys-TCO产生了最佳的瘤吸收率 (3.24 ± 0.95%ID/g) 和瘤与肌肉的比率 (8.30 ± 3.39).

结论:

DZ-TCO/68Ga-DOTA-Tz预定位系统实现了低背景高对比度瘤成像.
在48小时内,DZ-Lys-TCO和68Ga-DOTA-H-Tz的优化组合提供了卓越的性能.
该系统为精确和安全的放射性药物成像和治疗提供了一个有前途的平台.

关键词:

在PET成像中使用PET成像.生物对等化学的化学预定目标的预定目标.放射性药物制品放射性药物制品

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