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[¹⁸F]BIBD-239:首个在人类中的PET放射追踪器,具有用于质瘤分类和心肌成像的双重诊断实用性

Xin Wang^1,2, Xiaotong Li^1,2, Wei Zheng²

¹Department of Nuclear Medicine, Beijing Tiantan Hospital, Capital Medical University, Beijing 100071, China.

Molecular pharmaceutics

|September 19, 2025

概括

新型放射追踪器BIBD-239在诊断心脏和大脑疾病方面表现有前途. 它表现出有效的脑透和心肌吸收,有助于质瘤分级和心血管成像.

科学领域:

放射化学和核医学放射化学和核医学
在瘤学瘤学.
心脏病学心脏病学

背景情况:

新型PET追踪剂的开发对于准确的疾病诊断至关重要.
转位蛋白 (TSPO) 是一种生物标志物,与各种神经和瘤疾病有关.
评估心脏和大脑疾病需要特定和敏感的成像剂.

研究的目的:

为了评估新型正子发射断层扫描 (PET) 追踪器的合成和首次在人体上应用[F]BIBD-239.
研究BIBD-239在诊断心脏和大脑疾病方面的潜力,特别是质瘤分级和心肌成像.
评估[¹⁸F]BIBD-239在人类中的安全性和药理动力学特征.

主要方法:

符合GMP的BIBD-239的自动合成.
在老鼠中进行临床前评估,以确认TSPO特异性结合.
这是首次对健康志愿者和患有高度质瘤 (HGG) 和低度质瘤 (LGG) 的患者进行人体研究.
对血脑屏障的透,正常的大脑保留,心肌吸收和瘤与背景比率的分析.
剂量测量评估和与FDG的比较.

主要成果:

在80±5分钟内成功合成了具有高放射性化学纯度 (>95%),产量 (>15%) 和摩尔活性 (>120 GBq/μmol) 的BIBD-239.
在人类研究中观察到快速的血脑屏障透和低的正常大脑保留.
在没有体内脱的情况下证明了高且持续的心肌吸收.
与LGG (2.33) 相比,HGG (3.09) 的瘤与背景比率更高,吸收范围超出了MRI增强区域.
全身有效剂量低于FDG.

结论:

[¹⁸F]BIBD-239表现出强大的合成,有利的药理动力学和特定的TSPO结合.
该标记器在非侵入性质瘤分级和葡萄糖独立心肌成像中具有双重实用性.
这些发现支持[¹⁸F]BIBD-239用于神经瘤学和心血管评估的翻译.

关键词:

在这里,PET是PET.在 TSPO TSPO 中.[18F]BIBD-23939 这是一本书.质瘤质瘤是一种肌肉心脏成像成像肌肉心脏成像

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