Purpose

Boramino acids are a class of amino acid biomimics that replace the carboxylate group with trifluoroborate and can achieve the ¹⁸F-labeled positron emission tomography (PET) and boron neutron capture therapy (BNCT) with identical chemical structure.

Methods

This study reports a trifluoroborate-derived boronophenylalanine (BBPA), a derived boronophenylalanine (BPA) for BNCT, as a promising PET tracer for tumor imaging.

Results

Competition inhibition assays in cancer cells suggested the cell accumulation of [¹⁸F]BBPA is through large neutral amino acid transporter type-1 (LAT-1). Of note, [¹⁸F]BBPA is a pan-cancer probe that shows notable tumor uptake in B16-F10 tumor-bearing mice. In the patients with gliomas and metastatic brain tumors, [¹⁸F]BBPA-PET shows good tumor uptake and notable tumor-to-normal brain ratio (T/N ratio, 18.7 ± 5.5, n = 11), higher than common amino acid PET tracers. The [¹⁸F]BBPA-PET quantitative parameters exhibited no difference in diverse contrast-enhanced status (P = 0.115–0.687) suggesting the [¹⁸F]BBPA uptake was independent from MRI contrast-enhancement.

Conclusion

This study outlines a clinical trial with [¹⁸F]BBPA to achieve higher tumor-specific accumulation for PET, provides a potential technique for brain tumor diagnosis, and might facilitate the BNCT of brain tumors.

中文翻译：

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用于脑肿瘤诊断的双硼硼氨基酸 PET 示踪剂

目的

硼氨基酸是一类用三氟硼酸盐取代羧酸盐基团的氨基酸仿生体，可以实现具有相同化学结构的¹⁸ F标记正电子发射断层扫描（PET）和硼中子捕获治疗（BNCT）。

方法

这项研究报道了一种三氟硼酸衍生的硼苯丙氨酸 (BBPA)，一种用于 BNCT 的硼苯丙氨酸衍生 (BPA)，作为一种有前途的肿瘤成像 PET 示踪剂。

结果

癌细胞中的竞争抑制测定表明，[ ¹⁸ F]BBPA 的细胞积累是通过大型中性氨基酸转运蛋白 1 型 (LAT-1) 进行的。值得注意的是，[ ¹⁸ F]BBPA 是一种泛癌探针，在 B16-F10 荷瘤小鼠中显示出显着的肿瘤摄取。在胶质瘤和转移性脑肿瘤患者中，[ ¹⁸ F]BBPA-PET 显示出良好的肿瘤摄取和显着的肿瘤与正常脑的比率（T/N 比率，18.7 ± 5.5，n = 11），高于普通氨基酸PET 示踪剂。[ ¹⁸ F]BBPA-PET 定量参数在不同的对比增强状态下没有表现出差异（P = 0.115–0.687），表明[ ¹⁸ F]BBPA 摄取与 MRI 对比增强无关。

结论

^{这项研究概述了一项使用[ 18} F]BBPA进行的临床试验，以实现 PET 更高的肿瘤特异性积累，为脑肿瘤诊断提供了一种潜在的技术，并可能促进脑肿瘤的 BNCT。