Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research, Kobe, Hyogo, Japan; Novel PET Diagnostics Laboratory, RIKEN Innovation Center (RINC), Hyogo, Japan.
Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research, Kobe, Hyogo, Japan.
Biochem Biophys Res Commun. 2022 Mar 12;596:83-87. doi: 10.1016/j.bbrc.2022.01.099. Epub 2022 Jan 29.
In the first-in-human PET study, we evaluated the biodistribution and tumor accumulation of the novel PET probe, (S)-2-amino-3-[3-(2-F-fluoroethoxy)-4-iodophenyl]-2-methylpropanoic acid (F-FIMP), which targets the tumor-related L-type amino acid transporter 1 (LAT1), and compared it with L-[methyl-C]methionine (C-MET) and 2-Deoxy-2-F-fluoro-D-glucose (F-FDG). F-FIMP biodistribution was revealed by whole-body and brain scans in 13 healthy controls. Tumor accumulation of F-FIMP was evaluated in 7 patients with a brain tumor, and compared with those of C-MET and F-FDG. None of the subjects had significant problems due to probe administration, such as adverse effects or abnormal vital signs. F-FIMP was rapidly excreted from the kidneys to the urinary bladder. There was no characteristic physiological accumulation in healthy controls. F-FIMP PET resulted in extremely clear images in patients with suspected glioblastoma compared with C-MET and F-FDG. F-FIMP could be a useful novel PET probe for LAT1-positive tumor imaging including glioblastoma.
在首例人体 PET 研究中，我们评估了新型 PET 探针（S）-2-氨基-3-[3-（2-氟乙氧基）-4-碘苯基]-2-甲基丙氨酸（F-FIMP）的生物分布和肿瘤积累情况，该探针靶向与肿瘤相关的 L 型氨基酸转运蛋白 1（LAT1），并将其与 L-[甲基-C]蛋氨酸（C-MET）和 2-脱氧-2-氟-D-葡萄糖（F-FDG）进行了比较。F-FIMP 的全身和脑部扫描揭示了其在 13 名健康对照者中的分布情况。我们评估了 7 名脑肿瘤患者中 F-FIMP 的肿瘤积累情况，并将其与 C-MET 和 F-FDG 进行了比较。所有受试者均无因探针给药引起的明显问题，如不良反应或生命体征异常。F-FIMP 从肾脏迅速排泄到膀胱。在健康对照者中没有特征性的生理性积累。与 C-MET 和 F-FDG 相比，F-FIMP PET 在疑似胶质母细胞瘤患者中产生了极为清晰的图像。F-FIMP 可能是一种用于 LAT1 阳性肿瘤成像的有用的新型 PET 探针，包括胶质母细胞瘤。
