First-in-human assessment of the novel LAT1 targeting PET probe 18F-FIMP
First-in-human assessment of the novel LAT1 targeting PET probe 18F-FIMP
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DOI：
10.1016/j.bbrc.2022.01.099
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发表时间：
2022-02-01
影响因子：
3.1
通讯作者：
Watanabe, Yasuyoshi
中科院分区：
文献类型：
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作者：
Nozaki, Satoshi;Nakatani, Yuka;Watanabe, Yasuyoshi
在首次人体正电子发射计算机断层扫描研究中，我们评估了新型正电子发射计算机断层扫描探针(S)-2-amino-3-[3-(2-F-18-fluoroethoxy)-4-iodophenyl]-2-methylpropanoic酸(F-18-FIMP)的生物分布和肿瘤蓄积，并将其与L[甲基-C-11]蛋氨酸(C-11-MET)和2-脱氧-2-F-18-氟-D-葡萄糖硒(F-18-FDG)进行了比较。通过全身扫描和脑扫描揭示F-18-FIMP在13名健康对照体内的生物分布。对7例脑肿瘤患者进行了F-18-FIMP的肿瘤蓄积评价，并与C-11-MET和F-18-FDG进行了比较。没有一名受试者因服用探针剂而出现明显问题，如不良反应或生命体征异常。F-18-FIMP从肾脏迅速排泄到膀胱。健康对照组未见典型的生理性蓄积。与C-11-MET和F-18-FDG相比，F-18-FIMP PET在可疑胶质母细胞瘤患者中获得了极其清晰的图像。F-18-FIMP有望成为包括胶质母细胞瘤在内的LAT1阳性肿瘤的一种有用的新型PET探针。(C)爱思唯尔公司出版的《2022年》。
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-18-fluoroethoxy)-4-iodophenyl]-2-methylpropanoic acid (F-18-FIMP), which targets the tumor-related L-type amino acid transporter 1 (LAT1), and compared it with L-[methyl-C-11] methionine (C-11-MET) and 2-Deoxy-2-F-18-fluoro-D-gluco se (F-18-FDG). F-18-FIMP biodistribution was revealed by whole-body and brain scans in 13 healthy controls. Tumor accumulation of F-18-FIMP was evaluated in 7 patients with a brain tumor, and compared with those of C-11-MET and F-18-FDG. None of the subjects had significant problems due to probe administration, such as adverse effects or abnormal vital signs. F-18-FIMP was rapidly excreted from the kidneys to the urinary bladder. There was no characteristic physiological accumulation in healthy controls. F-18-FIMP PET resulted in extremely clear images in patients with suspected glioblastoma compared with C-11-MET and F-18-FDG. F-18-FIMP could be a useful novel PET probe for LAT1-positive tumor imaging including glioblastoma. (C) 2022 Published by Elsevier Inc.