First-in-human assessment of the novel LAT1 targeting PET probe 18F-FIMP

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.

Automated summary

In this first-in-human PET study, the biodistribution and tumor accumulation of a novel PET probe, F-18-FIMP, were evaluated. The results showed rapid excretion of F-18-FIMP from the kidneys and no characteristic physiological accumulation in healthy controls. Compared with other probes, F-18-FIMP provided clearer imaging in patients with brain tumors.