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

• Published in: Biochemical and biophysical research communications Vol. 596; pp. 83 - 87
• Main Authors: Nozaki, Satoshi, Nakatani, Yuka, Mawatari, Aya, Hume, William E., Wada, Yasuhiro, Ishii, Akira, Tanaka, Masaaki, Tsuyuguchi, Naohiro, Doi, Hisashi, Watanabe, Yasuyoshi
• Format: Journal Article
• Language: English
• Published: Elsevier Inc 12.03.2022
• Subjects: Amino acid transporter; Brain tumor; First-in-human study; LAT1; Positron emission tomography (PET); Brain tumor; First-in-human study; Amino acid transporter; LAT1; Positron emission tomography (PET)
• ISSN: 0006-291X; 1090-2104
• DOI: 10.1016/j.bbrc.2022.01.099

In the first-in-human PET study, we evaluated the biodistribution and tumor accumulation of the novel PET probe, (S)-2-amino-3-[3-(2-18F-fluoroethoxy)-4-iodophenyl]-2-methylpropanoic acid (18F-FIMP), which targets the tumor-related L-type amino acid transporter 1 (LAT1), and compared it with L-[methyl-11C]methionine (11C-MET) and 2-Deoxy-2-18F-fluoro-D-glucose (18F-FDG). 18F-FIMP biodistribution was revealed by whole-body and brain scans in 13 healthy controls. Tumor accumulation of 18F-FIMP was evaluated in 7 patients with a brain tumor, and compared with those of 11C-MET and 18F-FDG. None of the subjects had significant problems due to probe administration, such as adverse effects or abnormal vital signs. 18F-FIMP was rapidly excreted from the kidneys to the urinary bladder. There was no characteristic physiological accumulation in healthy controls. 18F-FIMP PET resulted in extremely clear images in patients with suspected glioblastoma compared with 11C-MET and 18F-FDG. 18F-FIMP could be a useful novel PET probe for LAT1-positive tumor imaging including glioblastoma. •The biodistribution and tumor accumulation of 18F-FIMP targeting the tumor-related L-type amino acid transporter 1 (LAT1).•18F-FIMP was no characteristic physiological accumulation in healthy controls.•18F-FIMP PET resulted in extremely clear images in patients with suspected glioblastoma compared with 11C-MET and 18F-FDG.