¹⁸F-Labeled brain-penetrant EGFR tyrosine kinase inhibitors for PET imaging of glioblastoma.

ABSTRACT: Significant evidence suggests that the failure of clinically tested epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (e.g. erlotinib, lapatinib, gefitinib) in glioblastoma (GBM) patients is primarily attributed to insufficient brain penetration, resulting in inadequate exposure to the targeted cells. Molecular imaging tools can facilitate GBM drug development by visualizing drug biodistribution and confirming target expression and localization. To assess brain exposure via PET molecular imaging, we synthesized fluorine-18 isotopologues of two brain-penetrant EGFR tyrosine kinase inhibitors developed specifically for GBM. Adapting our recently reported radiofluorination of N-arylsydnones, we constructed an ortho-disubstituted [¹⁸F]flu

SUBMITTER: Narayanam MK 

PROVIDER: S-EPMC10699577 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature