[18F]FEQA

[18F]FEQA is a fluorine-18 labeled irreversible tyrosine kinase inhibitor (TKI) developed as a positron emission tomography (PET) imaging agent to non-invasively quantify the density of Epidermal Growth Factor Receptor (EGFR) in tumors. Structurally based on the 4-anilinoquinazoline scaffold, [18F]FEQA features an acrylamide group at the 6-position which allows it to form a covalent bond with the Cys797 residue in the ATP-binding pocket of EGFR. This irreversible binding mechanism was designed to enhance the retention of the tracer in EGFR-overexpressing tissues, providing a clearer assessment of receptor expression compared to reversible tracers. It was primarily developed by Eyal Mishani's research group at Hadassah Hebrew University Hospital for potential applications in personalizing treatment for patients with EGFR-driven cancers, such as non-small cell lung cancer (NSCLC) and glioblastoma. However, like many early small-molecule EGFR PET probes, its clinical utility has been challenged by factors such as rapid metabolism and high non-specific binding in vivo.

Other names

N-{4-[(3'-[18F]fluoroethylphenyl)amino]-6-quinazolinyl} acrylamide[18F]N-{4-[(3'-fluoroethylphenyl)amino]-6-quinazolinyl} acrylamide18F-FEQA