Drug intelligence / Profile preview

18F-afatinib

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]afatinib is a fluorine-18-radiolabeled positron emission tomography (PET) imaging tracer derived from afatinib, a second-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Developed at the Vrije Universiteit Medisch Centrum (VUmc) with support from Boehringer Ingelheim, this radiotracer is designed to non-invasively visualize and quantify EGFR expression and mutation status in patients with non-small cell lung cancer (NSCLC). By irreversibly binding to the kinase domain of EGFR, [18F]afatinib uptake serves as a predictive biomarker to identify tumors harboring activating EGFR mutations (such as exon 19 deletions or L858R) and to select patients most likely to benefit from therapeutic afatinib treatment.

Other names
fluorine-18-afatinibfluorine18-afatinibfluorine 18-afatinib[18F]-afatinib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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