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Target intelligence / Profile preview
Epidermal Growth Factor Receptor Tyrosine Kinase (mutant) (EGFR-TKI)
- Target
- EGFR-TKI
- Molecular classification
- Receptor tyrosine kinases, ErbB/HER receptor tyrosine kinases, Transmembrane protein
01
Overview
The epidermal growth factor receptor (EGFR) is a transmembrane protein and member of the ErbB family of receptor tyrosine kinases. Somatic mutations that hyperactivate the EGFR tyrosine kinase domain are particularly associated with non-small cell lung cancer (NSCLC), colorectal cancer, and glioblastoma multiforme. EGFR-TKIs are small molecules designed to inhibit the aberrant kinase activity resulting from these mutations.
- Other names
- EGFR (mutant)Mutant EGFREGFR tyrosine kinase (mutant)
02
Mechanism of action
Tyrosine kinase inhibition
03
Biological functions
Cell proliferationCell survivalCell migrationCell differentiationSignal transduction
04
Disease associations
Cancer
05
Safety considerations
Primary/intrinsic resistanceAcquired/secondary resistanceToxicity associated with broad inhibition profiles (e.g., second-generation TKIs)
06
Interacting drugs
4 more in the full profile.
07
Biomarkers
Exon 19 deletionsExon 21 L858R substitutionT790M mutationC797S mutationBIM deletion polymorphism
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