Target intelligence / Profile preview

Epidermal Growth Factor Receptor Exon 20 Mutant (EGFR Exon 20 Mutant)

Target
EGFR Exon 20 Mutant
Molecular classification
Receptor Tyrosine Kinase, Transmembrane Receptor
01

Overview

The EGFR Exon 20 mutant represents a clinically significant subset characterized by unique structural changes that drive oncogenesis while conferring substantial therapeutic challenges due to inherent drug resistance properties. Exon 20 mutations occur within the region encoding part of the kinase domain and are frequently associated with acquired resistance to EGFR tyrosine kinase inhibitors. These mutations lead to persistent activation even without ligand stimulation, promoting tumorigenesis through unchecked proliferation.

Other names
EGFR Exon 20 insertionEGFR Exon 20 mutationsEGFR Exon 20 SNVs
02

Mechanism of action

Inhibition of EGFR tyrosine kinase activity, disruption of downstream signaling pathways (MAPK, PI3K/AKT, JNK)

03

Biological functions

Cell proliferationCell survivalCell differentiationCell migrationSignal transduction
04

Disease associations

CancerNon-Small Cell Lung Cancer (NSCLC)
05

Safety considerations

Drug resistancePoor response to first/second-generation TKIsMulti-drug resistance in compound mutations
06

Interacting drugs

First-generation EGFR TKIs (e.g., Gefitinib, Erlotinib)

5 more in the full profile.

07

Biomarkers

EGFR Exon 20 insertion mutationsEGFR Exon 20 SNVs (e.g., T790M, S768I, C797S)T790M/L858RT790M/C797X

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