Target intelligence / Profile preview

Epidermal Growth Factor Receptor Mutant Form 8 (EGFRvIII)

Target
EGFRvIII
Molecular classification
Receptor Tyrosine Kinase, Receptor, Growth Factor Receptor
01

Overview

Epidermal growth factor receptor mutant form 8 (EGFRvIII) is a specific mutant variant of the epidermal growth factor receptor (EGFR). It results from an in-frame deletion of exons 2–7 in the extracellular domain of the EGFR gene. This deletion leads to a truncated protein lacking part of its ligand-binding domain but retaining constitutive kinase activity, causing persistent activation of downstream signaling pathways and promoting uncontrolled cell proliferation, survival, migration, and tumorigenesis. It is most commonly found in glioblastoma multiforme (GBM) and is an attractive target for cancer therapies.

Other names
EGFR variant IIIEGFR deletion mutant (exons 2-7 deletion)
02

Mechanism of action

Constitutive activation of downstream signaling pathways (RAS/RAF/MEK/ERK MAPK and PI3K/AKT/mTOR) due to ligand-independent kinase activity.

03

Biological functions

Cell proliferationCell survivalTumorigenesisSignal transduction
04

Disease associations

CancerGlioblastoma MultiformeNon-Small Cell Lung Cancer
05

Safety considerations

On-target, off-tumor toxicity (potential for affecting normal EGFR signaling)Immune-related adverse events (for CAR-T therapies)Resistance development
06

Interacting drugs

Monoclonal antibodies targeting EGFRvIII

2 more in the full profile.

07

Biomarkers

EGFRvIII expression in tumor tissueEGFR gene amplification

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