Target intelligence / Profile preview

Epidermal Growth Factor Receptor L858R Mutant (EGFR L858R)

Target
EGFR L858R
Molecular classification
Receptor, Tyrosine Kinase, Growth Factor Receptor
01

Overview

The Epidermal Growth Factor Receptor (EGFR) L858R mutant is an activating point mutation in the EGFR gene, where arginine (R) is substituted for leucine (L) at amino acid position 858. This mutation leads to constitutive activation of the receptor’s tyrosine kinase activity, promoting oncogenic signaling pathways associated with increased tumor growth and resistance to apoptosis. It is commonly found in non-small cell lung cancer (NSCLC), particularly adenocarcinoma subtypes. Patients with the L858R mutation respond well initially to first-generation tyrosine kinase inhibitors (TKIs), but resistance often develops.

Other names
EGFR L858R mutantEGFR-L858RL858R EGFREGFR (L858R)
02

Mechanism of action

Inhibition of EGFR tyrosine kinase activity

03

Biological functions

Cell proliferationSignal transductionCell survivalTyrosine kinase activity
04

Disease associations

CancerNon-small cell lung cancer (NSCLC)Adenocarcinoma
05

Safety considerations

Acquired resistance to tyrosine kinase inhibitors (TKIs)Lower sensitivity and shorter duration of response to TKIs compared to exon 19 deletionsDevelopment of secondary mutations (e.g., T790M)Disease progression
06

Interacting drugs

2 more in the full profile.

07

Biomarkers

EGFR L858R mutation statusT790M mutation status

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