Annotation Detail

Information
Associated Genes
EGFR
Associated Variants
EGFR p.Leu858Arg (p.L858R) ( ENST00000275493.7, ENST00000450046.2, ENST00000455089.5 )
EGFR p.Leu858Arg (p.L858R) ( ENST00000275493.7, ENST00000450046.2, ENST00000455089.5 )
Associated Disease
lung non-small cell carcinoma
Source Database
CIViC Evidence
Description
In an in vitro study using NCI-H1781 cells (EGFR wild-type) and NCI-H3255 cells (EGFR L858R), inhibition of cell growth was used as an assay to determine sensitivity to irreversible tyrosine kinase inhibitor (TKI) drugs. Cells with an EGFR L858R mutation demonstrated an improved response to neratinib (IC50: 0.0049umol/L vs. 0.085umol/L) compared to wildtype EGFR cells or compared to reversible TKI drug erlotinib (IC50: 0.031umol/L vs. wildtype >1umol/L).
Variant Origin
somatic
Variant Origin
Somatic
Evidence URL
https://civic.genome.wustl.edu/links/evidence_items/2628
Gene URL
https://civic.genome.wustl.edu/links/genes/19
Variant URL
https://civic.genome.wustl.edu/links/variants/33
Evidence Type
Predictive
Disease
Lung Non-small Cell Carcinoma
Evidence Direction
Supports
Drug
Neratinib
Evidence Level
D
Clinical Significance
Sensitivity/Response
Pubmed
16818618
Drugs
Drug NameSensitivitySupported
NeratinibSensitivitytrue