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Target intelligence / Profile preview
Erb-B2 Receptor Tyrosine Kinase 2 (ERBB2)
- Target
- ERBB2
- Molecular classification
- Receptor Tyrosine Kinase, Tyrosine Kinase, RTK, ErbB Receptor Family
01
Overview
ERBB2 (Erb-B2 Receptor Tyrosine Kinase 2), also known as HER2, is a receptor tyrosine kinase that promotes cell proliferation and survival. Exon 20 insertion mutations, particularly in the kinase domain, lead to constitutive activation of the receptor, driving oncogenesis in various cancers, especially NSCLC. These mutations are predictive biomarkers for response to certain targeted therapies but also confer resistance to some TKIs, posing therapeutic challenges.
- Other names
- HER2neuHER-2/neuCD340
02
Mechanism of action
Tyrosine kinase inhibitor; Antibody-drug conjugate
03
Biological functions
Signal transductionCell proliferationCell survivalCell differentiation
04
Disease associations
CancerNon-small cell lung cancerBreast cancer
05
Safety considerations
Resistance to first-generation reversible TKIsAggressive tumor behaviorLimited response to conventional therapiesCardiotoxicityDiarrheaRash
06
Interacting drugs
Ado-trastuzumab emtansine
8 more in the full profile.
07
Biomarkers
ERBB2 exon 20 insertion mutationsY772_A775dupG776delinsVCG778_P780dupERBB2 amplification
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