Target intelligence / Profile preview

Estrogen receptor and Human epidermal growth factor receptor 2 (ER/HER2)

Target
ER/HER2
Molecular classification
Receptor, Transcription factor, Enzyme
01

Overview

The Estrogen Receptor (ER) and Human Epidermal Growth Factor Receptor 2 (HER2) are pivotal therapeutic targets}

Other names
ER/HER2 axisESR1/ERBB2Hormone receptor and HER2HR+/HER2+ signaling axis
02

Mechanism of action

Fulvestrant acts as a selective estrogen receptor degrader (SERD) that binds to the estrogen receptor (ER), inhibiting its transcriptional activity and promoting its degradation [12]. Trastuzumab is a monoclonal antibody that targets the extracellular domain of the human epidermal growth factor receptor 2 (HER2), blocking its homodimerization and heterodimerization, inhibiting downstream PI3K/AKT and MAPK signaling pathways, and mediating antibody-dependent cellular cytotoxicity (ADCC) [3, 4]. The combination of these agents simultaneously blocks the ER and HER2 signaling pathways, which frequently exhibit crosstalk leading to therapeutic resistance [1, 2].

03

Biological functions

Signal transductionCell cycleApoptosisCell proliferation
04

Disease associations

Cancer
05

Safety considerations

CardiotoxicityInjection site reactionsHot flashesFatigueGastrointestinal toxicity
06

Interacting drugs

Fulvestrant

7 more in the full profile.

07

Biomarkers

Estrogen receptor (ER) expressionHER2 overexpressionHER2 amplificationPIK3CA mutationMED1 expression

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