Drug intelligence / Profile preview

estrogen receptor beta inhibitor + EGFR inhibitor

Development stage
Preclinical
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Oral, Intramuscular
01

Overview

This refers to a combination therapy consisting of an estrogen receptor beta (ERβ) inhibitor and an epidermal growth factor receptor (EGFR) inhibitor. The rationale for this combination is based on evidence that cross-talk between ERβ and EGFR signaling pathways contributes to cancer cell proliferation, survival, and resistance mechanisms—particularly in non-small cell lung cancer (NSCLC). Preclinical studies have shown that combining an ERβ inhibitor such as fulvestrant with an EGFR tyrosine kinase inhibitor like erlotinib or gefitinib can synergistically inhibit tumor growth, induce apoptosis, and overcome acquired resistance to EGFR inhibitors. This dual-targeted approach aims to maximize anti-tumor efficacy by simultaneously blocking two critical pathways involved in tumor progression and drug resistance[1][2][3].

02

Targets

ESR2 (ERβ)

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