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EDO-1-116

Development stage: Preclinical
Lead developer: Georgetown University
Modality: Small Molecules

Overview

EDO-1-116 is a small molecule 4-aminopyrimidine derivative and an analog of the compound A9 (2,6-dibenzyl-5-phenylpyrimidin-4-amine). It was developed as a BRCA1-mimetic drug designed to inhibit estrogen receptor 1 (ER-1, also known as estrogen receptor alpha or ER-alpha) activity. By mimicking the tumor suppressor function of BRCA1, which naturally represses ER-1 activity, EDO-1-116 blocks estrogen-stimulated gene expression and cell proliferation. In preclinical studies, EDO-1-116 demonstrated an IC50 of 5 µM for inhibiting estrogen-dependent transcriptional activity, making it a potential therapeutic candidate for the treatment of breast cancer.

Other names: 4-(beta-naphthyl) A9 analog4-(β-naphthyl) A9 analog

Targets

ESR1 (ERα)

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