Drug intelligence / Profile preview

EDO-1-112

Development stage
Preclinical
Lead developer
Georgetown University
Modality
Small Molecules
Administration
Oral
01

Overview

EDO-1-112 is a novel synthetic 4-aminopyrimidine and a symmetric analog of the compound A9 (2,6-dibenzyl-5-phenylpyrimidin-4-amine). Developed by researchers at Georgetown University, EDO-1-112 acts as a BRCA1-mimetic drug. It is designed to inhibit the activity of estrogen receptor-1 (ER-1, also known as estrogen receptor alpha), thereby blocking estrogen-stimulated gene expression and cell proliferation. EDO-1-112 has demonstrated potent in vitro activity against estrogen-dependent transcriptional activity with an IC50 of 2.5 uM and is being investigated as a potential therapeutic agent for the treatment of breast cancer.

Other names
2,6-bis(4-(pyridin-3-yl)benzyl)-5-(4-(pyridin-3-yl)phenyl)pyrimidin-4-amine4-(3-pyridinyl) A9 analog
02

Targets

ESR1 (ERα)

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