Drug intelligence / Profile preview

SS5020

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

Overview

SS5020 is a novel benzopyran-based selective estrogen receptor modulator (SERM) and selective estrogen receptor downregulator (SERD) developed by researchers at Stony Brook University. It was designed as a safer alternative to tamoxifen for the treatment and prevention of breast cancer. Unlike tamoxifen, SS5020 does not exhibit genotoxic activity (it does not form DNA adducts) and lacks significant estrogenic/uterotrophic activity in the uterus, potentially reducing the risk of endometrial cancer. In preclinical models, SS5020 demonstrated potent antitumor activity against estrogen receptor (ER)-positive MCF-7 human breast cancer xenografts and DMBA-induced mammary tumors in rats, showing efficacy superior to tamoxifen and raloxifene.

Other names
2E-3-{4-[(7-hydroxy-2-oxo-3-phenyl-2H-chromen-4-yl)-methyl]-phenyl}-acrylic acid3-(4-((7-hydroxy-2-oxo-3-phenyl-2H-chromen-4-yl)-methyl)phenyl)acrylic acid7-hydroxycoumarin 25
02

Targets

ESR1 (ERα)

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