Drug intelligence / Profile preview

EGX358

Development stage
Unknown
Lead developer
Estrigenix Therapeutics
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Direct Infusion Into Hippocampus
01

Overview

EGX358 is a potent and highly selective small molecule agonist of the estrogen receptor beta (ERβ), developed to treat symptoms associated with menopause, including hot flashes and memory decline. It demonstrates approximately 750-fold selectivity for ERβ over estrogen receptor alpha (ERα), aiming to provide the cognitive and vasomotor benefits of hormone replacement therapy while minimizing risks such as breast cancer or adverse metabolic effects. In preclinical studies, EGX358 improved object recognition memory and reduced drug-induced hot flashes in ovariectomized mouse models without stimulating proliferation in ER+ breast cancer cells or causing organ toxicity. The compound does not inhibit primary liver enzymes at concentrations far exceeding its effective dose for ERβ activation. Estrigenix Therapeutics is developing EGX358 primarily as an oral therapy for menopausal women[2][3][4][6].

02

Targets

ESR2 (ERβ)

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