Drug intelligence / Profile preview

DHED

Development stage
Preclinical
Lead developer
University of North Texas Health Science Center
Modality
Small Molecules
Administration
Subcutaneous
01

Overview

DHED (10β,17β-dihydroxyestra-1,4-dien-3-one) is a brain-selective estrogen prodrug designed to deliver 17β-estradiol specifically to the central nervous system while avoiding peripheral estrogenic side effects. It is chemically engineered to cross the blood-brain barrier and undergo enzymatic conversion to active 17β-estradiol only within the brain. Research has demonstrated that DHED provides neuroprotective benefits in models of Parkinson's disease by protecting dopaminergic neurons, reducing α-synuclein aggregation (by promoting tetramerization and autophagy of monomers), and mitigating motor deficits. By targeting the brain selectively, DHED aims to provide the therapeutic benefits of hormone replacement therapy without the associated systemic risks, such as increased cancer risk in reproductive tissues.

Other names
10β,17β-dihydroxyestra-1,4-dien-3-one10beta,17beta-dihydroxyestra-1,4-dien-3-one
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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