Drug intelligence / Profile preview

etazolate

Development stage
Phase 2
Lead developer
Exonhit
Modality
Small Molecules
Administration
Oral
01

Overview

Etazolate is a small molecule drug of the pyrazolopyridine class with anxiolytic and neuroprotective properties. It acts as a positive allosteric modulator of the GABA A receptor at the barbiturate binding site, an adenosine A1 and A2 receptor antagonist, and a selective phosphodiesterase 4 (PDE4) inhibitor. Etazolate has been shown to stimulate secretion of soluble amyloid precursor protein alpha (sAPPα), which is neurotrophic and procognitive, thereby protecting neurons from beta-amyloid toxicity—a key mechanism implicated in Alzheimer's disease. The drug has demonstrated anxiolytic and antidepressant effects in preclinical models, with potential utility for mood disorders such as depression, anxiety associated with traumatic brain injury, cognitive disorders including Alzheimer's disease, vascular dementia, and other neuropsychiatric conditions. Etazolate was originally developed by Bristol Myers Squibb and later by ExonHit Therapeutics (now Eurobio Scientific). It has completed phase II clinical trials for Alzheimer's disease[1][2][3][5][6][7][8].

Other names
etazolate hydrochloride
02

Targets

ADORA2A (Adenosine A₂A Receptor)GABRR (GABA-A receptor subunit rho)PDE4 (Phosphodiesterase 4A1)ADORA1 (Adenosine receptor A1 subtype)

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