Drug intelligence / Profile preview

ENX-102

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

Overview

ENX-102 is an investigational, orally administered small molecule that acts as a subtype-selective positive allosteric modulator (PAM) of the gamma-aminobutyric acid type A receptor (GABA-A). It selectively enhances GABA neurotransmission at receptors containing the α2, α3, and α5 subunits while blocking activity at the α1 subunit. This selectivity is designed to provide anxiolytic effects without the sedative, psychomotor, and cognitive side effects commonly associated with non-selective GABA-A PAMs such as benzodiazepines. ENX-102 has demonstrated strong anxiolytic effects in preclinical models of generalized anxiety disorder (GAD) and has shown favorable safety and tolerability profiles in clinical studies. The drug is being developed primarily for generalized anxiety disorder but may have potential applications in other neuropsychiatric conditions such as panic disorder and social anxiety disorder[1][2][3][5][7][8].

02

Targets

GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRA3 (Gamma-aminobutyric acid receptor subunit alpha-3)

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