Phase 2 trial of therapeutic for anxiety initiated

Key takeaways:

• ENX-102 is an investigational GABA-A 2,3,5 positive allosteric modulator that blocks 1.
• The safety and efficacy of ENX-102 will be tested in a multicenter phase 2 trial.

A Southern California-based neuroscience company has announced initiation of a phase 2 clinical trial to evaluate the safety and efficacy of investigational therapeutic ENX-102 in those with generalized anxiety disorder.

According to a release from Engrail Therapeutics, ENX-102 is a highly selective gamma-aminobutyric acid A (GABA-A) 2,3,5 positive allosteric modulator (PAM) and antagonist at 1-containing GABA-A channels.

Targeting the GABA-A receptor is a clinically validated pharmacological approach to treat anxiety as well as other centrally mediated disorders. However, according to the release, broad-spectrum GABA-A modulators such as benzodiazepines possess flaws that limit chronic use, primarily driven by GABA-A 1 subunit containing channels. ENX-102 seeks to enhance GABA neurotransmission in receptors containing 2, 3, and 5 while blocking 1, according to the release.

“Translational and phase 1 clinical data indicate central target engagement with a highly differentiated safety and tolerability profile for ENX-102 vs. non-selective GABA-A PAMs such as benzodiazepines,” Kimberly Vanover, PhD, chief scientific officer of Engrail, said in the release. “ENX-102 exhibits a long half-life and can be dosed once daily without titration. These data support further evaluation of ENX-102 for efficacy in generalized anxiety disorder.”