Today, GABA Therapeutics commenced dosing for its Phase I clinical trial of the anxiolytic etifoxine in Melbourne, Australia – right on schedule. The Phase I, two-stage, double-blind, placebo-controlled single and multiple dose study will evaluate the pharmacokinetics, pharmacodynamics, and safety of oral etifoxine in up to 34 normal healthy volunteers.

“Data from this study could provide important insights for a broad range of neurological disorders beyond anxiety and depression.” said Dr. Ian Massey, co-founder and CEO of GABA Therapeutics.

Etifoxine Background

Clinical studies have shown that etifoxine has comparable speed of onset and anxiolytic efficacy as the world’s top two selling benzodiazepines (Xanax® and Ativan®), without the side effects of sedation, amnesia, ataxia, and dependence associated with benzodiazepines. The drug is non-addictive, and adverse drug effects occurred in just 21 per million patients (0.0021%), based on a pharmacovigilance study released by the French National Agency for the Safety of Medicines and Health Products that found no cases of abuse, misuse, or dependence after analyzing over 14 million prescriptions of etifoxine between 2000 and 2012.

Etifoxine appears to have a dual mechanism of action, leading to increases in endogenous neurosteroids such as allopregnanolone, which are essential for maintaining healthy brain biochemistry. Neurosteroids can induce potent anxiolytic, antidepressant, anticonvulsant, and analgesic effects, mainly through interaction with the GABA channel, the main inhibitory system in the brain. Although there is a great deal of clinical experience with etifoxine, little has been published on its pharmacokinetics and effects on neurosteroids in humans. Therefore, GABA’s Australian trial will be a key step in building reliable clinical data on Etifoxine’s efficacy and safety.

GABA’s flagship product, GRX-917, the deuterated version of etifoxine, has an identical mechanism of action, biology and pharmacology, as etifoxine, but with improved pharmacokinetics. Based on all the data for etifoxine , GRX-917 will be safer and clinically superior to America’s top two drug classes of anxiolytics: SSRIs/SNRIs and benzodiazepines. Additionally, the drug is not expected to be a controlled substance, since etifoxine is not a controlled substance in France or any other country in which it is sold. Currently, there is no clinically competitive anxiolytic drug on the market or in late stage development.

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