GRX-917 MECHANISM OF ACTION

Increasing the Production of Endogenous Neurosteroids

Neurosteroids are essential for proper brain and neurological function.

Increasing the production of endogenous neurosteroids has two key benefits:

• Neurosteroids are potent positive allosteric modulators at GABAA receptors
• Neurosteroids inhibit NLRP3 inflammation by over 90%

Neurosteroids are clinically anxiolytic, anti-depressant and anti-epileptic.

GRX-917/etifoxine stimulate translocation of cholesterol into mitochondria, thus increasing endogenous neurosteroid synthesis. 

Neurosteroids, such as allopregnanolone:

• Modulate neurotransmitter receptors, such as GABA-A
• Inhibit the TLR4/MyD88/NF-kB/NLRP3 inflammatory pathway, leading to reduced NLRP3 inflammasome activity and proinflammatory mediators

The anti-inflammatory and neuromodulatory effects of GRX-917/etifoxine supports the broad potential of this novel therapeutic class.