NeuroRx believes

that its therapeutic approach may offer an oral, outpatient treatment with the potential to significantly extend NRX-100 (ketamine)’s antidepressant/anti-suicidal effects

All information on this page refers to a mechanism of action of an investigational drug treatment regimen – not approved by the FDA

Mechanism of Action

NRX-101's proprietary dual-mechanism of action targets the NMDA and 5-HT2a receptors - two key receptors in the brain.

 

The NMDA receptor is a glutamate receptor found in nerve cells.  It is critical to the memory function as it controls signaling from neuron to neuron.  NMDA also directly regulates a calcium ion channel that controls the rate of ideation (formation of new ideas) in the brain. D-cycloserine, one of the active ingredients in NRX-101, targets the NMDA receptor and modulates NMDA activity, potentially fostering a normal pace of thought generation. Multiple human studies have demonstrated that administration of D-cycloserine triggers an antidepressant effect. However, our research indicates that the treatment requires administration with an antipsychotic to counteract the psychomimetic side effects.

 

The 5-HT2a receptor is a G protein-coupled receptor and a member of the serotonin family. It is known for its role in mediating certain antipsychotic effects. Lurasidone, the other active ingredient in NRX-101, is a 5-HT2a antagonist that is currently approved as an antipsychotic, and for use in bipolar depression. Laboratory studies have shown that Lurasidone and other 5-HT2a antagonists have an unexpected synergistic effect with D-cycloserine, potentially enhancing the antidepressant effect while minimizing the potential psychomimetic (hallucinations) side effects. A phase 2 human study has shown results consistent with this finding.

 

NRX-101's proprietary combination of D-cycloserine and Lurasidone is designed to be administered orally, daily for approximately six weeks following an initial, single infusion of NRX-100 (ketamine). The company believes that this therapeutic approach may offer an oral, outpatient treatment with the potential to significantly extend NRX-100 (ketamine)'s antidepressant/anti-suicidal effect.

 

 

 

 

NMDA regulates the speed of thoughts:

Too little NMDA activity > Increased Ideation, hallucinations, psychosis

Too much NMDA activity > Reduced Ideation, depression, suicide

© 2016 NeuroRx, Inc.

*These drugs are investigational and not approved by the US FDA

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