VistaGen Therapeutics, a biopharmaceutical company developing new generation medicines for anxiety, depression, and other CNS disorders, announced positive results from second preclinical study of their investigational drug, AV-101, in combination with probenecid.
AV-101 is an oral prodrug of 7-chloro-kynurenic acid (7-Cl-KYNA), a potent and selective full antagonist of the glycine site of the NMDAR (N-methyl-D-aspartate receptor), an ionotropic glutamate receptor in the brain. Unlike many other NMDAR antagonists, 7-Cl-KYNA reduces, rather than blocks, NMDA receptor signaling.
Probenecid is a safe FDA-approved oral drug used to treat gout. When used as an adjuvant, probenecid is known to increase the therapeutic benefit of numerous antiviral, anticancer and antibacterial drugs.
The results of the new preclinical study show that AV-101, when administered in combination with probenecid, substantially increased the brain concentration of 7-Cl-KYNA. Importantly, AV-101 has exhibited no dissociative or hallucinogenic psychological side effects or safety concerns similar to those that may be caused by NMDAR antagonists that block the ion channel of the NMDAR, such as amantadine, esketamine and ketamine.
With its favorable safety profile, AV-101, in combination with probenecid, has potential to be an oral new generation treatment for multiple CNS disorders.
The FDA has granted Fast Track designation for development of AV-101 as both a potential adjunctive treatment for major depressive disorder and as a non-opioid treatment for neuropathic pain.
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