AV-101, an Oral NMDR Glycine Site Antagonist for Depression and Neurological Disorders

AV-101, an Oral NMDR Glycine Site Antagonist for Depression and Neurological Disorders

AV-101 (4-Cl-KYN) is an investigational prodrug designed to be orally administered and to target the N-methyl-D-aspartate receptor (NMDAR), an ionotropic glutamate receptor in the brain. Abnormal NMDAR function is associated with numerous CNS diseases and disorders. AV-101’s active metabolite, 7-chloro-kynurenic acid (7-Cl-KYNA), has been observed to be a potent and selective full antagonist of the glycine co-agonist site of the NMDAR that inhibits the function of the NMDAR, but does not block NMDAR function like ketamine and other NMDAR antagonists. AV-101 has been observed in clinical trials to be orally bioavailable, well-tolerated and has not exhibited dissociative or hallucinogenic psychological side effects or safety concerns similar to those that may be caused by other NMDAR antagonists.

In light of these and findings from a wide range of preclinical studies, we believe that AV-101, in combination with FDA-approved probenecid, has potential to become a new oral treatment alternative for certain CNS indications involving the NMDAR. The FDA has granted Fast Track designation for development of AV-101 as a potential adjunctive treatment for MDD and as a non-opioid treatment for neuropathic pain.

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