AV-101, also known as “L-4-chlorokynurenine” and “4-Cl-KYN”, is a novel, orally available prodrug candidate focused on the treatment of neuropathic pain, depression, epilepsy and potentially other neurological conditions.

AV-101 is converted in the brain into an active metabolite, 7-chlorokynurenic acid (7-Cl-KYNA), which is an antagonist of the N-methyl-D-aspartate (NMDA) receptors. 7-Cl-KYNA is a synthetic analogue of kynurenic acid, which is a naturally occurring CNS regulatory compound, and is one of the most potent and selective blockers of the regulatory GlyB-site of the NMDA receptor.

In preclinical studies, AV-101 demonstrated very good levels of oral bioavailability, rapid and efficient transport across the blood-brain barrier and preferential conversion into 7-CKYNA at the site of seizures and potential neural damage in the brain and spinal cord.

AV-101 has successfully completed Phase 1 development in the U.S. under an active Investigational New Drug (IND) application on file at the U.S. FDA that defines the initial clinical development for neuropathic pain.

We believe the safety studies completed in our AV-101 Phase 1 program may enable Phase 2 development of AV-101 for neuropathic pain, epilepsy, and depression.

A non-confidential AV-101 program summary is available below. For additional information, please contact our Business Development Department at info@vistagen.com.