With grant funding from the U.S. National Institutes of Health (NIH), biotechnology company VistaGen Therapeutics, Inc. has successfully completed Phase 1 development of AV-101, an orally available small molecule prodrug candidate. AV-101 is targeted at the multibillion-dollar neurological disease and disorder market, including depression and neuropathic pain, which is a serious and chronic condition that causes pain after an injury or disease of the peripheral or central nervous system. In support of the company’s nonclinical and Phase 1 clinical development of AV-101, the NIH awarded VistaGen more than $8.8 million in grant funding.
Also known as “L-4-chlorokynurenine” and “4-CI-KYN,” AV-101 is converted in the brain into 7-chlorokynurenic acid (7-CI-KYNA), an active metabolite and an agonist of the N-methyl-D-aspartate (NMDA) receptors. One of the most potent and selective blockers of the regulatory GlyB-site of the NMDA receptor, 7-CI-KYNA is a synthetic analog of kynurenic acid, which is a naturally occurring CNS regulatory compound.
AV-101 demonstrated very good levels of oral bioavailability in preclinical studies, as well as rapid and efficient transport across the blood-brain barrier and preferential conversion into 7-CI-KYNA at the site of seizures and potential neural damage in the brain and spinal cord.
VistaGen believes the safety studies completed in its AV-101 Phase 1 program may enable Phase 2 development of the drug for both neuropathic pain and depression. AV-101 has the potential to treat other neurological conditions, as well.
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