AV-101 (4-Cl-KYN)

AV-101 (4-CI-KYN) is an orally available, clinical-stage prodrug candidate that readily gains access to the central nervous system (CNS), where it is rapidly converted in-vivo into its active metabolite, 7-chlorokynurenic acid (7-Cl-KYNA), a well-characterized, potent and highly selective antagonist of the NMDAR at the GlyB co-agonist site. Current evidence suggests that AV-101’s antagonism of NMDAR signaling may provide fast-acting antidepressant effects in the treatment of MDD. In addition, as confirmed in our AV-101 Phase 1 clinical studies, targeting the GlyB site of the NMDAR does not have the adverse side effects typically associated with classic NMDAR antagonists, such as ketamine, and other NMDA channel blockers. 

Preclinical studies also support the hypothesis that AV-101 has the potential to treat several additional CNS disorders and neurodegenerative diseases, including chronic neuropathic pain, epilepsy, Parkinson’s disease and Huntington’s disease, where modulation of the NMDAR or active metabolites of AV-101 may achieve therapeutic benefit.