Drug target · GRIN1

NMDA receptor

N-methyl-D-aspartate (NMDA) glutamate receptor — GluN1 glycine co-agonist site

7 compounds in the CNS pipeline act on NMDA receptor.

Compounds targeting NMDA receptor

CompoundActionAffinityLead programDeveloper
NRX-101 (D-cycloserine/lurasidone)primarySmall moleculePartial agonist—Phase 3Bipolar depressionNRx Pharmaceuticals, Inc.
AXS-05 (dextromethorphan-bupropion)primarySmall moleculeAntagonist—Phase 2Tobacco use disorderAxsome Therapeutics, Inc.
Blixeprodil (GM-1020)primarySmall moleculeAntagonistKi 3.25 µMPhase 2Major depressive disorderGilgamesh Pharmaceuticals, Inc.
AV-101 (L-4-chlorokynurenine)primarySmall moleculeAntagonist—Phase 1Levodopa-induced dyskinesia in Parkinson's diseaseVistagen Therapeutics, Inc.
AVP-786 (deudextromethorphan-quinidine)primarySmall moleculeAntagonist—DiscontinuedAgitation in Alzheimer's diseaseAvanir Pharmaceuticals
DalzanemdorprimarySmall moleculePAM—DiscontinuedHuntington's diseaseSage Therapeutics, Inc.
Esmethadone (REL-1017)Small moleculeAntagonist—DiscontinuedMajor depressive disorderRelmada Therapeutics, Inc.