apimostinel

Description: Apimostinel (NRX-1074; AGN-241660) is a novel and orally bioactive antidepressant which acts as a selective partial agonist of an allosteric site of the glycine site of the NMDA receptor complex, which is under investigation by Naurex (recently acquired by Allergan) for the treatment of major depressive disorder. Its mechanism of action and effects are similar to those of rapastinel (GLYX-13), which is under development as an adjunctive therapy for treatment-resistant depression also by Naurex; however, NRX-1074 is 100-fold more potent by weight and, unlike GLYX-13 (which must be administered via intravenous injection), is orally -active.

References:

1. Naurex'sFirst Orally Active Molecule, NRX-1074, Demonstrates StatisticallySignificant Improvement in Depression Scores within 24 Hours in Phase 2Study for Major Depressive Disorder. January 28, 2015.

2. Park M, Niciu MJ, Zarate CA Jr. Novel Glutamatergic Treatments for Severe MoodDisorders. Curr Behav Neurosci Rep. 2015 Dec; 2(4):198-208. Epub 2015 Oct 9.PubMed PMID: 26824031; PubMed Central PMCID: PMC4725605.