NRX-1074

NRX-1074 (threonyl-prolyl-2R-(2-benzyl)-prolyl-threonine amide) is an orally-active experimental pharmaceutical and selective partial agonist of the glycine site of the NMDA receptor which is under investigation as a novel antidepressant drug. The drug was developed by Naurex for the treatment of major depressive disorder (MDD). 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 hundredfold more potent by weight and, unlike GLYX-13, orally-active. NRX-1074 has shown rapid antidepressant effects in preclinical models of depression. In addition, similarly to GLYX-13, it is well-tolerated and lacks the schizophrenia-like psychotomimetic effects of other NMDA receptor antagonists such as ketamine.

As of 2015, an intravenous formulation of NRX-1074 is in a phase II clinical trial for MDD. Concurrently, an oral formulation is in phase I trials for MDD.