Zelquistinel acts through a unique binding site on the NMDA receptor, independent of the glycine site, to modulate receptor activity and enhance NMDAR-mediated synaptic plasticity.[4][5] Its
mechanism of action is similar to that of
rapastinel. However, unlike rapastinel, zelquistinel is orally bioavailable, exhibits increased potency, and has improved drug properties.[2][3][5]
On July 23, 2018, the U.S. FDA granted
Fast Track designation to the development of zelquistinel as an investigational new treatment for major depressive disorder.[6] As of August 2019, the drug had completed a
phase IIaclinical trial.[1][3][7]
^Clinical trial number NCT03586427 for "A Double-Blind, Placebo-Controlled, Fixed-Dose Study of AGN-241751 in Adult Participants With Major Depressive Disorder" at
ClinicalTrials.gov