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Routes of administration | By mouth |
Drug class | NMDA receptor modulator |
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Chemical and physical data | |
Formula | C15H25N3O5 |
Molar mass | 327.381 g·mol−1 |
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Zelquistinel (GATE-251, formerly AGN-241751) is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Allergan.[1][2][3]
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 IIa clinical trial.[1][3][7]