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| Other names | NRX-1074; AGN-241660; Threonyl-prolyl-2R-(2-benzyl)-prolyl-threonine amide |
| Routes of administration | By mouth |
| Drug class | NMDA receptor modulator |
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| Chemical and physical data | |
| Formula | C25H37N5O6 |
| Molar mass | 503.600 g·mol−1 |
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Apimostinel (GATE-202, formerlyNRX-1074) is an investigationalantidepressant, acting as a novel and selectivemodulator of theNMDA receptor.[1][2][3][4] It is currently under development for the acute treatment ofmajor depressive disorder (MDD) by Syndeio Biosciences, and previously byNaurex andAllergan.[5][6][7] As of February 2015, anintravenous formulation of apimostinel has completed aphase IIaclinical trial for MDD.[5][8]
Similar torapastinel (GLYX-13), itsmechanism of action 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.[9] However, apimostinel is 1000-fold more potent in vitro and is intended as an improved, follow-up drug to rapastinel.[2][5] Similar to rapastinel, apimostinel is anamidatedtetrapeptide, but has beenstructurally modified, via the addition of abenzyl group, to enhance its metabolic stability and pharmacokinetic profile. The drug has shown rapid and potentantidepressant effects inpre-clinical models ofdepression.[5] In addition, similarly to rapastinel, it is well tolerated and lacks thehallucinosis-likepsychotomimetic effects ofNMDA receptor antagonists such asketamine.[5]
