Apimostinel

Pharmacology

Apimostinel (GATE-202, formerly NRX-1074) is an investigational antidepressant, acting as a novel and selective modulator of the NMDA receptor.

It was derived from Rapastinel (GLYX-13), for improved potency and pharmacokinetics. Apimostinel is 1000-fold more potent in vitro and is intended as an improved, follow-up drug. Similar to Rapastinel, Apimostinel is an amidated tetrapeptide, but has been structurally modified, via the addition of a benzyl group, to enhance its metabolic stability and pharmacokinetic profile.

Estimated dose is 5mg IN. Half-life is <1h but lasts up to a week like Rapastinel and Zelquistinel.