Drug intelligence / Profile preview

apimostinel

Development stage
Phase 2
Lead developer
Syndeio Biosciences
Modality
Small Molecules, Peptides
01

Overview

Apimostinel is an investigational, rapid-acting antidepressant that functions as a novel and selective modulator of the N-methyl-D-aspartate (NMDA) receptor. It is a structurally modified amidated tetrapeptide, designed to enhance metabolic stability and pharmacokinetics compared to its predecessor, rapastinel. Apimostinel acts at a unique binding site on the NMDA receptor—distinct from the glycine site—to positively modulate receptor activity and enhance synaptic plasticity. This mechanism results in rapid antidepressant effects without the psychotomimetic or dissociative side effects associated with NMDA antagonists like ketamine. The drug has demonstrated statistically significant, robust antidepressant efficacy within 24 hours in clinical studies for major depressive disorder (MDD), with additional development for acute depressive disorders including depression with suicidality and postpartum depression[1][3][5][10].

Other names
apimostinel [USAN]Apimostinel (USAN)UNII-TTT1F11FZBUNII-TTT-1F11FZBUNII-TTT 1F11FZB
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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