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zelquistinel
- Development stage
- Phase 2
- Lead developer
- Syndeio Biosciences
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Targeted Protein Degraders (TPDs) → Small Molecules, Multivalent & Scaffold-Based Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Zelquistinel is an orally active small-molecule positive allosteric modulator of the NMDA (N-methyl-D-aspartate) receptor under development for the treatment of major depressive disorder (MDD). It binds to a unique site on the NMDA receptor, independent of the glycine site, and enhances NMDAR-mediated synaptic plasticity. This mechanism is designed to rapidly and durably improve synaptic strength and function in brain regions implicated in depression and other neuropsychiatric disorders. Zelquistinel demonstrates rapid antidepressant effects with both acute (24-hour) and sustained (1-week) efficacy after single doses in preclinical studies. Unlike earlier NMDA modulators such as rapastinel or ketamine, zelquistinel is orally bioavailable with high potency and improved safety/tolerability profile—lacking sedative or motor impairment side effects typical of NMDAR antagonists. The drug was originally discovered by Naurex, further developed by Allergan/AbbVie, licensed to Gate Neurosciences for clinical development, and also associated with Syndeio Biosciences[1][3][5][6][7].
- Other names
- zelquistinelAGN 241751AGN241751AGN-241751
02
Targets
NMDAR (Glutamate receptor ionotropic, NMDA)
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