GATE-251 / Gate Neurosciences - LARVOL DELTA

Zelquistinel (GATE-251) is an orally bioavailable novel NMDA receptor modulator that exhibits rapid and sustained antidepressant-like effects (Neuroscience 2021) - "Here we report that zelquistinel (AGN-241751), a novel, positive NMDAR modulator, exhibits high oral bioavailability and dose-proportional exposures in plasma and the central nervous system and produces sustained antidepressant-like effects in rodents by improving synaptic plasticity. Zelquistinel produces rapid and sustained anti-depressant effects by positively modulating the NMDAR and improving synaptic plasticity. Zelquistinel is currently in phase 2 development as a treatment for MDD."

CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry • GRIN2A

Zelquistinel (GATE-251): Results of a Phase 1 Single Ascending Dose Study to Evaluate the Safety, Pharmacokinetics, and EEG Effects of a Novel Rapid Acting, Orally-Bioavailable NMDA Receptor Modulator (ACNP 2021) - "GATE-251 was well-tolerated oral NMDA modulator with few treatment-related AEs. There was no evidence of psychotomimetic effects over the dose range evaluated. GATE-251 was rapidly absorbed into the plasma and exposure was dose-related."

Clinical • P1 data • PK/PD data • Alzheimer's Disease • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Pain • Psychiatry

Zelquistinel (GATE-251): Results of a Phase 1 Single Ascending Dose Study to Evaluate the Safety, Pharmacokinetics, and EEG Effects of a Novel Rapid Acting, Orally-Bioavailable NMDA Receptor Modulator (ACNP 2021) - "GATE-251 was well-tolerated oral NMDA modulator with few treatment-related AEs. There was no evidence of psychotomimetic effects over the dose range evaluated. GATE-251 was rapidly absorbed into the plasma and exposure was dose-related."

Clinical • P1 data • PK/PD data • Alzheimer's Disease • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Pain • Psychiatry

Safety and Tolerability of GATE-251 in Normal Human Volunteers (clinicaltrials.gov) - P1; N=68; Completed; Sponsor: Ronald M Burch MD PhD

New P1 trial • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry