PF-03463275 / Pfizer - LARVOL DELTA

Transport mechanism and pharmacology of the human GlyT1. (PubMed, Cell) - "Here, we report the cryo-EM structures of GlyT1 bound with substrate glycine and drugs ALX-5407, SSR504734, and PF-03463275...Additionally, we identified three specific pockets accommodating drugs, providing clear insights into the structural basis of their inhibitory mechanism and selectivity. Collectively, these structures offer significant insights into the transport mechanism and recognition of substrate and anti-schizophrenia drugs, thus providing a platform to design small molecules to treat schizophrenia."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

Randomized controlled trial of the glycine transporter 1 inhibitor PF-03463275 to enhance cognitive training and neuroplasticity in schizophrenia. (PubMed, Schizophr Res) - "PF-03463275 was not associated with improved CT learning parameters. Participation in CT was associated with improvement in MCCB scores."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

NCATS: Translational Neuroscience Optimization of GlyT1 Inhibitor (clinicaltrials.gov) - P2 | N=71 | Completed | Sponsor: Yale University | Active, not recruiting ➔ Completed

Trial completion • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

NCATS: Translational Neuroscience Optimization of GlyT1 Inhibitor (clinicaltrials.gov) - P2; N=90; Active, not recruiting; Sponsor: Yale University; Trial completion date: Dec 2020 ➔ Dec 2021; Trial primary completion date: Dec 2020 ➔ Jun 2021

Trial completion date • Trial primary completion date • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

NCATS: Translational Neuroscience Optimization of GlyT1 Inhibitor (clinicaltrials.gov) - P2; N=90; Recruiting; Sponsor: Yale University; Trial completion date: Jul 2018 ➔ Jan 2019

Trial completion date • Alzheimer's Disease • Biosimilar • CNS Disorders • Schizophrenia