AZD8529, a positive allosteric modulator at the mGluR2 receptor, does not improve symptoms in schizophrenia: A proof of principle study

Schizophr Res. 2016 Apr;172(1-3):152-7. doi: 10.1016/j.schres.2016.02.001. Epub 2016 Feb 26.

Abstract

Introduction: Activation of metabotropic glutamate (mGluR2/3) receptors has been proposed as an alternative mechanism to dopaminergic-based antipsychotics to correct glutamatergic deficits hypothesized to underlie schizophrenia symptoms. This study investigates the efficacy and safety of AZD8529, a selective positive allosteric modulator (PAM) at the mGlu2 receptor, in symptomatic patients with schizophrenia.

Methods: Patients were randomized to receive AZD8529 40 mg, risperidone 4 mg, or placebo as monotherapy. Treatment lasted for 28 days, and clinical efficacy was assessed using Positive and Negative Syndrome Scale (PANSS) and Clinical Global Impression (CGI) scores.

Results: There were no significant differences between patients treated with AZD8529 versus placebo in change from baseline to endpoint in PANSS total, negative and positive symptom subscale, or CGI-S scores. In contrast, risperidone demonstrated significant efficacy relative to placebo.

Conclusion: These results do not support a role for the mGluR-2 PAM AZD8529 as an antipsychotic and indicate that positive modulation of mGluR type 2 receptors alone is not sufficient for antipsychotic effects in acutely ill schizophrenia patients.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Allosteric Regulation
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / blood
  • Antipsychotic Agents / therapeutic use*
  • Double-Blind Method
  • Female
  • Humans
  • Indoles / adverse effects
  • Indoles / blood
  • Indoles / therapeutic use*
  • Male
  • Middle Aged
  • Oxadiazoles / adverse effects
  • Oxadiazoles / blood
  • Oxadiazoles / therapeutic use*
  • Psychiatric Status Rating Scales
  • Receptors, Metabotropic Glutamate / metabolism*
  • Risperidone / adverse effects
  • Risperidone / blood
  • Risperidone / therapeutic use
  • Schizophrenia / drug therapy*
  • Schizophrenia / metabolism
  • Treatment Outcome
  • Young Adult

Substances

  • AZD8529
  • Antipsychotic Agents
  • Indoles
  • Oxadiazoles
  • Receptors, Metabotropic Glutamate
  • metabotropic glutamate receptor 2
  • Risperidone