A randomized, placebo-controlled pilot trial of the delta opioid receptor agonist AZD2327 in anxious depression

Psychopharmacology (Berl). 2016 Mar;233(6):1119-30. doi: 10.1007/s00213-015-4195-4. Epub 2016 Jan 4.

Abstract

Rationale: Patients with anxious major depressive disorder (AMDD) have more severe symptoms and poorer treatment response than patients with non-AMDD. Increasing evidence implicates the endogenous opioid system in the pathophysiology of depression. AZD2327 is a selective delta opioid receptor (DOR) agonist with anxiolytic and antidepressant activity in animal models.

Objective: This double-blind, parallel group design, placebo-controlled pilot study evaluated the safety and efficacy of AZD2327 in a preclinical model and in patients with AMDD.

Methods: We initially tested the effects of AZD2327 in an animal model of AMDD. Subsequently, 22 subjects with AMDD were randomized to receive AZD2327 (3 mg BID) or placebo for 4 weeks. Primary outcome measures included the Hamilton Depression Rating Scale (HAM-D) and the Hamilton Anxiety Rating Scale (HAM-A). We also evaluated neurobiological markers implicated in mood and anxiety disorders, including vascular endothelial growth factor (VEGF) and electroencephalogram (EEG).

Results: Seven (54 %) patients responded to active drug and three (33 %) responded to placebo. No significant main drug effect was found on either the HAM-D (p = 0.39) or the HAM-A (p = 0.15), but the HAM-A had a larger effect size. Levels of AZ12311418, a major metabolite of AZD2327, were higher in patients with an anti-anxiety response to treatment compared to nonresponders (p = 0.03). AZD2327 treatment decreased VEGF levels (p = 0.02). There was a trend (p < 0.06) for those with an anti-anxiety response to have higher EEG gamma power than nonresponders.

Conclusion: These results suggest that AZD2327 has larger potential anxiolytic than antidepressant efficacy. Additional research with DOR agonists should be considered.

Trial registration: ClinicalTrials.gov NCT00759395.

Keywords: AZD2327; Anxiety; Anxiolytic; Anxious depression; BDNF; Biomarkers; EEG; Major depressive disorder; Opiate; Preclinical.

Publication types

  • Randomized Controlled Trial
  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Animals
  • Anti-Anxiety Agents / therapeutic use*
  • Anxiety / blood
  • Anxiety / drug therapy*
  • Anxiety / physiopathology
  • Benzamides / therapeutic use*
  • Brain / physiopathology
  • Depressive Disorder, Major / blood
  • Depressive Disorder, Major / drug therapy*
  • Depressive Disorder, Major / physiopathology
  • Disease Models, Animal
  • Double-Blind Method
  • Electroencephalography
  • Female
  • Humans
  • Male
  • Middle Aged
  • Pilot Projects
  • Piperazines / therapeutic use*
  • Rats, Sprague-Dawley
  • Receptors, Opioid, delta
  • Vascular Endothelial Growth Factor A / blood
  • Young Adult

Substances

  • 4-((3-aminophenyl)(4-(4-fluorobenzyl)piperazin-1-yl)methyl)-N,N-diethylbenzamide
  • Anti-Anxiety Agents
  • Benzamides
  • Piperazines
  • Receptors, Opioid, delta
  • Vascular Endothelial Growth Factor A

Associated data

  • ClinicalTrials.gov/NCT00759395