A polymorphism in the OPRM1 3'-untranslated region is associated with methadone efficacy in treating opioid dependence

Pharmacogenomics J. 2018 Jan;18(1):173-179. doi: 10.1038/tpj.2016.89. Epub 2016 Dec 13.

Abstract

The μ-opioid receptor (MOR) is the primary target of methadone and buprenorphine. The primary neuronal transcript of the OPRM1 gene, MOR-1, contains a ~13 kb 3' untranslated region with five common haplotypes in European-Americans. We analyzed the effects of these haplotypes on the percentage of opioid positive urine tests in European-Americans (n=582) during a 24-week, randomized, open-label trial of methadone or buprenorphine/naloxone (Suboxone) for the treatment of opioid dependence. A single haplotype, tagged by rs10485058, was significantly associated with patient urinalysis data in the methadone treatment group. Methadone patients with the A/A genotype at rs10485058 were less likely to have opioid-positive urine drug screens than those in the combined A/G and G/G genotypes group (relative risk=0.76, 95% confidence intervals=0.73-0.80, P=0.0064). Genotype at rs10485058 also predicted self-reported relapse rates in an independent population of Australian patients of European descent (n=1215) who were receiving opioid substitution therapy (P=0.003). In silico analysis predicted that miR-95-3p would interact with the G, but not the A allele of rs10485058. Luciferase assays indicated miR-95-3p decreased reporter activity of constructs containing the G, but not the A allele of rs10485058, suggesting a potential mechanism for the observed pharmacogenetic effect. These findings suggest that selection of a medication for opioid dependence based on rs10485058 genotype might improve outcomes in this ethnic group.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3' Untranslated Regions / genetics*
  • Adult
  • Alleles
  • Analgesics, Opioid / therapeutic use*
  • Australia
  • Buprenorphine / therapeutic use
  • Buprenorphine, Naloxone Drug Combination / therapeutic use
  • Female
  • Genotype
  • Humans
  • Male
  • Methadone / therapeutic use*
  • Narcotic Antagonists / therapeutic use
  • Opiate Substitution Treatment / methods
  • Opioid-Related Disorders / drug therapy*
  • Opioid-Related Disorders / genetics*
  • Polymorphism, Genetic / genetics*
  • Receptors, Opioid, mu / genetics*
  • White People / genetics

Substances

  • 3' Untranslated Regions
  • Analgesics, Opioid
  • Buprenorphine, Naloxone Drug Combination
  • Narcotic Antagonists
  • OPRM1 protein, human
  • Receptors, Opioid, mu
  • Buprenorphine
  • Methadone