No Pharmacokinetic Interactions Between Elbasvir or Grazoprevir and Methadone in Participants Receiving Maintenance Opioid Agonist Therapy

Clin Transl Sci. 2018 Nov;11(6):553-561. doi: 10.1111/cts.12564. Epub 2018 Jul 24.

Abstract

We conducted two phase I trials to evaluate the pharmacokinetic interactions between elbasvir (EBR), grazoprevir (GZR), and methadone (MK-8742-P010 and MK-5172-P030) in non-hepatitis C virus (HCV)-infected participants on methadone maintenance therapy. Coadministration of EBR or GZR with methadone had no clinically meaningful effect on EBR, GZR, or methadone pharmacokinetics. The geometric mean ratios (GMRs) for R- and S-methadone AUC0-24 were 1.03 (90% confidence interval (CI), 0.92-1.15) and 1.09 (90% CI, 0.94-1.26) in the presence/absence of EBR; and 1.09 (90% CI, 1.02-1.17) and 1.23 (90% CI, 1.12-1.35) in the presence/absence of GZR. The GMRs for EBR and GZR AUC0-24 in participants receiving methadone relative to a healthy historical cohort not receiving methadone were 1.20 (90% CI, 0.94-1.53) and 1.03 (90% CI, 0.76-1.41), respectively. These results indicate that no dose adjustment is required for individuals with HCV infection receiving stable methadone therapy and the EBR/GZR fixed-dose regimen.

Publication types

  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Amides
  • Analgesics, Opioid / agonists*
  • Antiviral Agents / administration & dosage
  • Antiviral Agents / pharmacokinetics*
  • Area Under Curve
  • Benzofurans / administration & dosage
  • Benzofurans / pharmacokinetics*
  • Carbamates
  • Cyclopropanes
  • Drug Interactions
  • Drug Therapy, Combination / methods
  • Female
  • Healthy Volunteers
  • Hepatitis C / complications
  • Hepatitis C / drug therapy
  • Humans
  • Imidazoles / administration & dosage
  • Imidazoles / pharmacokinetics*
  • Male
  • Methadone / administration & dosage
  • Methadone / pharmacokinetics*
  • Middle Aged
  • Opiate Substitution Treatment / methods
  • Opioid-Related Disorders / complications
  • Opioid-Related Disorders / rehabilitation
  • Quinoxalines / administration & dosage
  • Quinoxalines / pharmacokinetics*
  • Sulfonamides
  • Young Adult

Substances

  • Amides
  • Analgesics, Opioid
  • Antiviral Agents
  • Benzofurans
  • Carbamates
  • Cyclopropanes
  • Imidazoles
  • Quinoxalines
  • Sulfonamides
  • grazoprevir
  • elbasvir
  • Methadone