A drug interaction study investigating the effect of Rifabutin on the pharmacokinetics of Maraviroc in healthy subjects

PLoS One. 2019 Oct 24;14(10):e0223969. doi: 10.1371/journal.pone.0223969. eCollection 2019.


Effects of steady-state rifabutin on the pharmacokinetics of steady-state maraviroc were investigated in fourteen healthy adult female and male volunteers. Maraviroc 300 mg twice daily (BID) was given orally with food for fifteen days. On day six, rifabutin 300 mg once daily (QD, P.O.) was added to the regimen. Formal pharmacokinetic (PK) sampling was performed on days five and fifteen. Individual plasma drug concentration-time data for maraviroc, and rifabutin on day fifteen, were obtained using validated High Performance Liquid Chromatography (HPLC) tandem Mass Spectrometry (MS/MS). Rifabutin steady state exposure was comparable to data in the literature. Maraviroc area under the curve (AUC) and minimum plasma concentration (Clast or Cmin) were reduced by 17% and 30% respectively when co-administered with rifabutin. No unexpected or serious adverse eventsoccurred. Based on the reduced exposure of maraviroc observed in this study, increasing the dose of maraviroc may be studied to normalize its moderately reduced exposure following rifabutin co-administration, a moderate inducer of CYP3A4.

Trial registration: ClinicalTrials.gov NCT01894776.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Anti-Bacterial Agents / pharmacokinetics*
  • Drug Interactions*
  • Female
  • HIV Fusion Inhibitors / pharmacokinetics*
  • Healthy Volunteers
  • Humans
  • Male
  • Maraviroc / pharmacokinetics*
  • Middle Aged
  • Rifabutin / pharmacokinetics*
  • Tissue Distribution
  • Young Adult


  • Anti-Bacterial Agents
  • HIV Fusion Inhibitors
  • Rifabutin
  • Maraviroc

Associated data

  • ClinicalTrials.gov/NCT01894776

Grant support

This study was funded by ViiV Healthcare, a Pfizer affiliate. The Department of Medicine, University of Ottawa at The Ottawa Hospital provided support to DWC. ViiV Healthcare and the University of Ottawa had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.