The influence of febuxostat on coronary artery endothelial dysfunction in patients with coronary artery disease: A phase 4 randomized, placebo-controlled, double-blind, crossover trial

Am Heart J. 2018 Mar:197:85-93. doi: 10.1016/j.ahj.2017.11.006. Epub 2017 Nov 23.

Abstract

Background: The xanthine oxidase (XO) system is a significant source of vascular oxidative stress, which is believed to impair endothelial function, an important contributor to atherosclerotic disease. We tested whether febuxostat, a potent XO inhibitor, improves coronary endothelial function (CEF) in patients with stable coronary artery disease (CAD) in a single-center, randomized, placebo-controlled, double-blind crossover trial.

Methods: CEF was measured using noninvasive magnetic resonance imaging (MRI) assessment of changes in 30 patients with stable CAD and baseline impaired CEF. Patients received either febuxostat or placebo for 6 weeks and then were crossed over to the alternative for an additional 6 weeks. MRI-detected changes in coronary flow and in coronary cross-sectional area from rest to isometric handgrip exercise, a known endothelial-dependent stressor, were measured at the end of each 6 week period.

Results: Mean serum urate levels were lower at the end of the 6-week febuxostat period (2.9±0.8mg/dL) than at the end of the 6-week placebo period (5.9±0.04, P<.001). However, there were no significant differences in any of the CEF parameters measured at the end of the febuxostat and placebo periods.

Conclusions: In summary, although XO inhibition with febuxostat was well tolerated and lowered serum urate, it did not improve the primary end point of the study, CEF measured using MRI after 6 weeks of treatment. In conclusion, these findings suggest that short-term inhibition of XO does not significantly improve impaired CEF in patients with stable CAD.

Trial registration: ClinicalTrials.gov NCT01763996.

Publication types

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

MeSH terms

  • Coronary Artery Disease* / diagnosis
  • Coronary Artery Disease* / metabolism
  • Coronary Vessels* / diagnostic imaging
  • Coronary Vessels* / drug effects
  • Coronary Vessels* / physiopathology
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Monitoring / methods
  • Endothelium, Vascular* / drug effects
  • Endothelium, Vascular* / metabolism
  • Endothelium, Vascular* / physiopathology
  • Febuxostat / administration & dosage*
  • Female
  • Gout Suppressants / administration & dosage
  • Humans
  • Magnetic Resonance Imaging / methods
  • Male
  • Middle Aged
  • Oxidative Stress / drug effects
  • Treatment Outcome
  • Xanthine Oxidase* / antagonists & inhibitors
  • Xanthine Oxidase* / metabolism

Substances

  • Gout Suppressants
  • Febuxostat
  • Xanthine Oxidase

Associated data

  • ClinicalTrials.gov/NCT01763996