Atazanavir improves cardiometabolic measures but not vascular function in patients with long-standing type 1 diabetes mellitus

Acta Diabetol. 2015 Aug;52(4):709-15. doi: 10.1007/s00592-014-0708-6. Epub 2015 Jan 8.

Abstract

Aims: Vascular disease is the leading cause of morbidity and mortality in type 1 diabetes mellitus (T1DM). We previously demonstrated that patients with T1DM have impaired endothelial function, a forme fruste of atherosclerosis, as a result of increased oxidative stress. Bilirubin has emerged as a potent endogenous antioxidant with higher concentrations associated with lower rates of myocardial infarction and stroke.

Methods: We tested the hypothesis that increasing endogenous bilirubin using atazanavir would improve cardiometabolic risk factors and vascular function in patients with T1DM to determine whether targeting bilirubin may be a novel therapeutic approach to reduce cardiovascular disease risk in this population. In this single-arm, open-label study, we evaluated blood pressure, lipid profile, and conduit artery function in fifteen subjects (mean age 45 ± 9 years) with T1DM following a 4-day treatment with atazanavir.

Results: As anticipated, atazanavir significantly increased both serum total bilirubin levels (p < 0.0001) and plasma total antioxidant capacity (p < 0.0001). Reductions in total cholesterol (p = 0.04), LDL cholesterol (p = 0.04), and mean arterial pressure (p = 0.04) were also observed following atazanavir treatment. No changes were seen in either flow-mediated endothelium-dependent (p = 0.92) or nitroglycerine-mediated endothelium-independent (p = 0.68) vasodilation, measured by high-resolution B-mode ultrasonography at baseline and post-treatment.

Conclusion: Increasing serum bilirubin levels with atazanavir in subjects with T1DM over 4 days favorably reduces LDL and blood pressure but is not associated with improvements in endothelial function of conduit arteries.

Publication types

  • Clinical Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Antioxidants / metabolism
  • Atazanavir Sulfate / therapeutic use*
  • Atherosclerosis / etiology
  • Bilirubin / blood
  • Blood Pressure / drug effects
  • Cardiovascular System / drug effects*
  • Cardiovascular System / physiopathology
  • Cholesterol, LDL / blood
  • Diabetes Mellitus, Type 1 / complications
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Diabetes Mellitus, Type 1 / metabolism*
  • Diabetes Mellitus, Type 1 / physiopathology*
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / physiopathology
  • Female
  • Humans
  • Male
  • Middle Aged
  • Oxidative Stress / drug effects
  • Risk Factors
  • Vasodilation / drug effects
  • Vasodilation / physiology

Substances

  • Antioxidants
  • Cholesterol, LDL
  • Atazanavir Sulfate
  • Bilirubin