Effect of concomitant icosapent ethyl (eicosapentaenoic acid ethyl ester) on the pharmacokinetics of atorvastatin

Clin Drug Investig. 2015 Jan;35(1):45-51. doi: 10.1007/s40261-014-0252-8.

Abstract

Background and objective: Icosapent ethyl is a high-purity prescription form of eicosapentaenoic acid ethyl ester approved as an adjunct to diet to reduce triglyceride levels in adult patients with triglyceride levels ≥500 mg/dL (≥5.65 mmol/L). The objective of this open-label, drug-drug interaction study was to examine the effects of icosapent ethyl on the steady-state pharmacokinetics of atorvastatin, a commonly prescribed medication in patients with dyslipidaemia.

Methods: Thirty healthy subjects received atorvastatin 80 mg/day on days 1-7, icosapent ethyl 4 g/day on days 8-28, and co-administration on days 29-35. Primary end-points were natural log-transformed maximum plasma concentration (C(max)) and area under the concentration-versus-time curve from 0 to 24 h (AUC(0-24)) for atorvastatin, 2-hydroxyatorvastatin, and 4-hydroxyatorvastatin with and without icosapent ethyl.

Results: Of the 30 subjects enrolled, 26 completed the study. The 90% confidence intervals for C(max) and AUC(0-24) least-squares geometric mean ratios were within the 0.80-1.25 bounds. Concomitant administration of icosapent ethyl and atorvastatin was safe and well tolerated and icosapent ethyl did not significantly change the steady state C(max) and AUC(0-24) of atorvastatin, 2-hydroxyatorvastatin, or 4-hydroxyatorvastatin.

Conclusions: At steady-state concentrations, icosapent ethyl did not have an effect on the pharmacokinetics of atorvastatin. Co-administration of icosapent ethyl and atorvastatin was safe and well tolerated in healthy adult subjects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Atorvastatin
  • Cross-Over Studies
  • Drug Interactions / physiology
  • Drug Therapy, Combination
  • Eicosapentaenoic Acid / administration & dosage
  • Eicosapentaenoic Acid / analogs & derivatives*
  • Eicosapentaenoic Acid / pharmacokinetics
  • Female
  • Heptanoic Acids / administration & dosage*
  • Heptanoic Acids / pharmacokinetics*
  • Humans
  • Male
  • Middle Aged
  • Pyrroles / administration & dosage*
  • Pyrroles / pharmacokinetics*
  • Treatment Outcome

Substances

  • Heptanoic Acids
  • Pyrroles
  • eicosapentaenoic acid ethyl ester
  • Atorvastatin
  • Eicosapentaenoic Acid