The pharmacokinetics of edoxaban for the prevention and treatment of venous thromboembolism

Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):445-58. doi: 10.1517/17425255.2014.882897. Epub 2014 Jan 28.

Abstract

Introduction: Thromboembolic diseases will become the most important contributors to mortality and morbidity for modern societies. Current antithrombotic strategies using heparins or vitamin K antagonists are inconvenient, with limitations and inherent side effects. A series of new oral anticoagulants with powerful and reliable antithrombotic actions have been developed in the last decade.

Areas covered: Edoxaban is a direct and specific inhibitor of activated factor X, delivered orally. This article reviews literature from PubMed and articles referenced within. The text explores the pharmacological aspects of its antithrombotic action. Pharmacokinetics, metabolism and drug interactions are examined. The review places the results of recent clinical trials that have evaluated the antithrombotic potential of edoxaban versus standard antithrombotic therapies in the prophylaxis and treatment of venous thromboembolism into perspective. The possible relationship between the pharmacokinetic profile of edoxaban and the favorable results in clinical trials is discussed.

Expert opinion: Edoxaban is perceived as a major advance, compared to vitamin K antagonists, in the prevention and treatment of thromboembolic disease given its favorable efficacy, safety, pharmacokinetic profile and renal clearance. The results of ongoing large international trials exploring the prevention of thrombotic complications in patients in different clinical settings should ensure the approval of edoxaban to treat new indications.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / pharmacokinetics*
  • Anticoagulants / therapeutic use
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Factor Xa Inhibitors / chemistry
  • Factor Xa Inhibitors / pharmacokinetics*
  • Factor Xa Inhibitors / therapeutic use
  • Fibrinolytic Agents / pharmacokinetics*
  • Fibrinolytic Agents / therapeutic use
  • Humans
  • Pyridines / chemistry
  • Pyridines / pharmacokinetics*
  • Pyridines / therapeutic use
  • Randomized Controlled Trials as Topic
  • Thiazoles / chemistry
  • Thiazoles / pharmacokinetics*
  • Thiazoles / therapeutic use
  • Venous Thromboembolism / prevention & control*

Substances

  • Anticoagulants
  • Factor Xa Inhibitors
  • Fibrinolytic Agents
  • Pyridines
  • Thiazoles
  • edoxaban