Trends in the development of oral anticoagulants

Ther Deliv. 2015;6(6):685-703. doi: 10.4155/tde.15.22.

Abstract

Anticoagulation remains the therapy of choice for the prevention and treatment of venous and arterial thromboembolic disorders which can cause major organ damage or death. Heparins represent the antithrombotic drugs of choice in short and medium-term prophylaxis and therapy of thromboembolic diseases. Fondaparinux, a synthetic and structural analog of the antithrombin-binding pentasaccharide domain of heparin, has selective anti-Xa activity and longer half-life. However, anticoagulants are poorly absorbed by oral route because of their high molecular weight, hydrophilicity and negative charges. Long-term anticoagulation therapy is problematic because of side effects and frequent monitoring. Formulation approaches are particularly promising.

Keywords: Arixtra®; anticoagulation; arterial embolism; arterial thrombosis; atrial fibrillation; fondaparinux; heparin; heparin-induced thrombocytopenia; thromboembolic disorders; venous thrombosis; vitamin K antagonists.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / administration & dosage*
  • Anticoagulants / chemistry
  • Anticoagulants / pharmacology
  • Chemistry, Pharmaceutical / methods*
  • Drug Delivery Systems / methods*
  • Drug Discovery
  • Fondaparinux
  • Heparin / administration & dosage*
  • Heparin / chemistry
  • Heparin / pharmacology
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Molecular Weight
  • Nanoparticles
  • Particle Size
  • Polysaccharides / administration & dosage*
  • Polysaccharides / chemistry
  • Polysaccharides / pharmacology
  • Surface Properties

Substances

  • Anticoagulants
  • Polysaccharides
  • Heparin
  • Fondaparinux