title: Trends in the development of oral anticoagulants.
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.
authors.affiliation: Institut Galien Paris-Sud CNRS UMR 8612, 5 rue JB Clément, 92296 Châtenay-Malabry Cedex, France.
authors.forename: Bettina
authors.initials: B
authors.lastname: Ralay-Ranaivo
authors.affiliation: EA 4531 - Ingénierie des protéines de l'hémostase à potentiel thérapeutique, 5 rue JB Clément, 92296 Châtenay-Malabry Cedex, France.
authors.forename: Delphine
authors.initials: D
authors.lastname: Borgel
authors.affiliation: Institut Galien Paris-Sud CNRS UMR 8612, 5 rue JB Clément, 92296 Châtenay-Malabry Cedex, France.
authors.forename: Patrick
authors.initials: P
authors.lastname: Couvreur
authors.affiliation: Institut Galien Paris-Sud CNRS UMR 8612, 5 rue JB Clément, 92296 Châtenay-Malabry Cedex, France.|Institut of Molecular Sciences, UMR CNRS 8214, Université Paris-Sud, 91405 Orsay, France.
authors.forename: Ruxandra
authors.initials: R
authors.lastname: Gref
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D055808:Drug Discovery; D000077425:Fondaparinux; D006493:Heparin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008970:Molecular Weight; D053758:Nanoparticles; D010316:Particle Size; D011134:Polysaccharides / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D013499:Surface Properties
chemical_list: D000925:Anticoagulants; D011134:Polysaccharides; D006493:Heparin; D000077425:Fondaparinux
keywords: Arixtra®; anticoagulation; arterial embolism; arterial thrombosis; atrial fibrillation; fondaparinux; heparin; heparin-induced thrombocytopenia; thromboembolic disorders; venous thrombosis; vitamin K antagonists