title: New oral anticoagulants in development: potential for improved safety profiles.
abstract: Venous thromboembolism is the most frequent preventable cause of death in hospitalized patients. Currently available anticoagulants have limitations that restrict their widespread use, particularly in long-term indications. Vitamin K antagonists require frequent monitoring and dose adjustment, and have a narrow therapeutic window with the risk of bleeding. The low-molecular-weight heparins have more predictable pharmacokinetics and pharmacodynamics, and coagulation monitoring is not required. However, their subcutaneous administration limits their suitability for long-term use. Consequently, many patients fail to receive effective preventive therapy. Rivaroxaban, apixaban, and dabigatran are new anticoagulants in late-stage clinical development that inhibit a single, specific coagulation factor, unlike the Vitamin K antagonists and low-molecular-weight heparins. Studies suggest that they provide effective, predictable anticoagulation with a low bleeding risk and will potentially offer an improved clinical profile and wider safety margin compared with currently available therapies.
authors.affiliation: Hematology-Oncology Division, Beth Israel Deaconess Medical Center and VA Boston Healthcare System, Boston, MA, USA.
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Bauer
mesh_terms: D000284:Administration, Oral; D000925:Anticoagulants / Q000009:adverse effects / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology; D001777:Blood Coagulation / Q000187:drug effects*; D000069604:Dabigatran; D004341:Drug Evaluation; D015951:Factor Xa / Q000187:drug effects; D006801:Humans; D009025:Morpholines / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology; D011725:Pyridines / Q000494:pharmacology; D011728:Pyridones / Q000494:pharmacology; D000069552:Rivaroxaban; D013876:Thiophenes / Q000494:pharmacology; D013917:Thrombin / Q000187:drug effects; D054556:Venous Thromboembolism / Q000188:drug therapy* / Q000517:prevention & control
chemical_list: D000925:Anticoagulants; D001562:Benzimidazoles; D009025:Morpholines; D011720:Pyrazoles; D011725:Pyridines; D011728:Pyridones; D013876:Thiophenes; C522181:apixaban; D000069552:Rivaroxaban; D013917:Thrombin; D015951:Factor Xa; D000069604:Dabigatran