title: Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism.
abstract: Venous thromboembolism (VTE), which includes deep vein thrombosis and pulmonary embolism, is a common and potentially preventable cause of morbidity and mortality. Unfractionated heparin, low-molecular-weight heparin, and warfarin have been the cornerstone of VTE prevention and treatment but are being replaced by recently approved non-vitamin K antagonist oral anticoagulants (NOACs): dabigatran, rivaroxaban, apixaban, and edoxaban. The NOACs are at least as effective and as safe as heparins and warfarin for VTE prevention and treatment and are more convenient because they have a low propensity for food and drug interactions and are given in fixed doses without routine coagulation monitoring. The remaining limitations of currently available NOACs include their dependence on renal and hepatic function for clearance, and the lack of an approved antidote. Betrixaban is a new NOAC with distinct pharmacological characteristics: minimal renal clearance, minimal hepatic metabolism, and long half-life. It has undergone successful Phase II studies in orthopedic thromboprophylaxis, and in stroke prevention in atrial fibrillation. Currently, it is being evaluated in a Phase III trial of extended thromboprophylaxis in medical patients (APEX study). In this article, we describe the development of betrixaban, review its pharmacological profile, discuss the results of clinical trials, and examine its potential for VTE prevention and treatment.
authors.affiliation: Population Health Research Institute, Hamilton, ON, Canada ; Department of Haematology, Monash Medical Center, Clayton, VIC, Australia.
authors.forename: Noel C
authors.initials: NC
authors.lastname: Chan
authors.affiliation: Population Health Research Institute, Hamilton, ON, Canada ; Thrombosis and Atherosclerosis Research Institute, Hamilton, ON, Canada.
authors.forename: Vinai
authors.initials: V
authors.lastname: Bhagirath
authors.affiliation: Population Health Research Institute, Hamilton, ON, Canada ; Thrombosis and Atherosclerosis Research Institute, Hamilton, ON, Canada ; Department of Medicine, McMaster University, Hamilton, ON, Canada.
authors.forename: John W
authors.initials: JW
authors.lastname: Eikelboom
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004195:Disease Models, Animal; D065427:Factor Xa Inhibitors / Q000494:pharmacology*; D006493:Heparin / Q000627:therapeutic use; D006801:Humans; D011725:Pyridines / Q000494:pharmacology*; D054556:Venous Thromboembolism / Q000188:drug therapy* / Q000517:prevention & control*; D014812:Vitamin K / Q000037:antagonists & inhibitors; D014859:Warfarin / Q000627:therapeutic use
chemical_list: D001549:Benzamides; D065427:Factor Xa Inhibitors; D011725:Pyridines; D014812:Vitamin K; D014859:Warfarin; C543086:betrixaban; D006493:Heparin
keywords: anticoagulant; betrixaban; factor Xa inhibitors; pharmacology; venous thromboembolism