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Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism

Authors Chan NC, Bhagirath V, Eikelboom J

Received 28 April 2015

Accepted for publication 25 May 2015

Published 26 June 2015 Volume 2015:11 Pages 343—351

DOI https://doi.org/10.2147/VHRM.S63060

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 6

Editor who approved publication: Dr Daniel Duprez


Noel C Chan,1,2 Vinai Bhagirath,1,3 John W Eikelboom1,3,4

1Population Health Research Institute, Hamilton, ON, Canada; 2Department of Haematology, Monash Medical Center, Clayton, VIC, Australia; 3Thrombosis and Atherosclerosis Research Institute, 4Department of Medicine, McMaster University, Hamilton, ON, Canada

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.

Keywords: betrixaban, factor Xa inhibitors, anticoagulant, pharmacology, venous thromboembolism

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