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

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Chan NC, Bhagirath V, Eikelboom JW

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

Vasc Health Risk Manag. 2015 Jun 26;11:343-51. doi: 10.2147/VHRM.S63060. eCollection 2015.

PubMed ID

26170684 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drugs

Betrixaban

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Betrixaban	Coagulation factor X	Protein	Humans	Yes	Inhibitor	Details

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Betrixaban	P-glycoprotein 1	Protein	Humans	No	Substrate	Details
Betrixaban	Potassium voltage-gated channel subfamily H member 2	Protein	Humans	Unknown	Inhibitor	Details