Betrixaban - the next direct factor Xa inhibitor?
Venous thromboembolism is a major global health burden. Since the 1930s, prevention of stroke and pulmonary embolism in these patients has been achieved using conventional anticoagulants, such as heparin and warfarin. However, in recent years, four direct non-vitamin K antagonist oral anticoagulants (DOACs) have entered the market as alternative treatment options. Betrixaban is a fifth DOAC looking to gain marketing approval in the near future, and may have several potentially beneficial properties. Areas covered: Here, we outline the metabolism, pharmacokinetics, and pharmacodynamics of betrixaban, and summarise its clinical efficacy and safety based on the results of phase II/III trials. Expert commentary: Betrixaban has been demonstrated to have antithrombotic activity that may make it a valuable addition to the repertoire of DOACs currently available. The low renal clearance and minimal hepatic metabolism of the drug may make it particularly beneficial for patients with renal or hepatic dysfunction. The lack of an effective reversal agent may be a more significant issue for betrixaban compared with the already approved DOACs as it has a longer terminal half-life. Available data suggest that continued development of betrixaban is justified; however, further large randomised clinical trials are essential in order to clarify its efficacy and safety.
a Léman Research Institute , Neuhausen am Rheinfall , Switzerland.|b Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , University of Sevilla , Spain.
Martin
M
Thoenes
c Institute for Pharmacology and Preventive Medicine , Mahlow , Germany.
Joan
J
Minguet
c Institute for Pharmacology and Preventive Medicine , Mahlow , Germany.
Karin
K
Bramlage
b Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , University of Sevilla , Spain.|c Institute for Pharmacology and Preventive Medicine , Mahlow , Germany.
Peter
P
Bramlage
b Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , University of Sevilla , Spain.
Carmen
C
Ferrero
D000284:Administration, Oral; D000925:Anticoagulants / Q000494:pharmacology / Q000627:therapeutic use; D001549:Benzamides / Q000494:pharmacology / Q000627:therapeutic use*; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D065427:Factor Xa Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D011725:Pyridines / Q000494:pharmacology / Q000627:therapeutic use*; D016896:Treatment Outcome; D054556:Venous Thromboembolism / Q000097:blood / Q000188:drug therapy
D000925:Anticoagulants; D001549:Benzamides; D065427:Factor Xa Inhibitors; D011725:Pyridines; C543086:betrixaban
Betrixaban; DOAC; anticoagulants; factor Xa inhibitors; venous thromboembolism