title: Advances in oral anticoagulation therapy - What's in the pipeline?
abstract: Approximately 900,000 people are affected by some sort of venous thromboembolic (VTE) event every year in the United States. VTE diagnosis used to mean treatment with medications that required routine lab monitoring for safety and efficacy. Activated factor X (FXa) inhibition has emerged as a convenient pathway for management of VTE and currently three FXa inhibitors are available for anticoagulation management - rivaroxaban, apixaban, and edoxaban. Continued development of medications utilizing this pathway may offer advantages via novel pharmacokinetic or pharmacodynamic properties that may minimize the adverse effects associated with traditional anticoagulant therapy. This review summarizes the available information regarding pharmacokinetic, pharmacodynamic, and early safety and efficacy data for three factor Xa inhibitors being developed - darexaban, betrixaban and nokxaban. The studies reviewed in this article suggests that three newer agents possess the potential for promise based on early phase I and II trials.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, The University of Findlay, Findlay, OH 45840, USA. Electronic address: rao@findlay.edu.
authors.forename: P S S
authors.initials: PSS
authors.lastname: Rao
authors.affiliation: Department of Experiential Education, College of Pharmacy, The University of Findlay, Findlay, OH 45840, USA. Electronic address: burkart@findlay.edu.
authors.forename: T
authors.initials: T
authors.lastname: Burkart
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001381:Azepines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001549:Benzamides / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001777:Blood Coagulation / Q000187:drug effects; D055808:Drug Discovery; D065427:Factor Xa Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D011720:Pyrazoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D011725:Pyridines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D011728:Pyridones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D000069552:Rivaroxaban / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D013844:Thiazoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D054556:Venous Thromboembolism / Q000188:drug therapy*
chemical_list: D001381:Azepines; D001549:Benzamides; D065427:Factor Xa Inhibitors; D011720:Pyrazoles; D011725:Pyridines; D011728:Pyridones; D013844:Thiazoles; C522181:apixaban; C543086:betrixaban; D000069552:Rivaroxaban; C569750:darexaban; C552171:edoxaban
keywords: Activated factor X inhibitor; Anticoagulation therapy; Factor Xa; Novel oral anticoagulants; Venous thromboembolism