Advances in oral anticoagulation therapy – What's in the pipeline?

• Published in: Blood reviews Vol. 31; no. 4; pp. 205 - 211
• Main Authors: Rao, P.S.S, Burkart, T
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.07.2017
• Subjects: Activated factor X inhibitor; Administration, Oral; Animals; Anticoagulation therapy; Azepines - administration & dosage; Azepines - pharmacokinetics; Azepines - pharmacology; Azepines - therapeutic use; Benzamides - administration & dosage; Benzamides - pharmacokinetics; Benzamides - pharmacology; Benzamides - therapeutic use; Blood Coagulation - drug effects; Drug Discovery; Factor Xa; Factor Xa Inhibitors - administration & dosage; Factor Xa Inhibitors - pharmacokinetics; Factor Xa Inhibitors - pharmacology; Factor Xa Inhibitors - therapeutic use; Hematology, Oncology and Palliative Medicine; Humans; Novel oral anticoagulants; Pyrazoles - administration & dosage; Pyrazoles - pharmacokinetics; Pyrazoles - pharmacology; Pyrazoles - therapeutic use; Pyridines - administration & dosage; Pyridines - pharmacokinetics; Pyridines - pharmacology; Pyridines - therapeutic use; Pyridones - administration & dosage; Pyridones - pharmacokinetics; Pyridones - pharmacology; Pyridones - therapeutic use; Rivaroxaban - administration & dosage; Rivaroxaban - pharmacokinetics; Rivaroxaban - pharmacology; Rivaroxaban - therapeutic use; Thiazoles - administration & dosage; Thiazoles - pharmacokinetics; Thiazoles - pharmacology; Thiazoles - therapeutic use; Venous thromboembolism; Venous Thromboembolism - drug therapy; Activated factor X inhibitor; A nticoagulation therapy; N ovel oral anticoagulants; F actor Xa; V enous thromboembolism; Factor Xa; Anticoagulation therapy; Novel oral anticoagulants; Venous thromboembolism
• ISSN: 0268-960X; 1532-1681
• DOI: 10.1016/j.blre.2017.02.002

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.