IMR Press / FBL / Volume 11 / Issue 1 / DOI: 10.2741/1794

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article
Factor Xa inhibitors: new anti-thrombotic agents and their characteristics
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1 Department of Internal Medicine, Hokkaido University School of Medicine, Sapporo, Japan
2 Department of Clinical Laboratory, School of Dentistry, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido University School of Medicine, Sapporo, Japan
3 Department of Medicine II, Hokkaido University School of Medicine, Sapporo, Japan
Academic Editor:Arthur Chu
Front. Biosci. (Landmark Ed) 2006, 11(1), 232–248; https://doi.org/10.2741/1794
Published: 1 January 2006
(This article belongs to the Special Issue Blood coagulation, inflammation, and thrombosis)
Abstract

Factor Xa (FXa) is a key enzyme that is positioned at the convergence of the intrinsic and extrinsic pathways in the blood coagulation cascade, and inactivation by a specific FXa inhibitor effectively prevents the generation of thrombin. Various types of low molecular weight (LMW) heparin, which function as semi-selective and indirect FXa inhibitors, are replacing unfractionated heparin (UFH) as agents for the prevention and treatment of venous thromboembolism (VTE), as well as in initial treatment for coronary events. Of those, heparinoid has been shown to be safer and more effective for the prevention of postoperative VTE than UFH, especially for treatment of heparin-induced thrombocytopenia (HIT). Further, synthetic pentasaccharide has been found to offer advantages over current thromboprophylactic regimens in a number of patients undergoing major orthopedic surgery. Other studies have shown that pentasaccharide is more effective for overall VTE in comparison with LMW heparin, though it was also associated with an increased rate of major bleeding. Synthetic, selective, and direct inhibitors to FXa, such as DX-9065a, are highly potent and orally bioavailable antithrombotic agents that have demonstrated an improved side effect profile, probably by allowing sufficient thrombin to remain for platelet activation and normal hemostasis, while preventing pathological thrombus formation. For thrombosis therapy, the most desirable type of antithrombotic agent is an orally active drug that has a broad range of effective doses and no hemorrhagic side effects. Presently, many types of direct inhibitors are in various stages of clinical trials and expected to provide significant benefits as compared to currently utilized therapy strategies.

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