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2023
This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
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This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
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Edoxaban, a Novel Oral Factor Xa Inhibitor
Annals of Pharmacotherapy, 2015Objective: To evaluate the current literature and potential clinical role of edoxaban (Savaysa) for stroke prevention in nonvalvular atrial fibrillation (NVAF) and treatment of deep-vein thrombosis and pulmonary embolism. Data Sources: A PubMed and Cochrane Central Register of Controlled trials search was conducted in February2015 using the search ...
Katie B. Tellor +2 more
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Factor Xa Inhibitors in the Control of Thrombogenesis [PDF]
Hämostaseologie, 1999 SummaryIt is now well recognized that drugs with sole anti-Xa activity are capable of producing antithrombotic effects. The basic and clinical studies with pentasaccharide have validated this hypothesis. Synthetic heparin pentasaccharide is currently undergoing clinical trials in the prophylaxis of DVT in orthopedic surgery.
Walter Jeske +4 more
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Design and synthesis of factor Xa inhibitors and their prodrugs
Bioorganic & Medicinal Chemistry Letters, 2003In addition to our previously reported fluoro acrylamides Xa inhibitors 2 and 3, a series of potent and novel cyclic diimide amidine compounds has been identified. In efforts to improve their oral bioavailability, replacement of the amidine group with methyl amidrazone gives compounds of moderate potency (14, IC(50)=0.028 microM).
Willy Teng +11 more
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Progress in the discovery of Factor Xa inhibitors
Expert Opinion on Therapeutic Patents, 2006Factor Xa is a serine protease that has a critical role in the blood coagulation cascade by ultimately regulating the production of thrombin. There is now ample evidence for the role of Factor Xa inhibitors as anticoagulants and they represent potential new therapeutic agents for the treatment and prevention of arterial and venous thrombosis.
Danette Dudley +5 more
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Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2003Factor Xa (fXa) is an important serine protease in the blood coagulation cascade. Inhibition of fXa has emerged as an attractive target for potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein, we describe a series of non-benzamidine isoxazoline derivatives as fXa inhibitors.
Christopher D. Ellis +10 more
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Managing transitions from oral factor Xa inhibitors to unfractionated heparin infusions.
American Journal of Health-System Pharmacy, 2016PURPOSE Published evidence regarding the effects of oral factor Xa inhibitors on anticoagulation monitoring tests is reviewed with a focus on monitoring concerns that can arise during transitions to i.v. heparin therapy.
Andrew C. Faust +2 more
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Factor Xa inhibitors for acute coronary syndromes
Cochrane Database of Systematic Reviews, 2011The activation of coagulation mechanisms plays a central role in the pathogenesis of acute coronary syndromes (ACS). Administration of unfractionated heparin (UFH) and low molecular weight heparins (LMWH), agents preventing the progression of thrombus formation, is a crucial therapeutic strategy.
Joey Kwong +2 more
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[Heparin, thrombin and Factor Xa inhibitors].
Hamostaseologie, 2004Direct and indirect coagulation inhibitors are used to inhibit the activity of the serine proteases of the coagulation system. Indirect inhibitors act via antithrombin and heparin cofactor II. The main representatives are heparins, lowmolecular-weight heparins, fondaparinux, idraparinux and danaparoid.
T Fenyvesi, J Harenberg
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Inhibitors of Thrombin and Factor Xa
2000In medicine today, much effort is being made to develop new protease inhibitors for use as anticoagulants in multiple disease states. Deep venous thrombosis and pulmonary embolism, in particular, are major medical problems in the developed world. Similarly, myocardial infarction, stroke, and peripheral vascular disease are arterial thromboses for which
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