| Name | Factor Xa |
|---|---|
| Synonyms | Coagulation factor X; F10; Fx; Coagulation factor X precursor; FXA; Factor Xa; Prothrombinase; Stuart factor… |
| Name | warfarin |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18956996 | Baetz BE, Spinler SA: Dabigatran etexilate: an oral direct thrombin inhibitor for prophylaxis and treatment of thromboembolic diseases. Pharmacotherapy. 2008 Nov;28(11):1354-73. As the only oral anticoagulation option available in the United States, warfarin use remains widespread. Additional anticoagulation options include unfractionated low-molecular-weight heparins (e.g., and tinzaparin), and the indirect-acting factor Xa inhibitor, fondaparinux. |
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| 19505271 | Ageno W: Rivaroxaban for the prevention of venous thromboembolism following major orthopedic surgery: the RECORD trials. Expert Rev Cardiovasc Ther. 2009 Jun;7(6):569-76. These include parenteral anticoagulants such as the low-molecular-weight heparins or fondaparinux and oral anticoagulants such as warfarin. Rivaroxaban is the first of a new class of anticoagulants: the selective, direct Factor Xa inhibitors. |
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| 19222611 | Khoo CW, Tay KH, Shantsila E, Lip GY: Novel oral anticoagulants. Int J Clin Pract. 2009 Apr;63(4):630-41. Epub 2009 Feb 16. The antagonists (VKAs), such as warfarin, have been around for the last 65 years and its efficacy as thromboprophylaxis remained largely unchallenged, at least until recently. The novel oral anticoagulants are in 2 broad drug classes - the oral direct thrombin inhibitors and oral factor Xa inihibitors. |
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| 19185786 | Drouet L: [Rivaroxaban: mode of action] . Ann Fr Anesth Reanim. 2008 Dec;27 Suppl 3:S9-15. The targeting of factor-Xa factor, key component in the coagulation cascade, has the theoretical benefit of being an effective antithrombotic and a potential risk for hemorrhage, both highly dose-dependent. |
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| 18465493 | Robins P: Anticoagulation strategies. IDrugs. 1998 May;1(1):13-6. A number of individual presentations at this meeting dealt with the burgeoning field of anticoagulation strategies, and the fourth day (Wednesday) provided one of the most interesting symposia of the meeting, entitled 'Anticoagulation Strategies: Thrombin and Factor Xa Inhibition'. Chair RR Wexler (DuPont Merck, PA, USA) pointed out that classical anticoagulants, such as warfarin, suffer from poor oral bioavailability, lack of selectivity and short plasma half-life. |
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| 18302088 | Linkins LA, Warkentin TE: The approach to heparin-induced thrombocytopenia. . Semin Respir Crit Care Med. 2008 Feb;29(1):66-74. (e.g., warfarin) are therefore contraindicated during the acute (thrombocytopenic) phase of HIT. Treatment of HIT emphasizes substitution of with an alternative nonheparin anticoagulant, such as a direct thrombin inhibitor (lepirudin, argatroban), or an indirect (antithrombin-mediated) inhibitor of factor Xa (danaparoid, fondaparinux?). |
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| 20203456 | Osinbowale O, Ali L, Chi YW: Venous thromboembolism: a clinical review. Postgrad Med. 2010 Mar;122(2):54-65. Alternative oral anticoagulants, such as direct thrombin inhibitors and factor Xa inhibitors, are subjects of active research in alternative agents for oral anticoagulation, and have been recently approved for prophylaxis in Canada and the European Union. Warfarin is the only oral anticoagulant approved by the US Food and Drug Administration. |
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| 18425569 | Umer Usman MH, Raza S, Raza S, Ezekowitz M: Advancement in antithrombotics for stroke prevention in atrial fibrillation. J Interv Card Electrophysiol. 2008 Aug;22(2):129-37. Epub 2008 Apr 17. The current standard of therapy includes warfarin, acenocoumarol and phenprocoumon which have proven efficacy by reducing stroke by 68% against placebo. Newer agents such as direct thrombin inhibitors, factor Xa inhibitors, factor IX inhibitors, tissue factor inhibitors and a novel antagonist are being developed to overcome the limitations of current agents. |
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| 20040270 | Zikria J, Ansell J: Oral anticoagulation with Factor Xa and thrombin inhibitors: Is there an alternative to warfarin?. Discov Med. 2009 Dec;8(43):196-203. |
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| 20211293 | : Rivaroxaban-once daily, oral, direct factor Xa inhibition compared with antagonism for prevention of stroke and Embolism Trial in Atrial Fibrillation: rationale and design of the ROCKET AF study. Am Heart J. 2010 Mar;159(3):340-347.e1. Rivaroxaban is an oral direct factor Xa inhibitor in advanced development as an alternative to warfarin for the prevention and treatment of thromboembolic disorders. |
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| 18296593 | Gross PL, Weitz JI: New anticoagulants for treatment of venous thromboembolism. . Arterioscler Thromb Vasc Biol. 2008 Mar;28(3):380-6. Extended treatment usually involves the administration of antagonists, such as warfarin. These agents include idraparinux, a long-acting synthetic pentasaccharide that is given subcutaneously on a once-weekly basis, and new oral anticoagulants that target thrombin or factor Xa. |
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| 20062934 | Weitz JI: New oral anticoagulants in development. Thromb Haemost. 2010 Jan;103(1):62-70. Epub 2009 Oct 26. antagonists, such as warfarin, are administered orally, but produce a variable anticoagulant response because genetic polymorphisms, dietary intake and multiple drug-drug interactions affect their metabolism. These limitations have prompted the development of new oral anticoagulants that target thrombin or factor Xa and can be given in fixed doses without coagulation monitoring. |
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| 20234784 | Maegdefessel L, Azuma J, Tsao PS: Modern role for in management of atrial fibrillation and stroke reduction. Vasc Health Risk Manag. 2010 Mar 3;6:95-103. Treatment regimens for preventing thromboembolism in AF patients range from antagonists such as warfarin or coumadins, antiplatelet drugs like or to newly developed orally available antithrombotics like the direct thrombin inhibitor dabigatran, or the Factor Xa-inhibitor rivaroxaban. |
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| 18257025 | Savelieva I, Camm J: Update on atrial fibrillation: part I. Clin Cardiol. 2008 Feb;31(2):55-62. The limitations of warfarin prompted the development of new antithrombotic drugs, which include anticoagulants, such as direct oral thrombin inhibitors (dabigatran) and factor Xa inhibitors (rivaroxaban, apixaban). |
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| 20170841 | Hankey GJ, Eikelboom JW: Antithrombotic drugs for patients with ischaemic stroke and transient ischaemic attack to prevent recurrent major vascular events. Lancet Neurol. 2010 Mar;9(3):273-84. The direct thrombin inhibitor, dabigatran etexilate, has shown efficacy over warfarin in a recent trial. Other new anticoagulants, including the oral factor Xa inhibitors, rivaroxaban, apixaban, and edoxaban, the parenteral factor Xa inhibitor, idrabiotaparinux, and the novel VKA, tecarfarin, are currently being assessed. |
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| 18814828 | Usman MH, Notaro LA, Patel H, Ezekowitz MD: New developments in anticoagulation for atrial fibrillation. Curr Treat Options Cardiovasc Med. 2008 Sep;10(5):388-97. Warfarin reduces this incidence by two thirds and is the most effective agent for this indication. The direct thrombin inhibitor dabigatran is furthest along in clinical development, followed by the factor Xa inhibitors rivaroxaban and apixaban. |
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| 20211292 | Lopes RD, Alexander JH, Al-Khatib SM, Ansell J, Diaz R, Easton JD, Gersh BJ, Granger CB, Hanna M, Horowitz J, Hylek EM, McMurray JJ, Verheugt FW, Wallentin L: Apixaban for reduction in stroke and other ThromboemboLic events in atrial fibrillation (ARISTOTLE) trial: design and rationale. Am Heart J. 2010 Mar;159(3):331-9. The primary objective of ARISTOTLE is to determine if the factor Xa inhibitor, apixaban, is noninferior to warfarin at reducing the combined endpoint of stroke (ischemic or hemorrhagic) and systemic embolism in patients with AF and at least 1 additional risk factor for stroke. |
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| 19448531 | Kaplinska K, Mielicki WP: Direct analysis reveals an absence of gamma-carboxyglutamic acid in cancer procoagulant from human tissues. Blood Coagul Fibrinolysis. 2009 Jul;20(5):315-20. Cancer procoagulant, a direct blood coagulation factor X activator from malignant tissue, is considered as a -dependent protein, so it could serve as one of possible targets for the therapy with warfarin. |
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| 20101880 | Balaratnam S: Prevention and treatment of thromboembolic events in medical patients and new anticoagulants. Acta Clin Belg. 2009 Nov-Dec;64(6):547-52. The advent of more recent treatments such as factor Xa inhibitors and direct thrombin inhibitors may help to provide more conclusive preventative management of patients are risk of VTE. |
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| 18594479 | Hammwohner M, Goette A: Will warfarin soon be passe? New approaches to stroke prevention in atrial fibrillation. J Cardiovasc Pharmacol. 2008 Jul;52(1):18-27. Nevertheless, warfarin therapy has several limitations; therefore, new anticoagulants like warfarin analogs, thrombin inhibitors, or factor Xa inhibitors have been developed. |
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| 18520714 | Verheugt FW: Long-term anticoagulation in patients with coronary disease, and future developments. Curr Opin Cardiol. 2008 Jul;23(4):315-9. In addition, oral direct factor Xa blockers are also good candidates for replacing warfarin. |
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| 19342840 | Marti-Fabregas J, Mateo J: Old and new anticoagulant agents for the prevention and treatment of patients with ischemic stroke. Cerebrovasc Dis. 2009;27 Suppl 1:111-9. Epub 2009 Apr 3. Although ximelagatran was withdrawn early because of liver toxicity, it provided convincing evidence that new oral anticoagulants have the potential to replace warfarin. The new anticoagulants that are being investigated target factor Xa or thrombin. |
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| 19665679 | Ng VL: Anticoagulation monitoring. Clin Lab Med. 2009 Jun;29(2):283-304. This article reviews the commonly used anticoagulants (warfarin and and associated recommended laboratory testing. The newer anticoagulants analogs, direct factor Xa inhibitors, and direct thrombin inhibitors) and various applied coagulation laboratory testing and related issues are also discussed. |
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| 19550318 | Zikria JC, Ansell J: Oral anticoagulation with factor Xa and thrombin inhibitors: on the threshold of change. Curr Opin Hematol. 2009 Sep;16(5):347-56. Within the next few years, the treatment of arterial and venous thromboembolism is again poised to undergo a major change with the introduction of new oral anticoagulants that are likely to fulfill many of the unmet needs of current warfarin therapy. |
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| 19102516 | Levin A, Ben-Artzi M, Beckerman P, Haber G, Varon D, Ben-Yehuda A, Muszkat M: Factors associated with bleeding in elderly hospitalized patients treated with : a prospective, open-label, observational study. Drugs Aging. 2009;26(1):77-85. doi: 10.2165/0002512-200926010-00006. OBJECTIVE: To evaluate whether weight, age and renal function are associated with anti-factor Xa activity and with bleeding in elderly patients treated with |
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| 19012508 | Carreiro J, Ansell J: Apixaban, an oral direct Factor Xa inhibitor: awaiting the verdict. Expert Opin Investig Drugs. 2008 Dec;17(12):1937-45. For the last half-century, despite its many limitations warfarin has been the mainstay of treatment for patients with venous and arterial thromboembolic disease. |
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| 20135753 | Chan VH, Monagle P, Massicotte P, Chan AK: Novel paediatric anticoagulants: a review of the current literature. Blood Coagul Fibrinolysis. 2010 Mar;21(2):144-51. There are many limitations with respect to anticoagulants currently used in standard paediatric practice for prophylaxis and treatment of thrombosis: low molecular-weight heparin, and warfarin. In this review, we discuss several promising direct thrombin inhibitors and factor Xa inhibitors, and synthesize relevant drug information and clinical experience from the limited available case reports, case series, and nonrandomized dose-finding trials published to date. |
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| 20135071 | Ufer M: Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar 1;103(3):572-85. Epub 2010 Feb 2. Therapeutic oral anticoagulation is still commonly achieved by administration of warfarin or other antagonists that are associated with an untoward pharmacokinetic / pharmacodynamic (PK/PD) profile leading to a high incidence of bleeding complications or therapeutic failure. Of these, the thrombin inhibitor dabigatran and factor Xa inhibitor rivaroxaban have recently been licensed for thromboprophylaxis after orthopaedic surgery mainly in Europe. |
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| 18507371 | Imaeda Y, Kuroita T, Sakamoto H, Kawamoto T, Tobisu M, Konishi N, Hiroe K, Kawamura M, Tanaka T, Kubo K: Discovery of imidazo [1,5-c] -3-ones: weakly basic, orally active factor Xa inhibitors. J Med Chem. 2008 Jun 26;51(12):3422-36. Epub 2008 May 29. Compound 3q showed favorable oral bioavailability in rats and monkeys under both fasted and fed conditions and antithrombotic efficacy in a rat model of venous thrombosis after oral administration, without a significant increase in bleeding time (unlike warfarin). |
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| 20211294 | Eikelboom JW, O'Donnell M, Yusuf S, Diaz R, Flaker G, Hart R, Hohnloser S, Joyner C, Lawrence J, Pais P, Pogue J, Synhorst D, Connolly SJ: Rationale and design of AVERROES: apixaban versus to prevent stroke in atrial fibrillation patients who have failed or are unsuitable for antagonist treatment. Am Heart J. 2010 Mar;159(3):348-353.e1. The novel oral factor Xa inhibitor, apixaban, is being developed for prevention of stroke in AF. A noninferiority trial of apixaban versus a VKA (warfarin) is being conducted but does not address the large unmet need of AF patients at risk of stroke who are unsuitable for or unwilling to take a VKA. |
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| 18393143 | Fareed J, Hoppensteadt DA, Fareed D, Demir M, Wahi R, Clarke M, Adiguzel C, Bick R: Survival of heparins, oral anticoagulants, and after the year 2010. Semin Thromb Hemost. 2008 Feb;34(1):58-73. Both the anti-factor Xa and antithrombin agents have been developed for oral use and have provided impressive clinical outcomes in sponsor trials for the postsurgical prophylaxis of venous thrombosis; however, safety concerns related to liver enzyme elevations and thrombosis rebound have been reported with their use. Warfarin provides a convenient and affordable approach in the long-term outpatient management of thrombotic disorders. |
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| 18315548 | Wong PC, Crain EJ, Xin B, Wexler RR, Lam PY, Pinto DJ, Luettgen JM, Knabb RM: Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost. 2008 May;6(5):820-9. Epub 2008 Feb 25. In vivo, the values for antithrombotic ED (50) (dose that reduced thrombus weight or increased blood flow by 50% of the control) in AVST, VT and ECAT and the values for BT ED (3x) (dose that increased BT by 3-fold) were 0.27 +/- 0.03, 0.11 +/- 0.03, 0.07 +/- 0.02 and > 3 mg kg (-1) h (-1) i.v. for apixaban, 0.05 +/- 0.01, 0.05 +/- 0.01, 0.27 +/- 0.08 and > 3 mg kg (-1) h (-1) i.v. for the indirect FXa inhibitor fondaparinux, and 0.53 +/- 0.04, 0.27 +/- 0.01, 0.08 +/- 0.01 and 0.70 +/- 0.07 mg kg (-1) day (-1) p.o. for the oral anticoagulant warfarin, respectively. |
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| 18302091 | Hoppensteadt DA, Jeske W, Walenga J, Fareed J: The future of anticoagulation. Semin Respir Crit Care Med. 2008 Feb;29(1):90-9. Both the factor Xa and antithrombin agents have been developed for oral use and some of these agents are in clinical development. The oral anticoagulants such as warfarin provide a convenient and affordable approach in the long-term outpatient management of thrombotic disorders. |
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| 19351313 | Verma AK, Brighton TA: The direct factor Xa inhibitor rivaroxaban. Med J Aust. 2009 Apr 6;190(7):379-83. Warfarin and are the traditional mainstay anticoagulant therapies for treating thromboembolic disease. |
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| 20337579 | Benmira S, Banda ZK, Bhattacharya V: Old Versus New Anticoagulants: Focus on Pharmacology. Recent Pat Cardiovasc Drug Discov. 2010 Mar 26. low molecular weight heparin (LMWH) and warfarin are well-established anticoagulants still in widespread use despite their well known drawbacks. The major examples of these newer anticoagulants are the direct and indirect factor Xa inhibitors and the direct thrombin inhibitors. |
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| 20181379 | Salmela B, Joutsi-Korhonen L, Saarela E, Lassila R: Comparison of monitoring methods for lepirudin: Impact of warfarin and lupus anticoagulant. Thromb Res. 2010 Feb 23. Wide dose-responses to lepirudin (0-4.0microg/ml) were studied with APTT (Actin FSL ((R))), Ecarin Chromogenic Assay (ECA ((R))), chromogenic Anti-Factor IIa (Anti-FIIa, Hirudin Activity Assay ((R))), Prothrombinase-induced Clotting Time (PiCT ((R))), and plasma diluted Thrombin Time (dTT). |
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| 18491993 | Piccini JP, Patel MR, Mahaffey KW, Fox KA, Califf RM: Rivaroxaban, an oral direct factor Xa inhibitor. . Expert Opin Investig Drugs. 2008 Jun;17(6):925-37. The drug may have its greatest impact in providing a much-needed and attractive alternative to warfarin. |
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| 20124518 | Morell J, Sullivan B, Khalabuda M, McBride BF: Role of Orally Available Antagonists of Factor Xa in the Treatment and Prevention of Thromboembolic Disease: Focus on Rivaroxaban. J Clin Pharmacol. 2010 Feb 2. Interpatient variability in the safety and efficacy of oral anticoagulation with warfarin presents several challenges to clinicians, thus underscoring the emergent need for new orally available anticoagulants with predictable pharmacokinetic and pharmacodynamic profiles and ability to target circulating clotting factors. |
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| 19739042 | Sobieraj-Teague M, O'Donnell M, Eikelboom J: New anticoagulants for atrial fibrillation. Semin Thromb Hemost. 2009 Jul;35(5):515-24. Epub 2009 Sep 8. Most are small synthetic molecules that target factor IIa (e.g., dabigatran etexilate, AZD-0837) or factor Xa (e.g., rivaroxaban, apixaban, betrixaban, DU176b, idrabiotaparinux). A new antagonist (ATI-5923) with improved pharmacological properties compared with warfarin is also being evaluated in a phase III trial. |
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| 20179722 | Verheugt FW: Novel oral anticoagulants to prevent stroke in atrial fibrillation. Nat Rev Cardiol. 2010 Mar;7(3):149-54. Warfarin reduces the risk of stroke in atrial fibrillation by around 60%, while antiplatelet therapy is much less effective. Oral agents have been developed that directly inhibit the activity of thrombin (factor IIa), as well as drugs that directly block activated factor X (factor Xa), which is the first enzyme in the final common pathway to the activation of thrombin. |
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| 20131309 | Castellone DD, Van Cott EM: Laboratory monitoring of new anticoagulants. Am J Hematol. 2010 Mar;85(3):185-7. There are now a variety of new anticoagulant drugs in clinical use including several direct thrombin inhibitors (DTIs), such as argatroban, bivalirudin, and hirudin, as well as a Factor Xa inhibitor, fondaparinux. In addition, laboratory testing can assist with transitioning patients from DTI to warfarin therapy. |
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| 19365276 | De Caterina R, Kristensen SD, Renda G: New anticoagulants for atrial fibrillation. J Cardiovasc Med. 2009 Jun;10(6):446-53. Although warfarin and other antagonists have clearly the greatest efficacy among treatments commonly available in preventing stroke in atrial fibrillation, their use is associated with a substantial risk of major bleedings and are unpractical and difficult to use because of their narrow therapeutic window, their interaction with drugs and foods, and the need of frequent coagulation monitoring. These drugs fall in different pharmacological categories of oral direct thrombin inhibitors, parenteral long-lived indirect factor Xa inhibitors, and oral direct factor Xa inhibitors. |
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| 19074090 | Young G: New anticoagulants in children. Hematology Am Soc Hematol Educ Program. 2008:245-50. The most widely used agents in children are low-molecular-weight heparins (LMWH), and warfarin. Novel anticoagulants such as direct thrombin inhibitors and the selective factor Xa inhibitor, fondaparinux, have been approved for use in adults and have properties that suggest they may be safer and more efficacious than the standard agents; however, until recently, publications using these agents in children were limited to case reports. |
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| 19741508 | Fernlof G, Sjostrom BM, Lindell KM, Wall UE: Management of major bleedings during anticoagulant treatment with the oral direct thrombin inhibitor ximelagatran or warfarin. Blood Coagul Fibrinolysis. 2009 Sep 7. Several new oral anticoagulants are currently investigated in phase III programmes, mainly with inhibition of factor Xa or thrombin as their pharmacological target. |
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| 18506123 | Fareed J, Iqbal O, Cunanan J, Demir M, Wahi R, Clarke M, Adiguzel C, Bick R: Changing trends in anti-coagulant therapies. Int Angiol. 2008 Jun;27(3):176-92. Warfarin provides a convenient and affordable approach in the long-term outpatient management of thrombotic disorders. Both the anti-factor Xa and anti-IIa agents have been developed for oral use and have provided impressive clinical results. |
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| 20201481 | Friedman RJ: New oral anticoagulants for thromboprophylaxis after total hip or knee arthroplasty. Orthopedics. 2009 Dec;32(12 Suppl):79-84. doi: 10.3928/01477447-20091103-53. Conventional anticoagulants have several short-comings: for example, warfarin requires regular coagulation monitoring and low-molecular-weight heparins are inconvenient to use because they require subcutaneous administration. The development of new anticoagulants has focused on 2 classes of compounds: direct thrombin inhibitors and direct factor Xa inhibitors. |
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