Novel factor Xa inhibitors for prevention and treatment of thromboembolic diseases

Bibliography

• GEERTS WH, PINEO GF, HEIT JA et al.: Prevention of venous thromboembolism: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):338S-400S.
   PubMed Web of Science ®Google Scholar
• BULLER HR, AGNELLI G, HULL RD et al.: Antithrombotic therapy for venous thromboembolic disease: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):401S-428S.
   PubMedGoogle Scholar
• SINGER DE, ALBERS GW, DALEN JE et al.: Antithrombotic therapy in atrial fibrillation: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):429S-456S.
   PubMedGoogle Scholar
• HARRINGTON RA, BECKER RC, EZEKOWITZ M et al.: Antithrombotic therapy for coronary artery disease: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):513S-548S.
   PubMed Web of Science ®Google Scholar
• POPMA JJ, BERGER P, OHMAN EM et al.: Antithrombotic therapy during percutaneous coronary intervention: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):576S-599S.
   PubMed Web of Science ®Google Scholar
• DI NISIO M, MIDDELDORP S, BULLER HR: Direct thrombin inhibitors. N. Engl. J. Med. (2005) 353(10):1028-1040.
   PubMed Web of Science ®Google Scholar
• ALBERS GW, DIENER HC, FRISON L et al.: Ximelagatran versus warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a randomized trial. J. Am. Med. Assoc. (2005) 293(6):690-698.
   PubMed Web of Science ®Google Scholar
• ERIKSSON BI, AGNELLI G, COHEN AT et al.: Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement. Thromb. Haemost. (2003) 89(2):288-296.
   PubMed Web of Science ®Google Scholar
• OLSSON SB: Stroke prevention with the oral direct thrombin inhibitor ximelagatran compared with warfarin in patients with non-valvular atrial fibrillation (SPORTIF III): randomised controlled trial. Lancet (2003) 362(9397):1691-1698.
   PubMed Web of Science ®Google Scholar
• ERIKSSON BI, DAHL OE, BULLER HR et al.: A new oral direct thrombin inhibitor, dabigatran etexilate, compared with enoxaparin for prevention of thromboembolic events following total hip or knee replacement: the BISTRO II randomized trial. J. Thromb. Haemost. (2005) 3(1):103-111.
   PubMed Web of Science ®Google Scholar
• STANGIER J, NEHMIZ G, REILLY P et al.: Pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor dabigatran in a dose finding trial in atrial fibrillation. J. Thromb. Haemost. (2005) 3(S1):OR271.
   Google Scholar
• MANN KG, BRUMMEL K, BUTENAS S: What is all that thrombin for? J. Thromb. Haemost. (2003) 1(7):1504-1514.
   PubMed Web of Science ®Google Scholar
• HIRSH J, RASCHKE R: Heparin and low-molecular-weight heparin: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest (2004) 126(Suppl. 3):188S-203S.
   PubMed Web of Science ®Google Scholar
• FAREED J, HOPPENSTEADT D, WALENGA J et al.: Pharmacodynamic and pharmacokinetic properties of enoxaparin: implications for clinical practice. Clin. Pharmacokinet. (2003) 42(12):1043-1057.
   PubMed Web of Science ®Google Scholar
• MATTHIASSON SE, LINDBLAD B, STJERNQUIST U, BERGQVIST D: The haemorrhagic effect of low molecular weight heparins, dermatan sulphate and hirudin. Haemostasis (1995) 25(5):203-211.
   PubMedGoogle Scholar
• AMIRAL J, LORMEAU JC, MARFAING-KOKA A et al.: Absence of cross-reactivity of SR90107A/ORG31540 pentasaccharide with antibodies to heparin–PF4 complexes developed in heparin-induced thrombocytopenia. Blood Coagul. Fibrinolysis (1997) 8(2):114-117.
   PubMed Web of Science ®Google Scholar
• HOWARD AW, AARON SD: Low molecular weight heparin decreases proximal and distal deep venous thrombosis following total knee arthroplasty. A meta-analysis of randomized trials. Thromb. Haemost. (1998) 79(5):902-906.
   PubMed Web of Science ®Google Scholar
• PLANES A, VOCHELLE N, MAZAS F et al.: Prevention of postoperative venous thrombosis: a randomized trial comparing unfractionated heparin with low molecular weight heparin in patients undergoing total hip replacement. Thromb. Haemost. (1988) 60(3):407-410.
   PubMed Web of Science ®Google Scholar
• TURPIE AG, BAUER KA, ERIKSSON BI, LASSEN MR: Fondaparinux versus enoxaparin for the prevention of venous thromboembolism in major orthopedic surgery: a meta-analysis of 4 randomized double-blind studies. Arch. Intern. Med. (2002) 162(16):1833-1840.
   PubMed Web of Science ®Google Scholar
• BULLER HR, DAVIDSON BL, DECOUSUS H et al.: Fondaparinux or enoxaparin for the initial treatment of symptomatic deep venous thrombosis: a randomized trial. Ann. Intern. Med. (2004) 140(11):867-873.
   PubMed Web of Science ®Google Scholar
• LEADLEY RJ Jr: Coagulation factor Xa inhibition: biological background and rationale. Curr. Top. Med. Chem. (2001) 1(2):151-159.
   PubMedGoogle Scholar
• EISENBERG PR, SIEGEL JE, ABENDSCHEIN DR, MILETICH JP: Importance of factor Xa in determining the procoagulant activity of whole-blood clots. J. Clin. Invest. (1993) 91(5):1877-1883.
   PubMed Web of Science ®Google Scholar
• REZAIE AR: Prothrombin protects factor Xa in the prothrombinase complex from inhibition by the heparin–antithrombin complex. Blood (2001) 97(8):2308-2313.
   PubMed Web of Science ®Google Scholar
• BRUFATTO N, NESHEIM ME: The use of prothrombin (S525C) labeled with fluorescein to directly study the inhibition of prothrombinase by antithrombin during prothrombin activation. J. Biol. Chem. (2001) 276(21):17663-17671.
   PubMed Web of Science ®Google Scholar
• PERZBORN E, STRASSBURGER J, WILMEN A et al.: In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939 – an oral, direct factor Xa inhibitor. J. Thromb. Haemost. (2005) 3(3):514-521.
   PubMed Web of Science ®Google Scholar
• ANSELL J, BERGQVIST D: Current options in the prevention of thromboembolic disease. Drugs (2004) 64(Suppl. 1):1-5.
   PubMed Web of Science ®Google Scholar
• BONEU B, NECCIARI J, CARIOU R et al.: Pharmacokinetics and tolerance of the natural pentasaccharide (SR90107/Org31540) with high affinity to antithrombin III in man. Thromb. Haemost. (1995) 74(6):1468-1473.
   PubMed Web of Science ®Google Scholar
• FAAIJ RA, BURGGRAAF J, SCHOEMAKER RC, VAN AMSTERDAM RG, COHEN AF: Absence of an interaction between the synthetic pentasaccharide fondaparinux and oral warfarin. Br. J. Clin. Pharmacol. (2002) 54(3):304-308.
   PubMed Web of Science ®Google Scholar
• OLLIER C, FAAIJ RA, SANTONI A et al.: Absence of interaction of fondaparinux sodium with aspirin and piroxicam in healthy male volunteers. Clin. Pharmacokinet. (2002) 41(Suppl. 2):31-37.
   PubMed Web of Science ®Google Scholar
• MANT T, FOURNIE P, OLLIER C, DONAT F, NECCIARI J: Absence of interaction of fondaparinux sodium with digoxin in healthy volunteers. Clin. Pharmacokinet. (2002) 41(Suppl. 2):39-45.
   PubMed Web of Science ®Google Scholar
• BIJSTERVELD NR, MOONS AH, BOEKHOLDT SM et al.: Ability of recombinant factor VIIa to reverse the anticoagulant effect of the pentasaccharide fondaparinux in healthy volunteers. Circulation (2002) 106(20):2550-2554.
   PubMed Web of Science ®Google Scholar
• PAOLUCCI F, FRASA H, VAN AARLE F et al.: Two sensitive and rapid chromogenic assays of fondaparinux sodium (Arixtra) in human plasma and other biological matrices. Clin. Lab. (2003) 49(9-10):451-460.
   PubMedGoogle Scholar
• WALENGA JM, FAREED J, PETITOU M et al.: Intravenous antithrombotic activity of a synthetic heparin pentasaccharide in a human serum induced stasis thrombosis model. Thromb. Res. (1986) 43(2):243-248.
   PubMed Web of Science ®Google Scholar
• WALENGA JM, PETITOU M, LORMEAU JC et al.: Antithrombotic activity of a synthetic heparin pentasaccharide in a rabbit stasis thrombosis model using different thrombogenic challenges. Thromb. Res. (1987) 46(2):187-198.
   PubMed Web of Science ®Google Scholar
• WALENGA JM, BARA L, PETITOU M et al.: The inhibition of the generation of thrombin and the antithrombotic effect of a pentasaccharide with sole anti-factor Xa activity. Thromb. Res. (1988) 51(1):23-33.
   PubMed Web of Science ®Google Scholar
• WALENGA JM, JESKE WP, BARA L, SAMAMA MM, FAREED J: Biochemical and pharmacologic rationale for the development of a synthetic heparin pentasaccharide. Thromb. Res. (1997) 86(1):1-36.
   PubMed Web of Science ®Google Scholar
• LORMEAU JC, HERAULT JP: The effect of the synthetic pentasaccharide SR 90107/ORG 31540 on thrombin generation ex vivo is uniquely due to ATIII-mediated neutralization of factor Xa. Thromb. Haemost. (1995) 74(6):1474-1477.
   PubMed Web of Science ®Google Scholar
• BEGUIN S, CHOAY J, HEMKER HC: The action of a synthetic pentasaccharide on thrombin generation in whole plasma. Thromb. Haemost. (1989) 61(3):397-401.
   PubMed Web of Science ®Google Scholar
• LASSEN MR, BAUER KA, ERIKSSON BI, TURPIE AG: Postoperative fondaparinux versus preoperative enoxaparin for prevention of venous thromboembolism in elective hip-replacement surgery: a randomised double-blind comparison. Lancet (2002) 359(9319):1715-1720.
   PubMed Web of Science ®Google Scholar
• TURPIE AG, BAUER KA, ERIKSSON BI, LASSEN MR: Postoperative fondaparinux versus postoperative enoxaparin for prevention of venous thromboembolism after elective hip-replacement surgery: a randomised double-blind trial. Lancet (2002) 359(9319):1721-1726.
   PubMed Web of Science ®Google Scholar
• BAUER KA, ERIKSSON BI, LASSEN MR, TURPIE AG: Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after elective major knee surgery. N. Engl. J. Med. (2001) 345(18):1305-1310.
   PubMed Web of Science ®Google Scholar
• ERIKSSON BI, BAUER KA, LASSEN MR, TURPIE AG: Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip-fracture surgery. N. Engl. J. Med. (2001) 345(18):1298-1304.
   PubMed Web of Science ®Google Scholar
• ERIKSSON BI, LASSEN MR: Duration of prophylaxis against venous thromboembolism with fondaparinux after hip fracture surgery: a multicenter, randomized, placebo-controlled, double-blind study. Arch. Intern. Med. (2003) 163(11):1337-1342.
   PubMed Web of Science ®Google Scholar
• BULLER HR, DAVIDSON BL, DECOUSUS H et al.: Subcutaneous fondaparinux versus intravenous unfractionated heparin in the initial treatment of pulmonary embolism. N. Engl. J. Med. (2003) 349(18):1695-1702.
   PubMed Web of Science ®Google Scholar
• THE FIFTH ORGANIZATIONTO ASSESS STRATEGIES IN ACUTE ISCHEMIC SYNDROMES INVESTIGATORS: Comparison of fondaparinux and enoxaparin in acute coronary syndromes. N. Engl. J. Med. (2006) 354(14):1464-1476.
   PubMed Web of Science ®Google Scholar
• YUSUF S, MEHTA SR, CHROLAVICIUS S et al.: Effects of fondaparinux on mortality and reinfarction in patients with acute ST-segment elevation myocardial infarction: the OASIS-6 randomized trial. J. Am. Med. Assoc. (2006) 295(13):1519-1530.
   PubMed Web of Science ®Google Scholar
• FAAIJ RA, BURGGRAAF J, VAN AMSTERDAM RGM et al.: A Phase I single rising dose study to investigate the safety, tolerability and pharmacokinetics of idraparinux sodium in healthy young volunteers. In: The clinical pharmacology of novel antithrombotic compounds, Section 2, Chapter 6 (2005):79-94.
   Google Scholar
• AMSTERDAM R, FAAIJ RA, SCHOEMAKER RC et al.: The effect of age on the pharmacokinetics and effects of the long-acting synthetic pentasaccharide idraparinux sodium. In: The clinical pharmacology of novel antithrombotic compounds, Section 2, Chapter 7 (2005):95-108.
   Google Scholar
• FAAIJ RA, AMSTERDAM R, VAN MEEGEN E et al.: The multiple dose pharmacokinetics of the synthetic long-acting pentasaccharide idraparinux sodium in volunteers who recently completed treatment for venous thromboembolism. In: The clinical pharmacology of novel antithrombotic compounds, Section 2, Chapter 8 (2005):109-122.
   Google Scholar
• THE PERSIST INVESTIGATORS: A novel long-acting synthetic factor Xa inhibitor (SanOrg34006) to replace warfarin for secondary prevention in deep vein thrombosis. A Phase II evaluation. J. Thromb. Haemost. (2004) 2(1):47-53.
   PubMed Web of Science ®Google Scholar
• MURAYAMA N, TANAKA M, KUNITADA S et al.: Tolerability, pharmacokinetics, and pharmacodynamics of DX-9065a, a new synthetic potent anticoagulant and specific factor Xa inhibitor, in healthy male volunteers. Clin. Pharmacol. Ther. (1999) 66(3):258-264.
   PubMed Web of Science ®Google Scholar
• DYKE CK, BECKER RC, KLEIMAN NS et al.: First experience with direct factor Xa inhibition in patients with stable coronary disease: a pharmacokinetic and pharmacodynamic evaluation. Circulation (2002) 105(20):2385-2391.
   PubMed Web of Science ®Google Scholar
• BECKER RC, ALEXANDER JH, DYKE C et al.: Effect of the novel direct factor Xa inhibitor DX-9065a on thrombin generation and inhibition among patients with stable atherosclerotic coronary artery disease. Thromb. Res. (2006) 117(4):439-446.
   PubMed Web of Science ®Google Scholar
• ALEXANDER JH, DYKE CK, YANG H et al.: Initial experience with factor-Xa inhibition in percutaneous coronary intervention: the XaNADU-PCI pilot. J. Thromb. Haemost. (2004) 2(2):234-241.
   PubMed Web of Science ®Google Scholar
• ALEXANDER JH, YANG H, BECKER RC et al.: First experience with direct, selective factor Xa inhibition in patients with non-ST-elevation acute coronary syndromes: results of the XaNADU-ACS trial. J. Thromb. Haemost. (2005) 3(3):439-447.
   PubMed Web of Science ®Google Scholar
• PACCALY A, FRICK A, ROHATAGI S et al.: Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for Phase II/III simulation of exposure. J. Clin. Pharmacol. (2006) 46(1):37-44.
   PubMed Web of Science ®Google Scholar
• PACCALY A, OZOUX ML, CHU V et al.: Pharmacodynamic markers in the early clinical assessment of otamixaban, a direct factor Xa inhibitor. Thromb. Haemost. (2005) 94(6):1156-1163.
   PubMed Web of Science ®Google Scholar
• HINDER M: Anticoagulant and anti-platelet effects are maintained following coadministration of otamixaban, a direct factor Xa inhibitor, with tirofiban in healthy volunteers. Thromb. Haemost. (2005) 93(4):794-795.
   PubMed Web of Science ®Google Scholar
• HINDER M, FRICK A, ROSENBURG R et al.: Anticoagulant and anti-platelet effects are maintained following coadministration of otamixaban, a direct factor Xa inhibitor, and acetylsalicylic acid. Thromb. Haemost. (2006) 95(2):224-228.
   PubMed Web of Science ®Google Scholar
• KUBITZA D, BECKA M, VOITH B, ZUEHLSDORF M, WENSING G: Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor. Clin. Pharmacol. Ther. (2005) 78(4):412-421.
   PubMed Web of Science ®Google Scholar
• KUBITZA D, BECKA M, WENSING G, VOITH B, ZUEHLSDORF M: Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939-an oral, direct factor Xa inhibitor-after multiple dosing in healthy male subjects. Eur. J. Clin. Pharmacol. (2005) 61(12):873-880.
   PubMed Web of Science ®Google Scholar
• WEINZ C, BUETEHORN U, DAEHLER HP et al.: Pharmacokinetics of BAY 59-7939 – an oral, direct factor Xa inhibitor – in rats and dogs. Xenobiotica (2005) 35(9):891-910.
   PubMed Web of Science ®Google Scholar
• HARDER S, GRAFF J, HENTIG NV et al.: Effects of BAY 59-7939, an oral, direct factor Xa inhibitor, on thrombin generation in healthy volunteers. Blood (2003) 102:3003 (Abstract).
   PubMed Web of Science ®Google Scholar
• KUBITZA D, BECKA M, ZUEHLSDORF M, MUECK W: Effects of single-dose BAY 59-7939 – an oral, direct factor Xa inhibitor – in subjects with extreme body weight. Blood (2005) 106(11):1872 (Abstract).
   Google Scholar
• KUBITZA D, BECKA M, ZUEHLSDORF M, MUECK W: Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct factor Xa inhibitor, in healthy subjects. J. Clin. Pharmacol. (2006) 46(5):549-558.
   PubMed Web of Science ®Google Scholar
• KUBITZA D, BECKA M, ZUEHLSDORF M, MUECK W: No interaction between the novel, oral direct factor Xa inhibitor BAY 59-7939 and digoxin. J. Clin. Pharmacol. (2006) 46(6):702 (Abstract 11).
   Google Scholar
• KUBITZA D, MUECK W, BECKA M: The oral, direct factor Xa inhibitor BAY 59-7939 does not prolong the QTc interval. J. Clin. Pharmacol. (2006) 46(6):703 (Abstract 12).
   Google Scholar
• KUBITZA D, BECKA M, MUECK W, ZUEHLSDORF M: Aspirin has no effect on the safety, tolerability, pharmacodynamics and pharmacokinetics of BAY 59-7939 – an oral, direct factor Xa inhibitor. J. Thromb. Haemost. (2005) 3(Suppl. 1):P1105.
   Google Scholar
• KUBITZA D, BECKA M, MUECK W, ZUEHLSDORF M: Naproxen has no relevant effect on the safety, tolerability, pharmacodynamics, and pharmacokinetics of BAY 59-7939 – an oral, direct factor Xa inhibitor. Blood (2005) 106(11):1873 (Abstract).
   Google Scholar
• KUBITZA D, BECKA M, VOITH B, ZUEHLSDORF M: Effect of enoxaparin on the safety, tolerability, pharmacodynamics and pharmacokinetics of BAY 59-7939 – an oral, direct factor Xa inhibitor. J. Thromb. Haemost. (2005) 3(Suppl. 1):P1704.
   Google Scholar
• ERIKSSON BI, BORRIS L, DAHL OE et al.: Oral, direct factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement. J. Thromb. Haemost. (2006) 4(1):121-128.
   PubMed Web of Science ®Google Scholar
• TURPIE AG, FISHER WD, BAUER KA et al.: BAY 59-7939: an oral, direct factor Xa inhibitor for the prevention of venous thromboembolism in patients after total knee replacement. A Phase II dose-ranging study. J. Thromb. Haemost. (2005) 3(11):2479-2486.
   PubMed Web of Science ®Google Scholar
• HUISMAN MV, BORRIS LC, DAHL OE et al.: An oral, direct factor Xa inhibitor, rivaroxaban: once-daily regimen for thromboprophylaxis after hip replacement. Pathophysiol. Haemost. Thromb. (2006) 35(1-2):A1 (Abstract 1163).
   Web of Science ®Google Scholar
• TURPIE AGG, ERIKSSON BI, MUECK W et al.: Pharmacokinetic and pharmacodynamic analyses of rivaroxaban in patients undergoing orthopaedic surgery. Pathophysiol. Haemost. Thromb. (2006) 35(1-2):A2 (Abstract 1182).
   Google Scholar
• SWAMINATHAN A, FROST C, KNABB R et al.: Pharmacokinetic and pharmacodynamic characteristics in healthy volunteers of razaxaban, an orally-active, potent, selective inhibitor of factor Xa. Clin. Pharmacol. Ther. (2004) 75(2):6-PI-12.
   Web of Science ®Google Scholar
• LASSEN MR, DAVIDSON BL, GALLUS AS et al.: A Phase II randomized, double-blind, five-arm, parallel-group, dose-response study of a new oral directly-acting factor Xa inhibitor, razaxaban, for the prevention or deep vein thrombosis in knee replacement surgery. Blood (2003) 102(11):41.
   Google Scholar
• AGNELLI G, HAAS SK, KRUEGER KA, BEDDING AW, BRANDT JT: A Phase II study of the safety and efficacy of a novel oral fXa inhibitor (LY517717) for the prevention of venous thromboembolism following TKR or THR. Blood (2005) 106(11):278 (Abstract).
   Google Scholar
• ERIKSSON BI, TURPIE AGG, LASSEN MR et al.: YM150, an oral direct factor Xa inhibitor, as prophylaxis for venous thromboembolism in patients with elective primary hip replacement surgery. a dose escalation study. Blood (2005) 106(11):1865 (Abstract).
   Google Scholar
• MORISHIMA Y, FURUGOHRI T, ISOBE K et al.: In vitro characteristics, anticoagulant effects and in vivo antithrombotic efficacy of a novel, potent and orally active direct factor Xa inhibitor, DU-176b. ASH Annual Meeting Abstracts (2004) 104(11):1862.
   Google Scholar
• ZAFAR MU, GAZTANGA J, VELEZ M et al.: A phase-I study to assess the antithrombotic properties of Du-176b: an orally active direct factor-Xa inhibitor. J. Am. Coll. Cardiol. (2006) 47(4):288A (Abstract 908-161).
   Google Scholar
• CALATZIS A, SPANNAGL M, GEMPELER-MESSINA P et al.: The prothrombinase-induced clotting test: a new technique for the monitoring of anticoagulants. Haemostasis (2000) 30(Suppl. 2):172-174.
   Google Scholar
• SAMAMA MM, GEROTZIAFAS GT: Evaluation of the pharmacological properties and clinical results of the synthetic pentasaccharide (fondaparinux). Thromb. Res. (2003) 109(1):1-11.
   PubMed Web of Science ®Google Scholar