New anticoagulants

Weitz, 1997, Low‐molecular‐weight heparins, N Engl J Med, 337, 688, 10.1056/NEJM199709043371007 Gould, 1999, Low‐molecular‐weight heparins compared with unfractionated heparin for treatment of deep venous thrombosis. A meta‐analysis of randomized controlled trials, Ann Intern Med, 130, 800, 10.7326/0003-4819-130-10-199905180-00003 Gould, 1999, Low‐molecular‐weight heparins compared with unfractionated heparin for treatment of acute deep venous thrombosis. A cost‐effectiveness analysis, Ann Intern Med, 130, 789, 10.7326/0003-4819-130-10-199905180-00002 Quinlan, 2004, Low‐molecular‐weight heparin compared with intravenous unfractionated heparin for treatment of pulmonary embolism: a meta‐analysis of randomized, controlled trials, Ann Intern Med, 140, 175, 10.7326/0003-4819-140-3-200402030-00008 Eikelboom, 2000, Unfractionated heparin and low‐molecular‐weight heparin in acute coronary syndromes without ST‐elevation: a meta‐analysis, Lancet, 355, 1936, 10.1016/S0140-6736(00)02324-2 Hirsh, 1991, Oral anticoagulant drugs, N Engl J Med, 324, 1865, 10.1056/NEJM199106273242606 Falati, 2003, Accumulation of tissue factor into developing thrombi in vivo is dependent upon microparticle P‐selectin glycoprotein ligand 1 and platelet P‐selectin, J Exp Med, 197, 1585, 10.1084/jem.20021868 Myers, 2003, P‐selectin and leukocyte microparticles are associated with venous thrombogenesis, J Vasc Surg, 38, 1075, 10.1016/S0741-5214(03)01033-4 Palabrica, 1992, Leukocyte accumulation promoting fibrin deposition is mediated in vivo by P‐selectin on adherent platelets, Nature, 359, 848, 10.1038/359848a0 Davie, 1995, Biochemical and molecular aspects of the coagulation cascade, Thromb Haemost, 75, 1 Creasey, 1993, Tissue factor pathway inhibitor reduces mortality from Escherichia coli septic shock, J Clin Invest, 91, 2850, 10.1172/JCI116529 Elsayed, 1996, Effects of recombinant human tissue factor pathway inhibitor on thrombus formation and its in vivo distribution in a rat DIC model, Am J Clin Pathol, 106, 574, 10.1093/ajcp/106.5.574 Bajaj, 1997, Tissue factor pathway inhibitor: potential therapeutic applications, Thromb Haemost, 78, 471, 10.1055/s-0038-1657572 Abraham, 2001, Assessment of the safety of recombinant tissue factor pathway inhibitor in patients with severe sepsis: a multicenter, randomized, placebo‐controlled, single‐blind, dose escalation study, Crit Care Med, 29, 8081, 10.1097/00003246-200111000-00007 Abraham, 2003, Optimist Trial Study Group. Efficacy and safety of tifacogin (recombinant tissue factor pathway inhibitor) in severe sepsis: a randomized controlled trial, JAMA, 290, 238, 10.1001/jama.290.2.238 Stassens, 1996, Anticoagulant repertoire of the hookworm Ancylostoma caninum, Proc Natl Acad Sci USA, 93, 2149, 10.1073/pnas.93.5.2149 Lee, 2001, Dose–response study of recombinant factor VIIa/tissue factor inhibitor recombinant nematode anticoagulant protein c2 in prevention of postoperative venous thromboembolism in patients undergoing total knee replacement, Circulation, 104, 74, 10.1161/hc2601.091386 Banner, 1996, The crystal structure of the complex of blood coagulation factor VIIa with soluble tissue factor, Nature, 380, 41, 10.1038/380041a0 Harker, 1997, Antithrombotic strategies targeting thrombin activities, thrombin receptors and thrombin generation, Thromb Haemost, 78, 736, 10.1055/s-0038-1657621 Arnljots, 1997, Prevention of experimental arterial thrombosis by topical administration of active site‐inactivated factor VIIa, J Vasc Surg, 25, 341, 10.1016/S0741-5214(97)70356-2 Golino, 1998, Antithrombotic effects of recombinant human, active site‐blocked factor VIIa in a rabbit model of recurrent and arterial thrombosis, Circulation Res, 82, 39, 10.1161/01.RES.82.1.39 Jang, 1995, Influence of blockade at specific levels of the coagulation cascade on restenosis in a rabbit atherosclerotic femoral artery injury model, Circulation, 92, 3041, 10.1161/01.CIR.92.10.3041 Giesen, 1999, Blood‐borne tissue factor: another view of thrombosis, Proc Natl Acad Sci USA, 96, 2311, 10.1073/pnas.96.5.2311 Lincoff, 2000, JACC, 36, 312 Hoffman, 1995, Factors IXa and Xa play distinct roles in tissue‐dependent initiation of coagulation, Blood, 86, 1794, 10.1182/blood.V86.5.1794.bloodjournal8651794 Benedict, 1991, Active site‐blocked factor IXa prevents intravascular thrombus formation in the coronary vasculature without inhibiting extravascular coagulation in a canine thrombosis model, J Clin Invest, 88, 1760, 10.1172/JCI115495 Bajaj, 1985, A monoclonal antibody to factor IX that inhibits the factor VII:Ca potentiation of factor X activation, J Biol Chem, 260, 11574, 10.1016/S0021-9258(17)39070-1 Feuerstein, 1999, Antithrombotic efficacy of a novel murine antihuman factor IX antibody in rats, Arterioscler Thromb Vasc Biol, 19, 2554, 10.1161/01.ATV.19.10.2554 Feurerstein, 1999, An inhibitory anti‐factor IX antibody effectively reduces thrombus formation in a rat model of venous thrombosis, Thromb Haemost, 92, 1443, 10.1055/s-0037-1614852 Eisenberg, 1993, Importance of factor Xa in determining the procoagulant activity of whole‐blood clots, J Clin Invest, l91, 1877, 10.1172/JCI116404 Rezaie, 2001, Prothrombin protects factor Xa in the prothrombinase complex from inhibition by heparin–antithrombin complex, Blood, 97, 2308, 10.1182/blood.V97.8.2308 Brufatto, 2001, The use of prothrombin (S525C) labelled with fluorescein to directly study the inhibition of prothrombinase by antithrombin during prothrombin activation, J Biol Chem, 276, 17663, 10.1074/jbc.M011586200 Walenga, 2002, Fondaparinux: a synthetic heparin pentasaccharide as a new antithrombotic agent, Expert Opin Invest Drugs, 11, 397, 10.1517/13543784.11.3.397 Herbert, 1998, Biochemical and pharmacological properties of SANORG 340006, a potent and long‐acting synthetic pentasaccharide, Blood, 91, 4197, 10.1182/blood.V91.11.4197 Boneu, 1995, Pharmacokinetics and tolerance of the natural pentasaccharide (SR90107A/ORG31540) with high affinity to antithrombin III in man, Thromb Haemost, 74, 1468, 10.1055/s-0038-1649967 Walenga, 1997, Biochemical and pharmacological rationale for the development of a synthetic heparin pentasaccharide, Thromb Res, 86, 1, 10.1016/S0049-3848(97)00042-X Lagrange, 2002, Absence of placental transfer of pentasaccharide (Fondaparinux, Arixtra) in the dually perfused human cotyledon in vitro, Thromb Haemos, 87, 831, 10.1055/s-0037-1613092 Dempfle, 2004, Minor transplacental passage of fondaparinux in vivo (Letter to the Editor), N Engl J Med, 350, 1914, 10.1056/NEJM200404293501825 Elalamy, 1995, Absence of in vitro cross‐reaction of pen tasaccharide with the plasma heparin dependent factor of twenty‐five patients with heparin associated thrombocytopenia, Thromb Haemost, 74, 1384, 10.1055/s-0038-1649949 Amiral, 1997, Absence of cross‐reactivity of SR 90107A/ORG 31540 pentasaccharide with antibodies to heparin‐PF4 complexes developed on heparin‐induced thrombocytopenia, Blood Coagul Fibrinolysis, 8, 114, 10.1097/00001721-199703000-00005 Savi, 2005, Effect of fondaparinux on platelet activation in the presence of heparin‐dependent antibodies: a blinded comparative multicenter study with unfractionated heparin, Blood, 105, 139, 10.1182/blood-2004-05-2010 Harenberg, 2004, Treatment of heparin‐induced thrombocytopenia with fondaparinux, Haematologica, 89, 1017 Bijsterveld, 2002, Ability of recombinant factor VIIa to reverse the anticoagulant effect of the pentasaccharide fondaparinux in healthy volunteers, Circulation, 106, 2550, 10.1161/01.CIR.0000038501.87442.02 Bijsterveld, 2004, Recombinant factor VIIa reverses the anticoagulant effect of the long‐acting pentasaccharide idraparinux in healthy volunteers, Br J Haematol, 124, 653, 10.1111/j.1365-2141.2003.04811.x Eriksson, 2001, Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip‐fracture surgery, N Engl J Med, 345, 1340, 10.1056/NEJMoa011100 Turpie, 2002, Postoperative fondaparinux versus postoperative enoxaparin for prevention of venous thromboembolism after elective hip‐replacement surgery: a randomised double‐blind trial, Lancet, 359, 1721, 10.1016/S0140-6736(02)08648-8 Lassen, 2002, Postoperative fondaparinux versus preoperative enoxaparin for prevention of venous thromboembolism in elective hip‐replacement in elective hip‐replacement surgery: a randomised double‐blind comparison, Lancet, 359, 1715, 10.1016/S0140-6736(02)08652-X Bauer, 2001, Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after major elective knee surgery, N Engl J Med, 345, 1305, 10.1056/NEJMoa011099 Turpie, 2002, Prophylaxis studies. Fondaparinux vs. enoxaparin for the prevention of venous thromboembolism in major orthopedic surgery. A meta‐analysis of 4 randomized double‐blind studies, Arch Intern Med, 162, 1833, 10.1001/archinte.162.16.1833 Eriksson, 2003, PENTasaccharide in Hip‐FRActure Surgery Plus Investigators. Duration of prophylaxis against venous thromboembolism with fondaparinux after hip fracture surgery: a multicentre, randomized, placebo‐controlled, double‐blind study, Arch Intern Med, 163, 1733, 10.1001/archinte.163.11.1337 Cohen, 2003, Fondaparinux vs. placebo for the prevention of venous thromboembolism in acutely ill medical patients (ARTEMIS), J Thromb Haemost, 1 Agnelli, 2003, A randomized double‐blind study to compare the efficacy and safety of fondaparinux with dalteparin in the prevention of venous thromboembolism after high‐risk abdominal surgery: the Pegasus Study, J Thromb Haemost, 1 Buller, 2004, Fondaparinux or enoxaparin for the initial treatment of symptomatic deep venous thrombosis: a randomized trial, Ann Intern Med, 140, 867, 10.7326/0003-4819-140-11-200406010-00007 2003, Subcutaneous fondaparinux versus intravenous unfractionated heparin in the initial treatment of pulmonary embolism, N Engl J Med, 349, 1695, 10.1056/NEJMoa035451 Coussement, 2001, A synthetic factor Xa inhibitor (ORG31540/SR9017A) as an adjunct to fibrinolysis in acute myocardial infarction, Eur Heart J, 22, 1716, 10.1053/euhj.2001.2777 Fergusson, 2002, Meeting highlights – American Heart Association scientific sessions 2001, Circulation, 105, e37, 10.1161/hc0502.104277 2004, 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, 2, 47, 10.1111/j.1538-7836.2003.00516.x Herbert, 1996, DX‐9065a, a novel synthetic, selective and orally active inhibitor of factor Xa: in vitro and in vivo studies, J Pharmacol Exper Ther, 276, 1030 Murayama, 1996, Tolerability, pharmacokinetics and pharmacodynamics of DX‐9065a, a new synthetic potent anticoagulant and specific factor Xa inhibitor, in healthy male volunteers, Clin Pharmacol Ther, 66, 258, 10.1016/S0009-9236(99)70033-0 Dyke, 2002, First experience with direct factor Xa inhibition in patients with stable coronary disease: a pharmacokinetic and pharmacodynamic evaluation, Circulation, 105, 2385, 10.1161/01.CIR.0000016351.12759.52 Alexander, 2004, Initial experience with factor Xa inhibition in percutaneous coronary intervention: the XaNADU‐PIC Pilot, J Thromb Haemost, 2, 234, 10.1111/j.1538-7933.2004.00594.x Lassen, 2003, 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 of deep vein thrombosis in knee replacement surgery, Blood, 102, 15a Ettingshausen, 1999, Replacement therapy with protein C concentrate in infants and adolescents with meningococcal sepsis and purpura fulminans, Semin Thomb Hemost, 25, 537, 10.1055/s-2007-994962 White, 2000, An open‐label study of the adjuvant hemostatic support with protein C replacement therapy in purpura fulminans‐associated meningococcemia, Blood, 96, 3719, 10.1182/blood.V96.12.3719 Bernard, 2001, Efficacy and safety of recombinant activated protein C for severe sepsis, N Engl J Med, 344, 699, 10.1056/NEJM200103083441001 Manns, 2002, An economic evaluation of activated protein C treatment for severe sepsis, N Engl J Med, 347, 993, 10.1056/NEJMsa020969 Parkinson, 1990, Stable expression of a secretable deletion mutation of recombinant human thrombomodulin in mammalian cells, J Biol Chem, 265, 12602, 10.1016/S0021-9258(19)38386-3 Gomi, 1990, Antithrombotic effect of recombinant human thrombomodulin on thrombin‐induced thromboembolism in mice, Blood, 75, 1396, 10.1182/blood.V75.7.1396.1396 Aoki, 1994, Effects of recombinant human soluble thrombomodulin (rhs‐TM) on a rat model of disseminated intravascular coagulation with decreased levels of plasma antithrombin III, Thromb Haemost, 71, 452, 10.1055/s-0038-1642459 Kearon, 2003, A dose–response study of a recombinant human soluble thrombomodulin (ART‐123) for prevention of venous thromboembolism after unilateral total hip replacement, J Thromb Haemost, 1 Hirsh, 1991, Heparin, N Engl J Med, 324, 1565, 10.1056/NEJM199105303242206 Tollefsen, 1995, Insight into the mechanism of action of heparin cofactor II, Thromb Haemost, 74, 1209, 10.1055/s-0038-1649913 Weitz, 1990, Clot‐bound thrombin is protected from inhibition by heparin‐antithrombin III but is susceptible to inactivation by antithrombin III‐independent inhibitors, J Clin Invest, 86, 385, 10.1172/JCI114723 Hogg, 1989, Fibrin monomer protects thrombin from inactivation by heparin‐antithrombin III: implications for heparin efficacy, Proc Natl Acad Sci USA, 86, 3619, 10.1073/pnas.86.10.3619 Weitz, 1998, Thrombin binds to soluble fibrin degradation products where it is protected from inhibition by heparin‐antithrombin but susceptible to inactivation by antithrombin‐independent inhibitors, Circulation, 97, 544, 10.1161/01.CIR.97.6.544 Fox, 1993, Anticoagulant activity of Hirulog, a direct thrombin inhibitor, in humans, Thromb Haemost, 69, 157, 10.1055/s-0038-1651573 Stringer, 1992, Hirudins: antithrombin anticoagulants, Ann Pharmacother, 26, 1535, 10.1177/106002809202601211 Greinacher, 1999, Recombinant hirudin (lepirudin) provides safe and effective anticoagulation in patients with heparin‐induced thrombocytopenia. A prospective study, Circulation, 99, 73, 10.1161/01.CIR.99.1.73 Farner, 2001, A comparison of danaparoid and lepirudin in heparin‐induced thrombocytopenia, Thromb Haemost, 85, 950, 10.1055/s-0037-1615946 Reiss, 1995, Recombinant hirudin as a new anticoagulant during cardiac operations instead of heparin: successful for aortic valve replacement in man, J Thorac Cardiovasc Surg, 11, 265, 10.1016/S0022-5223(05)80033-9 Potzch, 1994, Recombinant hirudin as an anticoagulant in open‐heart surgery: a case‐report, Ann Hematol, 68, A53 Lewis, 2001, Argatroban anticoagulant therapy in patients with heparin‐induced thrombocytopenia, Circulation, 103, 1838, 10.1161/01.CIR.103.14.1838 Lewis, 2003, Argatroban anticoagulation in patients with heparin‐induced thrombocytopenia, Arch Intern Med, 163, 1849, 10.1001/archinte.163.15.1849 Weitz, 2002, Direct thrombin inhibitors in acute coronary syndromes: Present and future, Circulation, 105, 1004, 10.1161/hc0802.104331 Bittl, 1995, Treatment with bivalirudin (hirulog) as compared with heparin during coronary angioplasty for unstable or post‐infarction angina, N Engl J Med, 333, 764, 10.1056/NEJM199509213331204 Bittl, 2001, Bivalirudin versus heparin during coronary angioplasty for unstable or post‐infarction angina: final report reanalysis of the Bivalirudin Angioplasty Study, Am Heart J, 142, 952, 10.1067/mhj.2001.119374 Bittl, 1995, Comparative safety profiles of hirulog and heparin in patients undergoing coronary angioplasty. The Hirulog Angioplasty Study Investigators, Am Heart J, 130, 658, 10.1016/0002-8703(95)90303-8 Kong, 1999, Clinical outcomes of bivalirudin for ischemic heart disease, Circulation, 100, 2049, 10.1161/01.CIR.100.20.2049 Lincoff, 2002, Bivalirudin with planned or provisional abciximab versus low‐dose heparin and abciximab during percutaneous coronary revascularization: results of the Comparison of Abciximab Complications with Hirulog for Ischemic Events Trial (CACHET), Am Heart J, 143, 847, 10.1067/mhj.2002.122173 Lincoff, 2003, Bivalirudin and provisional GPIIb/IIIa blockade compared with heparin and planned GPIIb/IIIa blockade during percutaneous coronary intervention. REPLACE‐2 randomized trial, JAMA, 289, 853, 10.1001/jama.289.7.853 Eriksson, 2003, Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee joint replacement, Thromb Haemost, 89, 288, 10.1055/s-0037-1613445 Gustafsson, 2001, The direct thrombin inhibitor melagatran and its oral prodrug H376/95: intestinal absorption properties, biochemical and pharmacodynamic effects, Thromb Res, 101, 171, 10.1016/S0049-3848(00)00399-6 Bredberg, 2003, Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450‐mediatged drug–drug interactions, Clin Pharmacokinet, 42, 765, 10.2165/00003088-200342080-00005 Eriksson, 2003, Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran, Clin Pharmcokinet, 42, 743, 10.2165/00003088-200342080-00003 Johansson, 2003, Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor, Clin Pharmacokinet, 42, 381, 10.2165/00003088-200342040-00006 Eriksson, 2002, Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial, Lancet, 360, 1441, 10.1016/S0140-6736(02)11469-3 Heit, 2001, Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement, Arch Intern Med, 161, 2215, 10.1001/archinte.161.18.2215 Eriksson, 2002, The oral direct thrombin inhibitor ximelagatran, and its subcutaneous form, melagatran, compared with enoxaparin for prophylaxis of venous thromboembolism in total hip or total knee replacement: the EXPRESS study, Blood, 100, 299 Colwell, 2003, Comparison of ximelagatran, an oral direct thrombin inhibitor with enoxaparin for the prevention of venous thromboembolism following total hip replacement. A randomized, double‐blind study, J Thromb Haemost, 1, 2119, 10.1046/j.1538-7836.2003.00368.x Colwell, 2003, Randomized double‐blind comparison of ximelagatran, an oral direct thrombin inhibitor and warfarin to prevent venous thromboembolism (VTE) after total knee replacement, Blood, 102, 14 Francis, 2003, Comparison of ximelagatran with warfarin for prevention of venous thromboembolism after total knee replacement, N Engl J Med, 349, 1703, 10.1056/NEJMoa035162 Eriksson, 2003, A randomized, controlled, dose‐guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I, J Thromb Haemost, 1, 41, 10.1046/j.1538-7836.2003.00034.x Francis, 2003, Efficacy and safety of the oral direct thrombin inhibitor ximelagatran compared with current standard therapy for acute symptomatic deep vein thrombosis, with or without pulmonary embolism: the THRIVE Treatment Study, Blood, 102, 6a Schulman, 2003, Secondary prevention of venous thromboembolism with the oral direct thrombin inhibitor ximelagatran, N Engl J Med, 349, 1713, 10.1056/NEJMoa030104 Petersen, 2003, Ximelagatran versus warfarin for stroke prevention in patients with nonvalvular atrial fibrillation. SPORTIF II: a dose‐guiding tolerability, and safety study, J Am Coll Cardiol, 41, 1445, 10.1016/S0735-1097(03)00255-9 Peterson, 2001, A long‐term follow‐up of ximelagatran as an oral anticoagulant for the prevention of stroke and systemic embolism in patients with atrial fibrillation, Blood, 98, 2953 2003, 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, 362, 1691, 10.1016/S0140-6736(03)14841-6 Halperin, 2005, Ximelagatran: oral direct thrombin inhibition as anticoagulant therapy in atrial fibrillation, J Am Coll Cardiol, 45, 1, 10.1016/j.jacc.2004.09.049 Wallentin, 2003, Oral ximelagatran for secondary prophylaxis after myocardial infarction: the ESTEEM randomised controlled trial, Lancet, 362, 789, 10.1016/S0140-6736(03)14287-0 Gustafsson, 2003, Oral direct thrombin inhibitors in clinical development, J Int Med, 254, 322, 10.1046/j.1365-2796.2003.01225.x Wienen, 2001, Antithrombotic effects of the direct thrombin inhibitor BIBR953ZW and its orally active prodrug BIBR1048MS in a model of venous thrombosis in rabbits, Thromb Haemost, 86 Eriksson, 2005, 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, 3, 103, 10.1111/j.1538-7836.2004.01100.x Stangier, 2003, Pharmacokinetics of BIBR953ZW, the active form of the oral direct thrombin inhibitor dabigatran etexilate, in patients undergoing hip replacement, J Thromb Haemost, 1 Stangier, 2003, The effect of BIBR953ZW, the active form of the oral direct thrombin inhibitor BIBR1048, on the prolongation of the aPTT and ECT in orthopedic patients: a population pharmacodynamic study, J Thromb Haemost, 1 Eriksson, 2004, Dose escalating safety study of a new oral direct thrombin inhibitor, dabigatran etexilate, in patients undergoing total hip replacement: BISTRO 1, J Thromb Haemost, 2, 1573, 10.1111/j.1538-7836.2004.00890.x Albers, 2001, Antithrombotic therapy in atrial fibrillation, Chest, 119, 94S, 10.1378/chest.119.1_suppl.194S