New therapeutic option for thromboembolism – dabigatran etexilate

Bibliography

• Hyers TM. Management of venous thromboembolism: past, present, and future. Arch Intern Med 2003;163:759-68
   PubMed Web of Science ®Google Scholar
• Weitz JI. Low-molecular-weight heparins. N Engl J Med 1997;337:688-98
   PubMed Web of Science ®Google Scholar
• Eikelboom JW, Anand SS, Malmberg K, et al. Unfractionated heparin and low-molecular-weight heparin in acute coronary syndrome without ST elevation: a meta-analysis. Lancet 2000;355:1936-42
   PubMed Web of Science ®Google Scholar
• Becattini C, Agnelli G, Emmerich J, et al. Initial treatment of venous thromboembolism. Thromb Haemost 2006;96:242-50
   PubMedGoogle Scholar
• Hirsh J, Dalen J, Anderson DR, et al. Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range. Chest 2001;119:8S-21S
   PubMed Web of Science ®Google Scholar
• Weitz JI. Factor Xa or thrombin: is thrombin a better target? J Thromb Haemost 2007;5(Suppl 1):65-7
   PubMedGoogle Scholar
• Narayanan S. Multifunctional roles of thrombin. Ann Clin Lab Sci 1999;29:275-80
   PubMed Web of Science ®Google Scholar
• Bar Shavit R, Kahn A, Wilner GD, Fenton JW II. Monocyte chemotaxis: stimulation by specific exosite region in thrombin. Science 1983;220:728-31
   PubMedGoogle Scholar
• Chen LB, Buchanan JM. Mitogenic activity of blood components. I. Thrombin and prothrombin. Proc Natl Acad Sci USA 1975;72:131-5
   PubMed Web of Science ®Google Scholar
• McNamara CA, Sarembock IJ, Gimple LW, et al. Thrombin stimulates proliferation of cultured rat aortic smooth muscle cells by a proteolytically activated receptor. J Clin Invest 1993;91:94-8
   PubMed Web of Science ®Google Scholar
• Engelmann B, Luther T, Muller I. Intravascular tissue factor pathway – a model for rapid initiation of coagulation within the blood vessel. Thromb Haemost 2003;89:3-8
   PubMed Web of Science ®Google Scholar
• Stassen JM, Arnout J, Deckmyn H. The hemostatic system. Curr Med Chem 2004;11:2245-60
   PubMed Web of Science ®Google Scholar
• Blomback B, Blomback M. The molecular structure of fibrinogen. Ann NY Acad Sci 1972;202:77-97
   PubMed Web of Science ®Google Scholar
• Kikelj D. Peptidomimetic thrombin inhibitors. Pathophysiol Haemost Thromb 2003/2004;33:487-91
   PubMedGoogle Scholar
• Markwardt F. Development of direct thrombin inhibitors in comparison with glycosaminoglycans. Semin Thromb Hemost 2001;27:523-30
   PubMedGoogle Scholar
• Wiley MR, Fisher MJ. Small-molecule direct thrombin inhibitors. Expert Opin Ther Patents 1997;7:1265-82
   Web of Science ®Google Scholar
• Bates SM, Weitz JI. The status of new anticoagulants. Br J Haematol 2006;134:3-19
   PubMed Web of Science ®Google Scholar
• Markwardt F. Hirudin as alternative anticoagulant – a historical review. Semin Thromb Hemost 2002;28:405-14
   PubMed Web of Science ®Google Scholar
• Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40
   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 – the METHRO III study. Thromb Haemost 2003;89:288-96
   PubMed Web of Science ®Google Scholar
• Astrazeneca. AstraZeneca withdraws Exanta. Press release; 2006
   Google Scholar
• Das J, Kimball SD. Thrombin active site inhibitors. Bioorg Med Chem 1995;3:999-1007
   PubMed Web of Science ®Google Scholar
• Kettner C, Shaw E. D-Phe-Pro-ArgCH2C1-A selective affinity label for thrombin. Thromb Res 1979;14:969-73
   PubMed Web of Science ®Google Scholar
• Hauel NH, Nar H, Priepke H, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem 2002;45:1757-66
   PubMed Web of Science ®Google Scholar
• Sanderson PEJ, Naylor Olsen AM. Thrombin inhibitor design. Curr Med Chem 1998;5:289-304
   PubMed Web of Science ®Google Scholar
• Stangier J, Rathgen K, Stahle H, et al. The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects. Br J Clin Pharmacol 2007;64:292-303
   PubMed Web of Science ®Google Scholar
• Wienen W, Stassen JM, Priepke H, et al. In-vitro profile and ex vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost 2007;98:155-62
   PubMed Web of Science ®Google Scholar
• Stangier J, Stahle H, Rathgen K, Fuhr R. Pharmacokinetics and pharmacodynamics of the direct oral thrombin inhibitor dabigatran in healthy elderly subjects. Clin Pharmacokinet 2008;47:47-59
   PubMed Web of Science ®Google Scholar
• Stangier J, Rathgen K, Gansser D, et al. Pharmacokinetics of BIBR 953ZW, a novel low molecular weight direct thrombin inhibitor in healthy volunteers. Thromb Haemost 2001;86(Suppl Abs):OC2347
   Google Scholar
• Blech S, Ebner T, Ludwig Schwellinger E, et al. The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans. Drug Metab Dispos 2008;36:386-99
   PubMed Web of Science ®Google Scholar
• Stassen JM, Rathgen K, Zimmermann R, et al. Pharmacodynamics of the synthetic direct thrombin inhibitor BIBR 953ZW in healthy subjects. Thromb Haemost 2001;86(Suppl Abs):OC160
   Google Scholar
• Eriksson BI, Dahl OE, Ahnfelt L, et al. Dose escalating safety study of a new oral direct thrombin inhibitor, dabigatran etexilate, in patients undergoing total hip replacement: BISTRO I. J Thromb Haemost 2004;2:1573-80
   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;3:103-11
   PubMed Web of Science ®Google Scholar
• Ezekowitz MD, Reilly PA, Nehmiz G, et al. Dabigatran with or without concomitant aspirin compared with warfarin alone in patients with nonvalvular atrial fibrillation (PETRO Study). Am J Cardiol 2007;100:1419-26
   PubMed Web of Science ®Google Scholar
• Eriksson BI, Dahl OE, Van Dijk CN, et al. A new oral aniticoagulant, dabigatran etexilate, is effective and safe in preventing venous thromboembolism after total knee replacement surgery (the RE-MODEL trial). Blood 2006;108(Abs):573
   Web of Science ®Google Scholar
• Boehringer Ingelheim Corp. Phase III results for dabigatran etexilate, an investigational oral anticoagulant, presented today at XXIst congress of the International Society on Thrombosis and Haemostasis. Press release; 2007
   Google Scholar
• Boehringer Ingelheim Corp. Further phase III data shows dabigatran etexilate, a new oral anticoagulant, is effective and safe in preventing venous thromboembolism after orthopedic surgery. Press release; 2007
   Google Scholar
• Secondary prevention of venous thromboembolism. Id:NCT00329238. Clinical Trials.gov, 2007. Available from: http://www.clinicaltrials.gov [Accessed 27 August 2008]
   Google Scholar
• Randomized evaluation of long-term anticoagulant therapy (RE-LY) with dabigatran etexilate. Id:NCT00262600. Clinical Trials.gov, 2006. Available from: http://www.clinicaltrials.gov [Accessed 27 August 2008]
   Google Scholar
• Boehringer Ingelheim Corp. Most extensive thromboembolitic disease clinical trial program launched by Boehringer Ingelheim. Press release; 2006
   Google Scholar
• Boehringer Ingelheim Pharmaceuticals. Positive phase III results for new fixed oral dose anticoagulant presented at 48th Annual Meeting of the American Society of Hematology. Press release; 2006
   Google Scholar
• Eriksson BI, Dahl OE, Rosencher N, et al. Oral dabigatran etexilate vs. subcutaneous enoxaparin for the prevention of venous thromboembolism after total knee replacement: the RE-MODEL randomized trial. J Thromb Haemost 2007;5:2178-85
   PubMed Web of Science ®Google Scholar
• Eriksson BI, Dahl OE, Rosencher N, et al. Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial. Lancet 2007;370:949-56
   PubMed Web of Science ®Google Scholar
• Efficacy and safety of dabigatran compared to warfarin for 6 month treatment of acute symptomatic venous thromboembolism. Id:NCT00291330. Clinical Trials.gov, 2006. Available from: http://www.clinicaltrials.gov [Accessed 27 August 2008]
   Google Scholar
• Fuster V, Rydén LE, Cannom DS, et al. ACC/AHA/ESC 2006 guidelines for the management of patients with atrial fibrillation – executive summary: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines and the European Society of Cardiology Committee for Practice Guidelines (Writing Committee to Revise the 2001 Guidelines for the Management of Patients With Atrial Fibrillation). J Am Coll Cardiol 2006;48:854-906
   PubMed Web of Science ®Google Scholar
• Laposata M. Point-of-care coagulation testing: stepping gently forward. Clin Chem 2001;47:801-2
   PubMedGoogle Scholar
• Ieko M. Dabigatran etexilate, a thrombin inhibitor for the prevention of venous thromboembolism and stroke. Curr Opin Investig Drugs 2007;8:758-68
   PubMedGoogle Scholar
• Nowak G. Clinical monitoring of hirudin and direct thrombin inhibitors. Semin Thromb Hemost 2001;27:537-41
   PubMed Web of Science ®Google Scholar
• Carlsson SC, Mattsson C, Eriksson UG, et al. A review of the effects of the oral direct thrombin inhibitor ximelagatran on coagulation assays. Thromb Res 2005;115:9-18
   PubMed Web of Science ®Google Scholar
• Fenyvesi T, Jorg I, Harenberg J. Monitoring of anticoagulant effects of direct thrombin inhibitors. Semin Thromb Hemost 2002;28:361-8
   PubMed Web of Science ®Google Scholar
• Gosselin RC, King JH, Janatpour KA, et al. Comparing direct thrombin inhibitors using aPTT, ecarin clotting times, and thrombin inhibitor management testing. Ann Pharmacother 2004;38:1383-8
   PubMed Web of Science ®Google Scholar
• European Medicine Agency: meeting highlights from the Committee for Medicinal Products for Human Use. Press release; 2008
   Google Scholar
• Berry CN, Lassalle G, Lunven C, et al. SSR182289A, a novel, orally active thrombin inhibitor: in vitro profile and ex vivo anticoagulant activity. J Pharmacol Exp Ther 2002;303:1189-98
   PubMedGoogle Scholar
• Altenburger JM, Lassalle GY, Matrougui M, et al. SSR182289A, a selective and potent orally active thrombin inhibitor. Bioorg Med Chem 2004;12:1713-30
   PubMed Web of Science ®Google Scholar
• Combe S, Chander C, Kennedy A. Pharmacodynamics of TGN 255, a novel intravenous low molecular weight direct thrombin inhibitor, in healthy subjects. J Thromb Haemost 2005;3(Suppl 1):P1115
   PubMedGoogle Scholar
• Stern R, Chanoine F, Criswell K. Are coagulation times biomarkers? Data from a Phase I study of the oral thrombin inhibitor LB-30057 (CI-1028). J Clin Pharmacol 2003;43:118-21
   PubMed Web of Science ®Google Scholar
• Deng JZ, McMasters DR, Rabbat PM, et al. Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization. Bioorg Med Chem Lett 2005;15:4411-6
   PubMedGoogle Scholar
• Schwienhorst A. Direct thrombin inhibitors – a survey of recent developments. Cell Mol Life Sci 2006;63:2773-91
   PubMedGoogle Scholar