Oral IIa inhibitors

Hematology/Oncology Clinics of North America

Volumn 24, Issue 4, 2010, Pages 739-753

  Lee, Catherine J ^a   Badhwar, Gauri ^a   Ansell, Jack E ^a  

^a LENOX HILL HOSPITAL   (United States)

Author keywords

Dabigatran etexilate; Oral anticoagulation; Oral IIa inhibitors; Prevention; Thrombin; Venous thromboembolism

Indexed keywords

ACETYLSALICYLIC ACID; ALANINE AMINOTRANSFERASE; ATORVASTATIN; AZD 0837; BIBR 1087; BIBR 951; BLOOD CLOTTING FACTOR 10A INHIBITOR; BLOOD CLOTTING FACTOR 11; BLOOD CLOTTING FACTOR 12; BLOOD CLOTTING FACTOR 5; BLOOD CLOTTING FACTOR 8; BLOOD CLOTTING FACTOR 9; DABIGATRAN; DABIGATRAN ETEXILATE; DICLOFENAC; DIGOXIN; DRUG METABOLITE; ENOXAPARIN; FIBRINOGEN; H 067637; H 069927; MELAGATRAN; ODIPARCIL; OPIATE; PLACEBO; PROTHROMBIN; TGN 167; TRI 50C 04; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN; XIMELAGATRAN;

ACUTE HEART INFARCTION; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANTICOAGULANT THERAPY; ANTICOAGULATION; AREA UNDER THE CURVE; BLEEDING; CLINICAL TRIAL; DEEP VEIN THROMBOSIS; DOSE KIDNEY FUNCTION RELATION; DRUG ABSORPTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG HYDROLYSIS; DRUG METABOLISM; DRUG SAFETY; DYSPEPSIA; HEART ATRIUM FIBRILLATION; HUMAN; LIVER TOXICITY; LUNG EMBOLISM; MAXIMUM PLASMA CONCENTRATION; PARTIAL THROMBOPLASTIN TIME; PRIMARY PREVENTION; PRIORITY JOURNAL; PROTHROMBIN TIME; REVIEW; SECONDARY PREVENTION; SIDE EFFECT; STROKE; TOTAL HIP PROSTHESIS; TOTAL KNEE REPLACEMENT; VENOUS THROMBOEMBOLISM;

ANTICOAGULANTS; CLINICAL TRIALS AS TOPIC; HUMANS; PROTHROMBIN; THROMBOEMBOLISM;

EID: 77955115251     PISSN: 08898588     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.hoc.2010.05.001     Document Type: Review

References (41)

1. Gustafsson D., Nystrom J., Carlsson S., et al. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. Thromb Res 2001, 101(3):171-181.
2. Bergsrud E.A., Gandhi P.J. A review of the clinical uses of ximelagatran in thrombosis syndromes. J Thromb Thrombolysis 2003, 16(3):175-188.
3. Crowther M.A., Weitz J.I. Ximelagatran: the first oral direct thrombin inhibitor. Expert Opin Investig Drugs 2004, 13(4):403-413.
4. Eriksson B.I., Agnelli G., Cohen A.T., 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.
5. Eriksson B.I., Agnelli G., Cohen A.T., et al. The direct thrombin inhibitor melagatran followed by oral ximelagatran compared with enoxaparin for the prevention of venous thromboembolism after total hip or knee replacement: the EXPRESS study. J Thromb Haemost 2003, 1(12):2490-2496.
6. Colwell C.W., Berkowitz S.D., Davidson B.L., et al. 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 2003, 1(10):2119-2130.
7. Francis C.W., Berkowitz S.D., Comp P.C., et al. Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement. N Engl J Med 2003, 349(18):1703-1712.
8. Colwell C.W., Berkowitz S.D., Lieberman J.R., et al. Oral direct thrombin inhibitor ximelagatran compared with warfarin for the prevention of venous thromboembolism after total knee arthroplasty. J Bone Joint Surg Am 2005, 87(10):2169-2177.
9. Halperin J.L. Ximelagatran compared with warfarin for prevention of thromboembolism in patients with nonvalvular atrial fibrillation: Rationale, objectives, and design of a pair of clinical studies and baseline patient characteristics (SPORTIF III and V). Am Heart J 2003, 146(3):431-438.
10. Olsson S.B. 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.
11. Albers G.W., Diener H.C., Frison L., et al. Ximelagatran vs warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a randomized trial. JAMA 2005, 293(6):690-698.
12. O'Brien C.L., Gage B.F. Costs and effectiveness of ximelagatran for stroke prophylaxis in chronic atrial fibrillation. JAMA 2005, 293(6):699-706.
13. Fiessinger J.N., Huisman M.V., Davidson B.L., et al. Ximelagatran vs low-molecular-weight heparin and warfarin for the treatment of deep vein thrombosis: a randomized trial. JAMA 2005, 293(6):681-689.
14. Schulman S., Wahlander K., Lundstrom T., et al. Secondary prevention of venous thromboembolism with the oral direct thrombin inhibitor ximelagatran. N Engl J Med 2003, 349(18):1713-1721.
15. Wallentin L., Wilcox R.G., Weaver W.D., et al. Oral ximelagatran for secondary prophylaxis after myocardial infarction: the ESTEEM randomised controlled trial. Lancet 2003, 362(9386):789-797.
16. Keisu M., Andersson T.B. Drug-induced liver injury in humans: the case of ximelagatran. Handb Exp Pharmacol 2010, 196:407-418.
17. 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(2):386-399.
18. 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(3):292-303.
19. Eriksson B.I., Dahl O.E., 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(9):1573-1580.
20. Stangier J., Eriksson B.I., Dahl O.E., et al. Pharmacokinetic profile of the oral direct thrombin inhibitor dabigatran etexilate in healthy volunteers and patients undergoing total hip replacement. J Clin Pharmacol 2005, 45(5):555-563.
21. Eriksson B.I., Quinlan D.J., Weitz J.I. Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development. Clin Pharmacokinet 2009, 48(1):1-22.
22. Stangier J., Stahle H., Rathgen K., et al. Pharmacokinetics and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor, are not affected by moderate hepatic impairment. J Clin Pharmacol 2008, 48(12):1411-1419.
23. Stangier J., Stahle H., Rathgen K., et al. Pharmacokinetics and pharmacodynamics of the direct oral thrombin inhibitor dabigatran in healthy elderly subjects. Clin Pharmacokinet 2008, 47(1):47-59.
24. Stangier J. Clinical pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor dabigatran etexilate. Clin Pharmacokinet 2008, 47(5):285-295.
25. Stangier J., Clemens A. Pharmacology, pharmacokinetics, and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor. Clin Appl Thromb Hemost 2009, [Epub ahead of print].
26. Stangier J., Rathgen K., Stahle H., et al. Coadministration of dabigatran etexilate and atorvastatin: assessment of potential impact on pharmacokinetics and pharmacodynamics. Am J Cardiovasc Drugs 2009, 9(1):59-68.
27. Wienen W., Stassen J.M., 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(1):155-162.
28. Sorbera L., Bozzo J., Castaner J. Dabigatran/dabigatran etexilate. Drugs Future 2005, 30(9):877-885.
29. Eriksson B.I., Dahl O.E., Buller H.R., 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.
30. Wolowacz S.E., Roskell N.S., Plumb J.M., et al. Efficacy and safety of dabigatran etexilate for the prevention of venous thromboembolism following total hip or knee arthroplasty. A meta-analysis. Thromb Haemost 2009, 101(1):77-85.
31. Ginsberg J.S., Davidson B.L., Comp P.C., et al. Oral thrombin inhibitor dabigatran etexilate vs North American enoxaparin regimen for prevention of venous thromboembolism after knee arthroplasty surgery. J Arthroplasty 2009, 24(1):1-9.
32. Eriksson B.I., Dahl O.E., 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(11):2178-2185.
33. Eriksson B.I., Dahl O.E., 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(9591):949-956.
34. Schulman S., Kearon C., Kakkar A.K., et al. Dabigatran versus warfarin in the treatment of acute venous thromboembolism. N Engl J Med 2009, 361(24):2342-2352.
35. Ezekowitz M.D., Reilly P.A., 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(9):1419-1426.
36. Connolly S.J., Ezekowitz M.D., Yusuf S., et al. Dabigatran versus warfarin in patients with atrial fibrillation. N Engl J Med 2009, 361(12):1139-1151.
37. Olsson S.B., Rasmussen L.H., Tveit A., et al. Safety and tolerability of an immediate-release formulation of the oral direct thrombin inhibitor AZD0837 in the prevention of stroke and systemic embolism in patients with atrial fibrillation. Thromb Haemost 2010, 103:604-612.
38. Upreti V.V., Khurana M., Cox D.S., et al. Determination of endogenous glycosaminoglycans derived disaccharides in human plasma by HPLC: validation and application in a clinical study. J Chromatogr B Analyt Technol Biomed Life Sci 2006, 831(1-2):156-162.
39. Eriksson B.I., Quinlan D.J. Oral anticoagulants in development: focus on thromboprophylaxis in patients undergoing orthopaedic surgery. Drugs 2006, 66(11):1411-1429.
40. Spyropoulos A.C. Investigational treatments of venous thromboembolism. Expert Opin Investig Drugs 2007, 16(4):431-440.
41. Schwienhorst A. Direct thrombin inhibitors-a survey of recent developments. Cell Mol Life Sci 2006, 63(23):2773-2791.