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Volumn 11, Issue 30, 2005, Pages 3877-3884

Pharmacology and clinical potential of direct thrombin inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

ANTICOAGULANT AGENT; ANTIVITAMIN K; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; FIBRIN; HEPARIN; HIRUDIN; HIRULOG; LEPIRUDIN; MELAGATRAN; THROMBIN; THROMBIN INHIBITOR; THROMBOCYTE FACTOR 4; VON WILLEBRAND FACTOR; XIMELAGATRAN;

EID: 27744470403     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/138161205774580598     Document Type: Review
Times cited : (30)

References (46)
  • 1
    • 0027123107 scopus 로고
    • Molecular and cellular biology of blood coagulation
    • Furie B, Furie BC. Molecular and cellular biology of blood coagulation. N Engl J Med 1992; 326: 800-906.
    • (1992) N. Engl. J. Med. , vol.326 , pp. 800-906
    • Furie, B.1    Furie, B.C.2
  • 2
    • 0035817822 scopus 로고    scopus 로고
    • Role of thrombin signalling in platelets in haemostasis and thrombosis
    • Sambrano GR, Weiss EJ, Zheng YW, Huang W, Coughlin SR. Role of thrombin signalling in platelets in haemostasis and thrombosis. Nature 2001; 413: 74-8.
    • (2001) Nature , vol.413 , pp. 74-78
    • Sambrano, G.R.1    Weiss, E.J.2    Zheng, Y.W.3    Huang, W.4    Coughlin, S.R.5
  • 3
    • 0034648757 scopus 로고    scopus 로고
    • Thrombin signalling and protease-activated receptors
    • Coughlin SR. Thrombin signalling and protease-activated receptors. Nature 2000; 407: 258-64.
    • (2000) Nature , vol.407 , pp. 258-264
    • Coughlin, S.R.1
  • 4
    • 0030015015 scopus 로고    scopus 로고
    • Hirudins: From leeches to man
    • Wallis RB. Hirudins: from leeches to man. Semin Thromb Hemost 1996; 22: 185-196.
    • (1996) Semin. Thromb. Hemost. , vol.22 , pp. 185-196
    • Wallis, R.B.1
  • 6
    • 0036800881 scopus 로고    scopus 로고
    • Pharmacology of recombinant hirudin
    • Nowak G. Pharmacology of recombinant hirudin. Semin Thromb Hemost 2002; 28:415-24.
    • (2002) Semin. Thromb. Hemost. , vol.28 , pp. 415-424
    • Nowak, G.1
  • 7
    • 0035814770 scopus 로고    scopus 로고
    • Prognostic significance of thrombocytopenia during hirudin and heparin therapy in acute coronary syndrome without ST elevation: Organization to Assess Strategies for Ischemic Syndromes (OASIS-2)study
    • Eikelboom JW, Anand SS, Mehta. SR, Weitz JI, Yi C, Yusuf S. Prognostic significance of thrombocytopenia during hirudin and heparin therapy in acute coronary syndrome without ST elevation: Organization to Assess Strategies for Ischemic Syndromes (OASIS-2)study. Circulation 2001; 103: 643-50.
    • (2001) Circulation , vol.103 , pp. 643-650
    • Eikelboom, J.W.1    Anand, S.S.2    Mehta, S.R.3    Weitz, J.I.4    Yi, C.5    Yusuf, S.6
  • 8
    • 0002111750 scopus 로고    scopus 로고
    • Recombinant hirudin for treatment of heparin-induced thrombocytopenia
    • Warkentin TE, Greinacher A Ed, Marcel Dekker: New York
    • Greinacher A. Recombinant hirudin for treatment of heparin-induced thrombocytopenia. In: Warkentin TE, Greinacher A Ed, Heparin-induced thrombocytopenia. Marcel Dekker: New York 2000; 313-338.
    • (2000) Heparin-induced Thrombocytopenia , pp. 313-338
    • Greinacher, A.1
  • 9
  • 10
    • 0029161648 scopus 로고
    • Use of recombinant hirudin as antithrombotic treatment in patients with heparin-induced thrombocytopenia
    • Schiele F, Vuillemenot A, Kramarz P, Kieffer Y, Anguenot T, Bernard Y, et al. Use of recombinant hirudin as antithrombotic treatment in patients with heparin-induced thrombocytopenia. Am J Hematol 1995; 50: 20-5.
    • (1995) Am. J. Hematol. , vol.50 , pp. 20-25
    • Schiele, F.1    Vuillemenot, A.2    Kramarz, P.3    Kieffer, Y.4    Anguenot, T.5    Bernard, Y.6
  • 11
    • 0005214444 scopus 로고    scopus 로고
    • Monitoring of the action of antithrombin agents by ecarin clotting time. Pifirre R ed
    • Philadelphia, PA: Hanley. & Belfus
    • Nowak G. Monitoring of the action of antithrombin agents by ecarin clotting time. In: Pifirre R ed, New Anticoagulants for the Cardiovascular Patient. Philadelphia, PA: Hanley. & Belfus 1997; 530-550.
    • (1997) New Anticoagulants for the Cardiovascular Patient , pp. 530-550
    • Nowak, G.1
  • 12
    • 0025346345 scopus 로고
    • 2nd Design and characterization of hirulogs: A novel class of bivalent peptide inhibitors of thrombin
    • Maraganore JM, Bourdon P, Jablonski J, Ramachandran KL, Fenton JW 2nd. Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin. Biochemistry 1990; 29: 7095-7101.
    • (1990) Biochemistry , vol.29 , pp. 7095-7101
    • Maraganore, J.M.1    Bourdon, P.2    Jablonski, J.3    Ramachandran, K.L.4    Fenton, J.W.5
  • 13
    • 0028587155 scopus 로고
    • Kinetic mechanism for the interaction of hirulog with thrombin
    • Parry MA, Maraganore JM, Stone SR. Kinetic mechanism for the interaction of hirulog with thrombin. Biochemistry 1994; 33: 14807-14814.
    • (1994) Biochemistry , vol.33 , pp. 14807-14814
    • Parry, M.A.1    Maraganore, J.M.2    Stone, S.R.3
  • 14
    • 0035983918 scopus 로고    scopus 로고
    • Bivalirudin pharmacokinetics and pharmacodynamics: Effect of renal finiction, dose and gender
    • Robson R, White H, Aylward P, Frampton C. Bivalirudin pharmacokinetics and pharmacodynamics: effect of renal finiction, dose and gender. Clin Pharmacol Ther 2002; 71: 433-9.
    • (2002) Clin. Pharmacol. Ther. , vol.71 , pp. 433-439
    • Robson, R.1    White, H.2    Aylward, P.3    Frampton, C.4
  • 16
    • 27744563832 scopus 로고    scopus 로고
    • Argatroban Package Insert
    • Argatroban Package Insert 2001.
    • (2001)
  • 17
    • 0034049121 scopus 로고    scopus 로고
    • The pharmacokinetics and pharmacodynamics of argatroban: Effects of age, gender, and hepatic or renal dysfunction
    • Swan SK, Hursting MJ. The pharmacokinetics and pharmacodynamics of argatroban: effects of age, gender, and hepatic or renal dysfunction. Pharmacotherapy 2000; 20: 318-329.
    • (2000) Pharmacotherapy , vol.20 , pp. 318-329
    • Swan, S.K.1    Hursting, M.J.2
  • 18
    • 0035251672 scopus 로고    scopus 로고
    • The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: Intestinal absorption properties, biochemical and pharmacodynamic effects
    • Gustafsson D, Nystrom J, Carlsson S, Bredberg U, Eriksson U, Gyzander E, el al. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. Thromb Res 2001; 101: 171-81.
    • (2001) Thromb. Res. , vol.101 , pp. 171-181
    • Gustafsson, D.1    Nystrom, J.2    Carlsson, S.3    Bredberg, U.4    Eriksson, U.5    Gyzander, E.6
  • 19
    • 0037372498 scopus 로고    scopus 로고
    • Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs and humans
    • Eriksson UG, Bredberg U, Hoffmann K-J, Thuresson A., Garielsson M, Eriksson H, et al. Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs and humans. Drug Metab Dispos 2003; 31: 294-305.
    • (2003) Drug Metab. Dispos. , vol.31 , pp. 294-305
    • Eriksson, U.G.1    Bredberg, U.2    Hoffmann, K.-J.3    Thuresson, A.4    Garielsson, M.5    Eriksson, H.6
  • 20
    • 0042122764 scopus 로고    scopus 로고
    • Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran
    • Eriksson UG, Johansson S, Attman PO, Mulec H, Frison L, Fager G, el al. Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran. Clin Pharmacokinet 2003; 42: 743-53.
    • (2003) Clin. Pharmacokinet. , vol.42 , pp. 743-753
    • Eriksson, U.G.1    Johansson, S.2    Attman, P.O.3    Mulec, H.4    Frison, L.5    Fager, G.6
  • 21
    • 0037256123 scopus 로고    scopus 로고
    • Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor
    • Johansson LC, Frison L, Logren U, Fager G, Gustafsson D, Eriksson UG. Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. Clin Pharmacokinet 2003; 42: 381-92.
    • (2003) Clin. Pharmacokinet. , vol.42 , pp. 381-392
    • Johansson, L.C.1    Frison, L.2    Logren, U.3    Fager, G.4    Gustafsson, D.5    Eriksson, U.G.6
  • 22
  • 23
    • 0037512328 scopus 로고    scopus 로고
    • No influence of obesity on the pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran
    • Sarich TC, Teng R, Peters GR, Wollbratt M, Homolka R,. Svensson M, et al. No influence of obesity on the pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran. Clin Pharmacokinet 2003; 42: 485-92.
    • (2003) Clin. Pharmacokinet. , vol.42 , pp. 485-492
    • Sarich, T.C.1    Teng, R.2    Peters, G.R.3    Wollbratt, M.4    Homolka, R.5    Svensson, M.6
  • 24
    • 19244372487 scopus 로고    scopus 로고
    • No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor
    • Wahlander K, Eriksson-Lepkowska M, Frison L, Fager G, Eriksson UG. No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. Clin Pharmacokinet 2003; 42: 755-64.
    • (2003) Clin. Pharmacokinet. , vol.42 , pp. 755-764
    • Wahlander, K.1    Eriksson-Lepkowska, M.2    Frison, L.3    Fager, G.4    Eriksson, U.G.5
  • 27
    • 0025146426 scopus 로고
    • Clot-bound thrombin is protected from inhibition by heparin-antithrombin III, but is susceptible to inactivation by antithrombin III-independent inhibition
    • Weitz JI, Hudoba M, Massel D, Maraganore J, Hirsh J. Clot-bound thrombin is protected from inhibition by heparin-antithrombin III, but is susceptible to inactivation by antithrombin III-independent inhibition. J Clin Invest 1990; 86: 385-91.
    • (1990) J. Clin. Invest. , vol.86 , pp. 385-391
    • Weitz, J.I.1    Hudoba, M.2    Massel, D.3    Maraganore, J.4    Hirsh, J.5
  • 28
    • 0031936090 scopus 로고    scopus 로고
    • Thrombin binds to soluble fibrin degradation products where it is protected from inhibition by heparin-antithrombin but is susceptible to inactivation by antithrombin-independent inhibitors
    • Weitz J, Leslie B, Hudoba M. Thrombin binds to soluble fibrin degradation products where it is protected from inhibition by heparin-antithrombin but is susceptible to inactivation by antithrombin-independent inhibitors. Circulation 1998; 97: 544-52.
    • (1998) Circulation , vol.97 , pp. 544-552
    • Weitz, J.1    Leslie, B.2    Hudoba, M.3
  • 29
    • 0035871772 scopus 로고    scopus 로고
    • Prothrombin protects factor Xa in the prothrombinase complex from inhibition by the heparin-antithtombin complex
    • Rezaie AR. Prothrombin protects factor Xa in the prothrombinase complex from inhibition by the heparin-antithtombin complex. Blood 2001; 97: 2308-13.
    • (2001) Blood , vol.97 , pp. 2308-2313
    • Rezaie, A.R.1
  • 30
    • 2142812859 scopus 로고    scopus 로고
    • Factor Xa is highly protected from antithrombin-fondaparinux and antithrombin-enoxaparin when incorporated into the prothrombinase complex
    • Brufatto N, Ward A, Nesheim ME. Factor Xa is highly protected from antithrombin-fondaparinux and antithrombin-enoxaparin when incorporated into the prothrombinase complex. J Thromb Haemost 2003; 1: 1258-63.
    • (2003) J. Thromb. Haemost. , vol.1 , pp. 1258-1263
    • Brufatto, N.1    Ward, A.2    Nesheim, M.E.3
  • 31
    • 0033961169 scopus 로고    scopus 로고
    • Pharmacologic modulation of thrombin generation associated with human clots by human purified antithrombin alone or in the presence of low molecular weight heparin or unfractionated heparin
    • Meddahi S, Bara L, Fessi H, Samama MM, Pharmacologic modulation of thrombin generation associated with human clots by human purified antithrombin alone or in the presence of low molecular weight heparin or unfractionated heparin. Blood Cloagul Fibrinolysis 2000; 11: 51-9.
    • (2000) Blood Cloagul. Fibrinolysis , vol.11 , pp. 51-59
    • Meddahi, S.1    Bara, L.2    Fessi, H.3    Samama, M.M.4
  • 32
    • 0027199974 scopus 로고
    • Importance of factor Xa in determining the procoagulant activity of whole-blood clots
    • 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: 1877-83.
    • (1993) J. Clin. Invest. , vol.91 , pp. 1877-1883
    • Eisenberg, P.R.1    Siegel, J.E.2    Abendschein, D.R.3    Miletich, J.P.4
  • 33
    • 0022378677 scopus 로고
    • Effects of heparin, its low molecular weight fractions and other glycosaminoglycans on thrombus growth in vtvo
    • Boneu B, Buchanan MR, Cade JF, Van Ryn J, Fernandez F, Ofosu FA, et al. Effects of heparin, its low molecular weight fractions and other glycosaminoglycans on thrombus growth in vtvo. Thromb Res 1985; 40: 81-89.
    • (1985) Thromb. Res. , vol.40 , pp. 81-89
    • Boneu, B.1    Buchanan, M.R.2    Cade, J.F.3    Van Ryn, J.4    Fernandez, F.5    Ofosu, F.A.6
  • 34
    • 0038157329 scopus 로고    scopus 로고
    • Crystal structure of the Gplba alpha-thrombin complex essential for platelet aggregation
    • Dumas JJ, Kumar R, Seehra J, Somers WS, Mosyak L. Crystal structure of the Gplba alpha-thrombin complex essential for platelet aggregation. Science 2003; 301: 222-6.
    • (2003) Science , vol.301 , pp. 222-226
    • Dumas, J.J.1    Kumar, R.2    Seehra, J.3    Somers, W.S.4    Mosyak, L.5
  • 35
    • 0037815126 scopus 로고    scopus 로고
    • Modulation of alpha-thrombin function by distinct interactions with platelet glycoprotein Ib alpha
    • Celikel R, McClintock RA, Roberts JR, Mendolicchio QL, Ware J, Varughese KI, el al. Modulation of alpha-thrombin function by distinct interactions with platelet glycoprotein Ib alpha. Science 2003; 301: 218-21.
    • (2003) Science , vol.301 , pp. 218-221
    • Celikel, R.1    McClintock, R.A.2    Roberts, J.R.3    Mendolicchio, Q.L.4    Ware, J.5    Varughese, K.I.6
  • 36
    • 0034635224 scopus 로고    scopus 로고
    • 282 region of platelet glycoprotein Ibα interacts with heparin-binding site α-thrombin and protects the enzyme from heparin-catalyzed inhibition by antithrombin III
    • 282 region of platelet glycoprotein Ibα interacts with heparin-binding site α-thrombin and protects the enzyme from heparin-catalyzed inhibition by antithrombin III. J Biol Chem 2000; 275: 3887-3895.
    • (2000) J. Biol. Chem. , vol.275 , pp. 3887-3895
    • De Cristofaro, R.1    De Candia, E.2    Rutella, S.3    Weitz, J.I.4
  • 37
    • 0035128503 scopus 로고    scopus 로고
    • Oral anticoagulants: Mechanism of action, clinical effectiveness, and optimal therapeutic range
    • Hirsh J, Dalen JE, Anderson DR, Poller L, Bussey H, Ansell J, et al. Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range. Chest 2001; 119: 8S-21S.
    • (2001) Chest , vol.119
    • Hirsh, J.1    Dalen, J.E.2    Anderson, D.R.3    Poller, L.4    Bussey, H.5    Ansell, J.6
  • 38
    • 10744222644 scopus 로고    scopus 로고
    • The anticoagulant therapy with bivalirudin to assist in the performance of percutaneous coronary intervention in patients with heparin-induced thrombocytopenia (ATBAT) Study: Main results
    • Mahaffey KW, Lewis BE, Wildermann NM Berkowitz, SD, Oliverio RM, Turco MA, et al. The anticoagulant therapy with bivalirudin to assist in the performance of percutaneous coronary intervention in patients with heparin-induced thrombocytopenia (ATBAT) Study: main results. J Invasive Cardiol 2003; 15: 611-6.
    • (2003) J. Invasive Cardiol. , vol.15 , pp. 611-616
    • Mahaffey, K.W.1    Lewis, B.E.2    Wildermann, N.M.3    Berkowitz, S.D.4    Oliverio, R.M.5    Turco, M.A.6
  • 39
    • 0037176525 scopus 로고    scopus 로고
    • Direct thrombin inhibitors in acute coronary syndromes: Principal results of a meta-analysis based on individual patients' data
    • Direct Thrombin Inhibitor Trialists' Collaborative Group
    • Direct Thrombin Inhibitor Trialists' Collaborative Group. Direct thrombin inhibitors in acute coronary syndromes: principal results of a meta-analysis based on individual patients' data. Lancet 2002; 359:294-302.
    • (2002) Lancet , vol.359 , pp. 294-302
  • 40
    • 0035206428 scopus 로고    scopus 로고
    • Bivalirudin versus heparin during coronary angioplasty for unstable post-infarction angina: The final report of the Bivalirudin Angioplasty Study
    • Bittl JA, Chaitman BR, Feit F, Kimball W, Topol EJ. Bivalirudin versus heparin during coronary angioplasty for unstable post-infarction angina: the final report of the Bivalirudin Angioplasty Study. Am Hear J 200 1; 142: 952-959.
    • (2001) Am. Hear. J. , vol.142 , pp. 952-959
    • Bittl, J.A.1    Chaitman, B.R.2    Feit, F.3    Kimball, W.4    Topol, E.J.5
  • 42
    • 0037453968 scopus 로고    scopus 로고
    • Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial
    • Lincoff AM, Bittl JA, Harrington RA, Feit F, Kleiman NS, Jackman JD, et al. Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial. JAMA 2003; 289: 853-63.
    • (2003) JAMA , vol.289 , pp. 853-863
    • Lincoff, A.M.1    Bittl, J.A.2    Harrington, R.A.3    Feit, F.4    Kleiman, N.S.5    Jackman, J.D.6
  • 43
    • 0343580449 scopus 로고    scopus 로고
    • Comparison of the effects of two doses of recombinant hirudin compared with heparin in patients with acute myocardial ischaemia without ST elevation: A pilot study Organization to Assess Strategies for Ischemic Syndromes (OASIS) Investigators
    • Organization to Assess Strategies for Ischemic Syndromes (OASIS) Investigators
    • Organization to Assess Strategies for Ischemic Syndromes (OASIS) Investigators. Comparison of the effects of two doses of recombinant hirudin compared with heparin in patients with acute myocardial ischaemia without ST elevation: a pilot study. Organization to Assess Strategies for Ischemic Syndromes (OASIS) Investigators. Circulation 1997; 96: 769-77.
    • (1997) Circulation , vol.96 , pp. 769-777
  • 44
    • 0141885177 scopus 로고    scopus 로고
    • Development of proteinase-activated receptor 1 antagonists as terapeutic agents for thrombosis, restenosis and inflammatory diseases
    • Ahm HS, Chackalamannil S, Boykow G, Graziano MP, Foster C. Development of proteinase-activated receptor 1 antagonists as terapeutic agents for thrombosis, restenosis and inflammatory diseases, Curr Pharm Design 2003; 9(28): 2349-65
    • (2003) Curr. Pharm. Design , vol.9 , Issue.28 , pp. 2349-2365
    • Ahm, H.S.1    Chackalamannil, S.2    Boykow, G.3    Graziano, M.P.4    Foster, C.5
  • 45
    • 0742306378 scopus 로고    scopus 로고
    • Adjunctive therapy for percutaneous revascularization in acute myocardial infarction
    • Brener SJ, Topol EJ. Adjunctive therapy for percutaneous revascularization in acute myocardial infarction. Curr Pharm Design 2004; 10(4): 399-405.
    • (2004) Curr. Pharm. Design , vol.10 , Issue.4 , pp. 399-405
    • Brener, S.J.1    Topol, E.J.2
  • 46
    • 0141954082 scopus 로고    scopus 로고
    • Recent advances in the discovery and development of direct coagulation factor Xa inhibitors
    • Gould WR, Leadley RJ. Recent advances in the discovery and development of direct coagulation factor Xa inhibitors. Curr Pharm Design 2003; 9(28): 2337-47.
    • (2003) Curr. Pharm. Design , vol.9 , Issue.28 , pp. 2337-2347
    • Gould, W.R.1    Leadley, R.J.2


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