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Gregory Wcisel, D. Joyce, Arna Gudmundsdóttir, D. Shasby (2002)
Human recombinant activated protein C in meningococcal sepsis.Chest, 121 1
C. Esmon (2001)
Role of Coagulation Inhibitors in InflammationThrombosis and Haemostasis, 86
L. Rao, M. Ezban (2000)
Active site‐blocked activated factor VII as an effective antithrombotic agent: mechanism of actionBlood Coagulation & Fibrinolysis, 11
B.I. Eriksson, G. Agnelli, A.T. Cohen (2003)
Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacementThromb Haemost, 89
Blood Coagulation, Fibrinolysis and Cellular Haemostasis
S. Worthley, J. Osende, G. Helft, J. Badimón, V. Fuster (2001)
Coronary artery disease: pathogenesis and acute coronary syndromes.The Mount Sinai journal of medicine, New York, 68 3
G. Feuerstein, J. Toomey, R. Valocik, P. Koster, A. Patel, M. Blackburn (1999)
An Inhibitory Anti-factor IX Antibody Effectively Reduces Thrombus Formation in a Rat Model of Venous ThrombosisThrombosis and Haemostasis, 82
R. Hull, G. Pineo, P. Stein, A. Mah, S. Macisaac, O. Dahl, Matthew Butcher, R. Brant, W. Ghali, D. Bergqvist, G. Raskob (2001)
Extended Out-of-Hospital Low-Molecular-Weight Heparin Prophylaxis against Deep Venous Thrombosis in Patients after Elective Hip ArthroplastyAnnals of Internal Medicine, 135
P. Hogg, C. Jackson (1989)
Fibrin monomer protects thrombin from inactivation by heparin-antithrombin III: implications for heparin efficacy.Proceedings of the National Academy of Sciences of the United States of America, 86 10
A. Turpie, K. Bauer, B. Eriksson, M. Lassen (2002)
Postoperative fondaparinux versus postoperative enoxaparin for prevention of venous thromboembolism after elective hip-replacement surgery: a randomised double-blind trialThe Lancet, 359
K. Bauer, B. Eriksson, M. Lassen, A. Turpie (2001)
Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after elective major knee surgery.The New England journal of medicine, 345 18
S. Nand (1993)
Hirudin therapy for heparin-associated thrombocytopenia and deep venous thrombosisAm J Hematol, 43
Agnes Lee, G. Agnelli, H. Büller, J. Ginsberg, J. Heit, W. Rote, G. Vlasuk, L. Costantini, J. Julian, P. Comp, J. Meer, F. Piovella, G. Raskob, M. Gent (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 ReplacementCirculation: Journal of the American Heart Association, 104
T. Rydel, K. Ravichandran, A. Tulinsky, W. Bode, R. Huber, C. Roitsch, J. Fenton (1990)
The structure of a complex of recombinant hirudin and human alpha-thrombin.Science, 249 4966
C. Kearon, M. Gent, J. Hirsh, J. Weitz, M. Kovacs, D. Anderson, A. Turpie, D. Green, Jeffrey Ginsberg, P. Wells, B. Mackinnon, J. Julian (1999)
A comparison of three months of anticoagulation with extended anticoagulation for a first episode of idiopathic venous thromboembolism.The New England journal of medicine, 340 12
E. Abraham, K. Reinhart, P. Svoboda, A. Seibert, D. Olthoff, A. Nogare, R. Postier, G. Hempelmann, T. Butler, E. Martin, C. Zwingelstein, Sandra Percell, V. Shu, A. Leighton, A. Creasey (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 studyCritical Care Medicine, 29
I. Fox, Adrian Dawson, P. Loynds, Jane Eisner, K. Findlen, Elizabeth Levin, D. Hanson, T. Mant, J. Wagner, J. Maraganore (1993)
Anticoagulant Activity of Hirulog™, a Direct Thrombin Inhibitor, in HumansThrombosis and Haemostasis, 69
V. Fuster, L. Badimon, J.J. Badimon (1992)
The pathogenesis of coronary artery disease and the acute coronary syndromesN Engl J Med, 326
S. Bajaj, S. Rapaport, S. Maki (1985)
A monoclonal antibody to factor IX that inhibits the factor VIII:Ca potentiation of factor X activation.The Journal of biological chemistry, 260 21
R.D. Hull, G.F. Pineo, P.D. Stein (2001)
Extended out-of-hospital low-molecular-weight heparin prophylaxis against deep venous thrombosis in patients after elective hip arthroplasty: a systemic reviewAnn Intern Med, 135
(1998)
Effects of recombinant hirudin (lepirudin) compared with heparin on death, myocardial infarction, refractory angina, and revascularization procedures in patients with acute myocardial ischemia without ST elevation: a randomized trialLancet, 353
D. Fitzgerald, Natalie Murphy (1996)
Argatroban: a synthetic thrombin inhibitor of low relative molecular mass.Coronary artery disease, 7 6
J. Heit, C. Colwell, C. Francis, Jeffrey Ginsberg, S. Berkowitz, J. Whipple, G. Peters (2001)
Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement: a phase 2 dose-finding study.Archives of internal medicine, 161 18
J. Herbert, J. Herault, A. Bernat, Van Amsterdam, J. Lormeau, M. Petitou, C. Boeckel, P. Hoffmann, D. Meuleman (1998)
Biochemical and pharmacological properties of SANORG 34006, a potent and long-acting synthetic pentasaccharide.Blood, 91 11
P. Petersen (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 [abstract]Blood, 98
B. Eriksson, P. Kälebo, David Bergqvisty, O. Dahl, S. Lindbratt, A. Bylock, L. Frison, UG Eriksson, L. Welin, D. Gustafsson (2002)
Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trialThe Lancet, 360
F. Schiele, A. Vuillemenot, P. Kramarz, Y. Kieffer, T. Anguenot, Y. Bernard, J. Bassand (1995)
Use of recombinant hirudin as antithrombotic treatment in patients with heparin‐induced thrombocytopeniaAmerican Journal of Hematology, 50
F. Riess, Christine Löwer, Christoph Seelig, N. Bleese, J. Kormann, G. Müller‐Berghaus, B. Pötzsch (1995)
Recombinant hirudin as a new anticoagulant during cardiac operations instead of heparin: successful for aortic valve replacement in man.The Journal of thoracic and cardiovascular surgery, 110 1
Claude, R. Benedict, Jane Ryan, Barry, Wolitzky, Robert, Ramos, Marlène, Gerlach, Pim, Tijburg, David Stem (1991)
Active site-blocked factor IXa prevents intravascular thrombus formation in the coronary vasculature without inhibiting extravascular coagulation in a canine thrombosis model.The Journal of clinical investigation, 88 5
J. Toomey, Michael Blackburn, Barbara Storer, R. Valocik, Paul Koster, G. Feuerstein (2000)
Comparing the antithrombotic efficacy of a humanized anti-factor IX(a) monoclonal antibody (SB 249417) to the low molecular weight heparin enoxaparin in a rat model of arterial thrombosis.Thrombosis research, 100 1
J. Weitz (1997)
Low-molecular-weight heparins.The New England journal of medicine, 337 10
(1997)
Comparison of the effects of two doses of recombinant hirudin compared with heparin in patients with acute myocardial ischemia without ST elevation: a pilot studyCirculation, 96
B. Eriksson, K. Bauer, M. Lassen, A. Turpie (2001)
Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip-fracture surgery.The New England journal of medicine, 345 18
J. Parkinson, B. Grinnell, R. Moore, J. Hoskins, C. Vlahos, N. Bang (1990)
Stable expression of a secretable deletion mutant of recombinant human thrombomodulin in mammalian cells.The Journal of biological chemistry, 265 21
J. Eikelboom, D. Quinlan, J. Douketis (2001)
Extended-duration prophylaxis against venous thromboembolism after total hip or knee replacement: a meta-analysis of the randomised trialsThe Lancet, 358
B. Furie, B. Furie (1992)
Molecular and cellular biology of blood coagulation.The New England journal of medicine, 326 12
B. Eriksson, P. Kälebo, B. Zachrisson, S. Ekman, D. Bach, P. Close (1996)
Prevention of deep-vein thrombosis after total hip replacement: direct thrombin inhibition with recombinant hirudin, CGP 39393The Lancet, 347
Bengt Eriksson, Peer Wille-Jørgensen, P. Kälebo, P. Mouret, N. Rosencher, Peter Bosch, Markus Baur, Steffan Ekman, Doris Bach, S. Lindbratt, Philippe Close (1997)
A comparison of recombinant hirudin with a low-molecular-weight heparin to prevent thromboembolic complications after total hip replacement.The New England journal of medicine, 337 19
J. Maraganore, P. Bourdon, J. Jablonski, K. Ramachandran, J. Fenton (1990)
Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin.Biochemistry, 29 30
K. Stringer, J. Lindenfeld (1992)
Hirudins: Antithrombin AnticoagulantsAnnals of Pharmacotherapy, 26
S. Stone, J. Hofsteenge (1986)
Kinetics of the inhibition of thrombin by hirudin.Biochemistry, 25 16
J. Herbert, A. Bernat, F. Dol, J. Hérault, B. Crépon, J. Lormeau (1996)
DX 9065A a novel, synthetic, selective and orally active inhibitor of factor Xa: in vitro and in vivo studies.The Journal of pharmacology and experimental therapeutics, 276 3
Robert Baughman, S. Kapoor, Rajesh Agarwal, James Kisicki, F. Catella-Lawson, Garret Fitzgerald (1998)
Oral delivery of anticoagulant doses of heparin. A randomized, double-blind, controlled study in humans.Circulation, 98 16
J. Witting, P. Bourdon, D. Brezniak, J. Maraganore, J. Fenton, J. Fenton (1992)
Thrombin-specific inhibition by and slow cleavage of hirulog-1.The Biochemical journal, 283 ( Pt 3)
A. Lincoff, J. Bittl, R. Harrington, F. Feit, N. Kleiman, J. Jackman, I. Sarembock, D. Cohen, D. Spriggs, R. Ebrahimi, G. Keren, J. Carr, E. Cohen, A. Betriu, W. Desmet, D. Kereiakes, W. Rutsch, R. Wilcox, P. Feyter, A. Vahanian, E. Topol (2003)
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, 289 7
J. Weitz, M. Hudoba, D. Massel, J. Maraganore, J. Hirsh (1990)
Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors.The Journal of clinical investigation, 86 2
M.R. Lassen, K.A. Bauer, B.I. Eriksson (2002)
Postoperative fondaparinux versus preoperative enoxaparin for prevention of venous thromboembolism in elective hip replacement surgery; a randomised double-blind comparisonLancet, 359
J. Vasquez, A. Vichiendilokkul, Syed Mahmood, F. Baciewicz (2002)
Anticoagulation with bivalirudin during cardiopulmonary bypass in cardiac surgery.The Annals of thoracic surgery, 74 6
J. Hirsh (1991)
Drug therapy : heparinThe New England Journal of Medicine, 324
G. Agnelli, P. Prandoni, M. Santamaria, P. Bagatella, A. Iorio, M. Bazzan, M. Moia, G. Guazzaloca, A. Bertoldi, C. Tomasi, G. Scannapieco, W. Ageno (2001)
Three months versus one year of oral anticoagulant therapy for idiopathic deep venous thrombosis. Warfarin Optimal Duration Italian Trial Investigators.The New England journal of medicine, 345 3
T. Ortel, Beng Chong (1998)
New treatment options for heparin-induced thrombocytopenia.Seminars in hematology, 35 4 Suppl 5
D. Tollefsen (1995)
Insight into the Mechanism of Action of Heparin Cofactor IIThrombosis and Haemostasis, 74
J. Bittl, B. Chaitman, F. Feit, William Kimball, E. Topol (2001)
Bivalirudin versus heparin during coronary angioplasty for unstable or postinfarction angina: Final report reanalysis of the Bivalirudin Angioplasty Study.American heart journal, 142 6
Ean, L, Ouis, Incent, Ay, S. S., Teingrub, Effrey, H. D., Elterbrand (2001)
Efficacy and safety of recombinant human activated protein C for severe sepsis.The New England journal of medicine, 344 10
Kevin Schulman (1995)
Cost-effectiveness analyses.The New England journal of medicine, 332 2
J. Hirsh (1991)
HeparinN Engl J Med, 324
J. Weitz, B. Leslie, M. Hudoba (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 6
K. Gomi, M. Zushi, G. Honda (1990)
Antithrombotic effect of recombinant human thrombomodulin on thrombin-induced thromboembolism in miceBlood, 75
H. White, Hirulog, Early Investigators (2001)
Thrombin-specific anticoagulation with bivalirudin versus heparin in patients receiving fibrinolytic therapy for acute myocardial infarction: the HERO-2 randomised trialThe Lancet, 358
S. Schulman, A.-S. Rhedin, P. Lindmarker (1995)
A comparison of six weeks with six months of oral anticoagulant therapy after a first episode of venous thromboembolismN Engl J Med, 332
L. Alberio, B. Lämmle, C. Esmon (2001)
Protein C replacement in severe meningococcemia: rationale and clinical experience.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, 32 9
M. Eijnden, Sari-lrina Steenhauer, P. Reitsma, R. Bertina (1997)
Tissue Factor Expression during Monocyte-Macrophage DifferentiationThrombosis and Haemostasis, 77
S. Yusuf, C. Granger, J. Eikelboom, S. Mehta, J. Pogue, P. Tait, S. Behar, M. Benderly, H. Hod, E. Kaplinsky, Natasha Barrett, R. Bilke, M. Luz, M. Marhoefer, L. Roi, D. Trenery, J. Bittl, H. Boersma, M. Flather, C. Baigent, M. Simoons, R. Califf, K. Pieper, E. Topol, J. Weitz, P. Serruys, H. White, K. Neuhaus, U. Zeymer, J. Simes, P. Close, Susan Edwards, P. Gallo, M. Henis, Sonia Anand, William Kimball, C. Meanwell, J. Villiger, E. Antman, E. Braunwald, M. Gibson, S. Murphy, L. Grip, P. Held, Trialist Dti. (2002)
Direct thrombin inhibitors in acute coronary syndromes: principal results of a meta-analysis based on individual patients' dataThe Lancet, 359
M. Gonze, J. Manord, A. Leone-Bay, R. Baughman, C. Garrard, W. Sternbergh, S. Money (1998)
Orally administered heparin for preventing deep venous thrombosis.American journal of surgery, 176 2
D. Gustafsson, J. Nyström, S. Carlsson, U. Bredberg, U. Eriksson, E. Gyzander, M. Elg, T. Antonsson, K. Hoffmann, A. Ungell, H. Sørensen, S. Någård, Anna Abrahamsson, R. Bylund (2001)
The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects.Thrombosis research, 101 3
P. Walsh (2001)
Roles of Platelets and Factor XI in the Initiation of Blood Coagulation by ThrombinThrombosis and Haemostasis, 86
G. Broze (1995)
Tissue Factor Pathway InhibitorThrombosis and Haemostasis, 74
M. Yamamoto, T. Nakagaki, W. Kisiel (1992)
Tissue factor-dependent autoactivation of human blood coagulation factor VII.The Journal of biological chemistry, 267 27
G. Vlasuk (1993)
Structural and Functional Characterization of Tick Anticoagulant Peptide (TAP): A Potent and Selective Inhibitor of Blood Coagulation Factor XaThrombosis and Haemostasis, 70
P. Bergum, A. Cruikshank, S. Maki, C. Kelly, W. Ruf, G. Vlasuk (2001)
Role of Zymogen and Activated Factor X as Scaffolds for the Inhibition of the Blood Coagulation Factor VIIa-Tissue Factor Complex by Recombinant Nematode Anticoagulant Protein c2*The Journal of Biological Chemistry, 276
T. Rivera, A. Leone-Bay, D. Paton, H. Leipold, R. Baughman (1997)
Oral Delivery of Heparin in Combination with Sodium N-[8-(2-Hydroxybenzoyl)amino]caprylate: Pharmacological ConsiderationsPharmaceutical Research, 14
P. Prandoni, A. Lensing, A. Cogo, S. Cuppini, S. Villalta, M. Carta, A. Cattelan, P. Polistena, E. Bernardi, M. Prins (1996)
The Long-Term Clinical Course of Acute Deep Venous ThrombosisAnnals of Internal Medicine, 125
R. Harvey, E. Degryse, L. Stefani, F. Schamber, J. Cazenave, M. Courtney, P. Tolstoshev, J. Lecocq (1986)
Cloning and expression of a cDNA coding for the anticoagulant hirudin from the bloodsucking leech, Hirudo medicinalis.Proceedings of the National Academy of Sciences of the United States of America, 83 4
A. Leone-Bay, T. Rivera-Schaub, S. Majuru (2001)
Phase I study to assess the safety and tolerability of an oral heparin tablet [abstract]Blood, 98
P. Stassens, P. Bergum, Y. Gansemans, L. Jespers, Y. Laroche, Steven Huang, S. Maki, J. Messens, M. Lauwereys, M. Cappello, P. Hotez, I. Lasters, G. Vlasuk (1996)
Anticoagulant repertoire of the hookworm Ancylostoma caninum.Proceedings of the National Academy of Sciences of the United States of America, 93 5
Y. Aoki, Rika Ohishi, Ryoichi Takei, O. Matsuzaki, M. Mohri, Kengo Saitoh, K. Gomi, T. Sugihara, T. Kiyota, Shuji Yamamoto, T. Ishida, I. Maruyama (1994)
Effects of Recombinant Human Soluble Thrombomodulin (rhs-TM) on a Rat Model of Disseminated Intravascular Coagulation with Decreased Levels of Plasma Antithrombin IIIThrombosis and Haemostasis, 71
J. Bittl, J. Strony, J. Brinker, W. Ahmed, C. Meckel, B. Chaitman, J. Maraganore, E. Deutsch, B. Adelman, B. Adelman (1995)
Treatment with bivalirudin (Hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. Hirulog Angioplasty Study Investigators.The New England journal of medicine, 333 12
Arterial and venous thrombosis are a major cause of morbidity and mortality. Anticoagulants are a cornerstone of treatment in patients with these disorders. The two most frequently used anticoagulants, heparin and warfarin, have pharmacological and/or biophysical limitations that make them difficult to use in day-to-day clinical practice. Development of new anticoagulants, which were designed to overcome these limitations, has been facilitated by an increased understanding of the coagulation cascade, the advent of molecular modeling and structure-based drug design, and the realization that the treatment of thrombosis and its complications consumes billions of dollars in annual healthcare expenditures. New anticoagulants target various steps in the coagulation pathway. Coagulation is triggered by the factor VIIa/tissue factor complex and propagated by factors Xa and IXa, together with their activated cofactors, factor Va and VIIIa, respectively. Thrombin, the final effector in coagulation, then converts soluble fibrinogen into insoluble fibrin, the major matrix protein of the clot. New anticoagulation drugs that target each of these clotting enzymes have been developed. This review will focus on those drugs in more advanced stages of clinical evaluation. These include inhibitors of initiation of coagulation (tissue factor pathway inhibitor, nematode anticoagulant peptide and active-site blocked factor VIIa), inhibitors of propagation of coagulation (active-site blocked factor IXa, antibodies against factor IX/IXa, fondaparinux sodium, direct factor Xa inhibitors, protein C derivatives and soluble thrombomodulin), and thrombin inhibitors (hirudin, bivalirudin, argatroban and ximelagatran).
American Journal of Cardiovascular Drugs – Springer Journals
Published: Sep 20, 2012
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