New anticoagulants for venous thromboembolic disease

IDrugs

Volumn 7, Issue 1, 2004, Pages 50-57

  Chang, Patrick ^a  

^a THOMAS JEFFERSON UNIVERSITY   (United States)

Author keywords

Anticoagulants; Factor Xa inhibitors; Fondaparinux; Selective thrombin inhibitors; Tissue factor pathway inhibitor; Ximelagatran

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; [N [4 [(1 ACETIMIDOYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL]ACETIC ACID; ACTIVATED PROTEIN C; ANTICOAGULANT AGENT; ANTICOAGULANT PROTEIN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 9; DROTRECOGIN; FONDAPARINUX; HEPARIN; IDRAPARINUX; LOW MOLECULAR WEIGHT HEPARIN; PLASMIN; RECOMBINANT THROMBOMODULIN; THROMBIN INHIBITOR; TISSUE FACTOR PATHWAY INHIBITOR; WARFARIN; XIMELAGATRAN; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 9A; THROMBIN;

BLOOD CLOTTING; CLINICAL TRIAL; DRUG HALF LIFE; HUMAN; NEMATODE; REVIEW; THROMBOCYTOPENIA; VENOUS THROMBOEMBOLISM; ANIMAL; BLOOD; DRUG ANTAGONISM; DRUG EFFECT; FIBRINOLYSIS; PATHOPHYSIOLOGY; PHYSIOLOGY; VEIN THROMBOSIS;

ANIMALS; ANTICOAGULANTS; FACTOR IXA; FACTOR VIIA; FACTOR XA; FIBRINOLYSIS; HUMANS; THROMBIN; VENOUS THROMBOSIS;

EID: 2142708151     PISSN: 13697056     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (75)

1. Anderson FA Jr, Wheeler HB, Goldberg RJ, Hosmer DW, Patwardhan NA, Jovanovic B, Forcier A, Dalen JE: A population-based perspective of the hospital incidence and case-fatality rates of deep vein thrombosis and pulmonary embolism. The Worcester DVT Study. Arch Intern Med(1991) 151(5):933-938.
2. Davie EW: Biochemical and molecular aspects of the coagulation cascade. Thromb Haemost (1995) 75(1):1-6.
3. Hoffman M, Monroe DM 3rd: A cell-based model of hemostasis. Thromb Haemost (2001) 85(6):958-965. This review provided a new prospective on hemostasis.
4. Hirsh J: Heparin. N Engl J Med (1991) 324(22):1565-1574. An excellent review of the benefits and risks of heparin.
5. Rao LV, Rapaport SI: Studies of a mechanism inhibiting the initiation of the extrinsic pathway of coagulation. Blood (1937) 69(2):645-651.
6. Broze GJ Jr: Tissue factor pathway inhibitor. Thromb Haemost (1995) 74(1):90-93.
7. Brownstein C, Falcone DJ, Jacovina A, Hajjar KA: A mediator of cell surface-specific plasmin generation. Ann NY Acad Sci (2001) 947:143-155.
8. Bajaj MS, Birkroft JJ, Steer SA, Bajaj SP: Structure and biology of tissue factor pathway inhibitor. Thromb Haemost (2001) 86(4):959-972.
9. Hoibraaten E, Qvigstad E, Andersen TO, Mowinckel MC, Sandset PM: The effects of hormone replacement therapy (HRT) on hemostatic variables in women with previous venous thromboembotism - results from a randomized, double-blind, clinical trial. Thromb Haemost (2001) 85(5):775-781.
10. Dahm A, van Hylckama Vlieg A, Bendz B, Rosendaal F, Bertina RM, Sandset PM: Low levels of tissue factor pathway inhibitor (TFPI) increase the risk of venous thrombosis. Blood (2003) 101(11):4387-4392. This article describes the evidence linking TFPI and venous thrombosis.
11. Brown DM, Kania NM, Choi ET, Lantieri LA, Pasia EN, Wun TC, Khouri RK: Local irrigation with tissue factor pathway inhibitor inhibits intimal hyperplasia induced by arterial interventions. Arch Surg (1996) 131(10):1086-1090.
12. Creasey AA, Chang AC, Feigen L, Wun TC, Taylor FB Jr, Hinshaw LB: Tissue factor pathway inhibitor reduces mortality from Escherichia coli septic shock. J Clin Invest (1993) 91(6):2850-2856.
13. Abraham E, Reinhart K, Opal S, Demeyer I, Doig C, Rodriguez AL, Beale R, Svoboda P, Laterre PF, Simon S, Light B et al: Efficacy and safety of tifacogin (recombinant tissue factor pathway inhibitor) in severe sepsis, a randomized controlled trial. J Am Med Assoc (2003) 290(2):238-247. The pivotal study halting further trials of TFPI in severe sepsis.
14. Cappello M, Vlasuk GP, Bergum PW, Huang S, Hotez PJ: Ancylostoma caninum anticoagulant peptide: A hookworm-derived inhibitor of human coagulation Factor Xa. Proc Natl Acad Sci USA (1995) 92(13):6152-6156.
15. Friederich PW, Levi M, Bauer KA, Vlasuk GP, Rote WE, Breederveld D, Keller T, Spataro M, Barzegar S, Buller HR: Ability of recombinant Factor VIIa to generate thrombin during inhibition of tissue factor in human subjects. Circulation (2001) 103(21):2555-2559.
16. Lee A, Agnelli G, Buller H, Ginsberg J, Heit J, Rote W, Vlasuk G, Costantini L, Julian J, Comp P, van Der Meer J et al: Dose response study of recombinant Factor VIIa/tissue Factor inhibitor recombinant nematode anticoagulant protein C2 in the prevention of post-operative venous thromboembolism in patients undergoing total knee replacement. Circulation (2001) 104(1):74-78.
17. Turpie AG: Overview of the clinical results of pentasaccharide in major orthopedic surgery. Haematologica (2001) 86(Suppl 11):59-62. An excellent review of pentasaccharide studies.
18. Presta L, Sims P, Meng YG, Moran P, Bullens S, Bunting S, Schoenfeld J, Lowe D, Lai J, Rancatore P, Iverson M et al: Generation of a humanized, high affinity anti-tissue factor antibody for use as a novel antithrombotic therapeutic. Thromb Haemost (2001) 85(3):379-389.
19. Kelley RF, Refino CJ, O'Connell MP, Modi N, Sehl P, Lowe D, Pater C, Bunting S: A soluble tissue factor mutant is a selective anticoagulant and antithrombotic agent. Blood (1997) 89(9):3219-3227.
20. Soderstrom T, Hedner U, Amljots B: Active site-inactivated Factor VIIa prevents thrombosis without increased surgical bleeding: Topical and intravenous administration in a rat model of deep arterial injury. J Vasc Surg (2001) 33(5):1072-1079.
21. Lincoff AM: First clinical of a tissue-factor inhibitor administered during percutanous coronary revasculatization: A randomized, double-blinded, dose-escalation trial assessing safety and efficacy of FFR-FVIIa in percutanous transluminal coronary angioplasty (ASIS) trial. J Am Coll Cardiol (2000) 36:312-313.
22. Benedict CR, Ryan J, Wolitzky B, Ramos R, Gertach M, Tijburg P, Stern D: 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 (1991) 88(5):1760-1765.
23. Feuerstein GZ, Toomey JR, Valocik R, Koster P, Patel A, Blackburn MN: An inhibitory anti-Factor IX antibody effectively reduces thrombus formation in a rat model of venous thrombosis. Thromb Haemost (1999) 82:1443-1450.
24. Waxman L, Smith DE, Arcuri KE, Vlasuk GP: Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation Factor Xa. Science (1990) 248(4955):593-596.
25. Tuszynski GP, Gasic TB, Gasic GJ: Isolation and characterization of antistasin. An inhibitor of metastasis and coagulation. J Biol Chem (1987) 262(20):9718-9723.
26. Hauptmann J, Kaiser B: Anticoagulant and antithrombotic action of the Factor Xa inhibitor antistasin (ATS). Thromb Res (1993) 71(2):169-174.
27. Faria F, Kelen EM, Sampaio CA, Bon C, Duval N, Chudzinski-Tavassi AM: A new Factor Xa inhibitor (lefaxin) from the Haementeria depressa leech. Thromb Haemost (1999) 82(5):1469-1473.
28. Vlasuk GP, Ramjit D, Fujita T, Dunwiddie CT, Nutt EM, Smith DE, Shebuski RJ: Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective Factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rabbit model of venous thrombosis. Thromb Haemost (1991) 65(3):257-262.
29. Hara T, Yokoyama A, Tanabe K, Ishihara H, Iwamoto M: DX-9065a, an orally active, specific inhibitor of Factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb Haemost (1995) 74(2):635-639.
30. Rogers KL, Chi L, Rapundalo ST, Kramer JB, Gallagher KP: Effects of a Factor Xa inhibitor, DX-9065a, in a novel rabbit model of venous thrombosis. Basic Res Cardiol (1999) 94(1):15-22.
31. Murayama N, Tanaka M, Kunitada S, Yamada H, Inoue T, Terada Y, Fujita M, Ikeda Y: Tolerability, pharmacokinetics, and pharmacodynamics of DX-9065a, a new synthetic potent anticoagulant and specific Factor Xa inhibitor, in healthy male volunteers. Clin Pharmacol Ther (1999) 66(3):258-264. The basic background of DX-9065a is described.
32. Taniuchi Y, Sakai Y, Hisamichi N, Kayama M, Mano Y, Sato K, Hirayama F, Koshio H, Matsumoto Y, Kawasaki T: Biochemical and pharmacologic characterization of YM-60828, a newly synthesized and orally active inhibitor of human Factor Xa. Thromb Haemost (1998) 79(3):543-548.
33. Hirayama F, Koshio H, Katayama N, Ishihara T, Kaizawa H, Taniuchi Y, Sato K, Sakai-Moritani Y, Kaku S, Kurihara H, Kawasaki T et al: Design, synthesis and biological activity of YM-60828 derivatives. Part 2: Potent and orally-bioavailable Factor Xa inhibitors based on benzothiadiazine-4-one template. Bioorg Med Chem (2003) 11(3):367-381.
34. Hirayama F, Koshio H, Ishihara T, Watanuki S, Hachiya S, Kaizawa H, Kuramochi T, Katayama N, Kurihara H, Taniuchi Y, Sato K et al: Design, synthesis and biological activity of YM-60828 derivatives: Potent and orally-bioavailable Factor Xa inhibitors based on naphthoanilide and naphthalensulfonanilide templates. Bioorg Med Chem (2002) 10(8):2597-2610.
35. Sato K, Kawasaki T, Hisamichi N, Taniuchi Y, Hirayama F, Koshio H, Ichihara M, Matsumoto Y: Antithrombotic effects of YM-60828 in three thrombosis models in guinea pigs. Eur J Pharmacol (1998) 350(1):87-91.
36. Kawasaki T, Sato K, Sakai Y, Taniuchi Y, Hirayama F, Koshio H, Ichihara M, Matsumoto Y: Comparative studies of an orally-active Factor Xa inhibitor, YM-60828 with other antithrombotic agents in a rat model of arterial thrombosis. Thromb Haemost (1998) 79(2):410-416.
37. Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM et al: Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2′-(methylsulfonyl)-[1,1-biphenyl] -4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-caroxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation Factor Xa. J Med Chem (2001) 44(4):566-578.
38. Wong PC, Quan ML, Crain EJ, Watson CA, Wexler RR, Knabb RM: Nonpeptide Factor Xa inhibitors: Studies with SF303 and SK549: A new antithrombotic. J Pharmacol Exp Ther (2000) 292(1):351-357.
39. Abendschein DR, Baum PK, Martin DJ, Vergona R, Post J, Rumennik G, Sullivan ME, Eisenberg PR, Light DR: Effects of ZK-807834, a novel inhibitor of Factor Xa, on arterial and venous thrombosis in rabbits. J Cardiovasc Pharmacol (2000) 35(5):796-805.
40. Schering AG: 2002 Annual Report on Form 20-F. Company Publication (2003) March 18.
41. Boneu B, Necciari J, Cariou R, Sie P, Gabaig AM, Kieffer G, Dickinson J, Lamond G, Moelker H, Mant T: Pharmacokinetics and tolerance of the natural pentasaccharide (SR90107/Org31540) with high affinity to antithrombin III in man. Thromb Haemost (1995) 74(6):1468-1473.
42. Herbert JM, Herault JP, Bernat A, van Amsterdam RG, Lormeau JC, Petitou M, van Boeckel C, Hoffmann P, Meuleman DG: Biochemical and pharmacological properties of SANORG 34006, a potent and long-acting synthetic pentasaccharide. Blood (1998) 91(11):4197-4205.
43. Turpie AG, Bauer KA, Eriksson, BI, Lassen MR: Postoperative fondaparinux versus postoperative enoxparin for prevention of venous thromboembolism after elective hip replacement surgery: A randomized double-Mind trial. Lancet (2002) 359(9319):1721-1726.
44. Lassen MR, Bauer KA, Eriksson BI, Turpie AG: Postoperative fondaparinux versus preoperative enoxaparin for prevention of venous thromboembolism in elective hip-replacement surgery: A randomized double-blind comparison. Lancet (2002) 359(9319):1715-1720.
45. Eriksson BI, Bauer KA, Lassen MR, Turpie AG: Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip-fracture surgery. N Engl J Med (2001) 345(18):1298-1304.
46. Bauer KA, Eriksson BI, Lassen MR, Turpie AG: Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after elective major knee surgery. N Engl J Med (2001) 345(18):1305-1310.
47. REMBRANDT Investigators: Treatment of proximal deep vein thrombosis with a novel synthetic compound (SR90107A/Org31540) with a novel synthetic compound (SR90107A/Org1540) with pure anti-Factor Xa activity: A phase II evaluation. Circulation (2000) 102(22):2726-2731.
48. MATISSE Investigators: Fondaparinux (Arixtra) in comparison to low-molecular weight heparin for the initial treament of symptomatic deep venous thrombosis or pulmonary embolism: The Matisse clinical outcome studies. Blood (2002) 100:Abs 83a. The outcome of this trial demonstrated the effectiveness of fondaparinux in treating DVT.
49. MATISSE Investigators: The MATISSE-DVT trial, a randomized, double-blind study comparing once-daily fondaparinux (Arixtra®) with the low-molecular-weight heparin (LMWH) enoxaparin, twice daily, in the initial treatment of symptomatic deep-vein thrombosis (DVT). International Society on Thrombosis and Haemostasia Congress, Birmingham, UK (2003):Abs OC332.
50. Buller HR, Davidson BL, Decousus H, Gallus A, Gent M, Piovella F, Prins MH, Raskob G, van den Berg-Segers AE, Cariou R, Leeuwenkamp O et al: Subcutaneous fondaparinux versus intravenous unfractionated heparin in the initial treatment of pulmonary embolism. N Engl J Med (2003) 349(18):1695-1702.
51. The PERSIST Investigators: A novel long-acting synthetic Factor Xa inhibitor (idraparinux sodium) to replace warfarin for secondary prevention in deep vein thrombosis: A phase II evaluation. Blood (2002) 100:Abs82a. This abstract provides a basic understanding of the clinical parameters of idraparinux.
52. Lee Y, Kim SH, Byun Y: Oral delivery of new heparin derivatives in rats. Pharm Res (2000) 17(10):1259-1264.
53. Rivera TM, Leone-Bay A, Paton DR, Leipold HR, Baughman RA: Oral delivery of heparin in combination with sodium N-[8-(2-hydroxybenzoyl)amino]caprylate: Pharmacological considerations. Pharm Res (1997) 14(12):1830-1834.
54. Baughman RA, Kapoor SC, Agarwal RK, Kisicki J, Catella-Lawson F, FitzGerald GA: Oral delivery of anticoagulant doses of heparin. A randomized, double-blind, controlled study in humans. Circulation (1998) 98(16):1610-1615.
55. Product candidates. Emisphere Technologies Inc, Tarrytown, NY, USA. http://emisphere.com/html/pc_oh.html
56. Abbas, R, Agarwal R, Rivera-Schaub T, Leone-Bay A, Chaudhary K, Baughman RA: Evaluation of the effect of three different oral heparin/SNAC formulations on the pharmacokinetics (PK) of heparin following oral administration in healthy subjects. AAPS PharmSci (2002) 4(4):Abs R6216.
57. Lee J, Arbit E, Maher J, Dinh S, Liu P: Preclinical tolerability monitoring using telemetry of the oral delivery agent, N-[8-2-hydroxybenzoyl) amino]caprylate (SNAC). Safety Pharmacology Society Annual Meeting, Chicago, IL, USA (2001).
58. Malkov D, Wang H, Liang E, Dinh S, Gomez-Orellana I: Mechanism of oral delivery of heparin with EMISPHERE® delivery agents. AAPS PharmSci (2001) 3(3):Abstract.
59. Bounameaux H, Ehringer H, Gast A, Hulting J, Rasche H, Rapold HJ, Reber G, Tschopp TB: Differential inhibition of thrombin activity and thrombin generation by a synthetic direct thrombin inhibitor (napsagatran, Ro 46-6240) and unfractionated heparin in patients with deep vein thrombosis. ADVENT investigators. Thromb Haemost (1999) 81(4):498-501.
60. Greinacher A, Eichler P, Lubenow N, Kwasny H, and Luz M: Heparin-induced thrombocytopenia with thromboembolic complications: Meta-analysls of 2 prospective trials to assess the value of parenteral treatment with lepirudin and its therapeutic aPTT range. Blood (2000) 96(3):846-851.
61. Greinacher A, Janssens U, Berg G, Bock M, Kwasny H, Kemkes-Matthes B, Eichler P, Volpel H, Potzsch B, Luz M: Lepirudin (recombinant hirudin) for parenteral anticoagulation in patients with heparin-induced thrombocytopenia. Circulation (1999) 100(6):587-593. Evidence supporting the use of lepirudin in HIT.
62. Kelton JG: Argatroban - A novel thrombin-specific inhibitor for the treatment of heparin-induced thrombocytopenia. Today's Ther Trends (2002) 20(1):15-35.
63. Hirsh J: Modulating the coagulation cascade: New targets for antithrombotics and anticoagulants. Am Heart J (2001) 142(2 Suppl):S3-S8.
64. Lorrain J, Millet L, Lechaire I, Lochot S, Ferrari P, Visconte C, Sainte-Marie M, Lunven C, Berry CN, Schaeffer P, Herbert JM et al: Antithrombotic properties of SSR182289A, a new, orally active thrombin inhibitor. J Pharmacol Exp Ther (2003) 304(2):567-574.
65. Gustatsson D: Oral direct thrombin inhibitors in clinical development. J Intern Med (2003) 254(4):322-334.
66. Gustafsson D: Pharmacodynamic properties of H376/95, a prodrug of the direct thrombin inhibitor melagatran, intended for oral use. Blood (1997) 94:Abs26a.
67. Eriksson H, Eriksson UG, Frison L, Thorsen M: Intravenous treatment of acute deep vein thrombosis (DVT) with melagatran, a synthetic low molecular weight thrombin inhibitor. Thromb Haemost (1997) 77 (Suppl):Abs OC2411.
68. Eriksson H, Wahlander K, Gustafsson D, Welin LT, Frison L, Schulman S: 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 (2003) 1 (1):41-47. Gives a basic understanding of a drug which could potentially replace warfarin.
69. Bernard GR, Vincent JL, Laterre PF, La Rosa SP, Dhainout JR, Lopez-Rodriguez A, Steingrub JS, Garber GE, Helterbrand JD, Ely EW, Fisher CJ Jr. Efficacy and safety of recombinant activated protein C for severe sepsis. N Engl J Med (2001) 344(10):699-709.
70. Mohri M: ART-123: Recombinant human soluble thrombomodulin. Cardiovasc Drug Rev (2000) 18(4):312-325. Reviews soluble thrombomodulin.
71. Momi S el al: Recombinant soluble thrombomodulin prevents thrombin-induced thromboembolism in mice independently of direct thrombin inhibition. Haematologica (2000) 85(Suppl 5):87-88.
72. Gomi K, Zushi M, Honda G, Kawahara S, Matsuzaki O, Kanabayashi T, Yamamoto S, Maruyama I, Suzuki K: Antithrombotic effect of recombinant human thrombomodulin on thrombin-induced thromboembolism in mice. Blood (1990) 75(7):1396-1399.
73. Aoki Y, Ohishi R, Takei R, Matsuzaki O, Mohri M, Saitoh K, Gomi K, Sugihara T, Kiyoto T, Yamamoto S et al: 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 (1994) 71(4):452-555.
74. Maruyama I: Recombinant thrombomodulin and activated protein C in the treatment of disseminated intravascular coagulation. Thromb Haemost (1999) 82(2):718-721.
75. Ouriel K: Comparison of safety and efficacy of various thrombolytic agents. Rev Cardiovascular Med (2002) 3(Suppl 2):S17-S24.