Fondaparinux sodium: A review of its use in the treatment of acute venous thromboembolism

American Journal of Cardiovascular Drugs

Volumn 5, Issue 5, 2005, Pages 335-346

  Robinson, Dean M ^a   Wellington, Keri ^a  

^a ADIS INTERNATIONAL INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLSALICYLIC ACID; ANTITHROMBIN; ANTIVITAMIN K; BLOOD CLOTTING FACTOR 10A INHIBITOR; BLOOD CLOTTING FACTOR 7; BLOOD CLOTTING FACTOR 9A; CYTOCHROME P450; DALTEPARIN; DIGOXIN; ENOXAPARIN; FONDAPARINUX; HEPARIN; HEPARIN LYASE; LOW MOLECULAR WEIGHT HEPARIN; PENTASACCHARIDE; PIROXICAM; RECOMBINANT BLOOD CLOTTING FACTOR 7A; THROMBIN; WARFARIN;

ANTICOAGULATION; BLEEDING; BODY WEIGHT; CLINICAL TRIAL; CONSTIPATION; CORRELATION ANALYSIS; CREATININE CLEARANCE; DEEP VEIN THROMBOSIS; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG EXCRETION; DRUG EXPOSURE; DRUG FEVER; DRUG METABOLISM; DRUG TOLERABILITY; ECHOGRAPHY; EUROPE; HEADACHE; HEPARIN INDUCED THROMBOCYTOPENIA; HUMAN; INCIDENCE; INSOMNIA; LUNG EMBOLISM; MORTALITY; NAUSEA; NONHUMAN; OUTPATIENT; PRIORITY JOURNAL; PROTEIN CONFORMATION; RECURRENT DISEASE; REVIEW; THROMBOCYTE ACTIVATION; THROMBOCYTOPENIA; THROMBOGENESIS; UNITED STATES; VENOUS THROMBOEMBOLISM;

ACUTE DISEASE; ANTICOAGULANTS; ANTITHROMBIN III; CLINICAL TRIALS; HUMANS; POLYSACCHARIDES; VENOUS THROMBOSIS;

EID: 24944495296     PISSN: 11753277     EISSN: None     Source Type: Journal    
DOI: 10.2165/00129784-200505050-00007     Document Type: Review

References (75)

1. Hyers TM. Management of venous thromboembolism: past, present, and future. Arch Intern Med 2003 Apr 14; 163 (7): 759-68
2. Bates SM, Ginsberg JS. Clinical practice: treatment of deep-vein thrombosis. N Engl J Med 2004 Jul 15; 351 (3): 268-77
3. Hirsh J, Hoak J. Management of deep vein thrombosis and pulmonary embolism: a statement for healthcare professionals. Council on Thrombosis (in consultation with the Council on Cardiovascular Radiology), American Heart Association. Circulation 1996 Jun 15; 93 (12): 2212-45
4. Girard P, Musset D, Parent F, et al. High prevalence of detectable deep venous thrombosis in patients with acute pulmonary embolism. Chest 1999 Oct; 116 (4): 903-8
5. Kearon C. Natural history of venous thromboembolism. Circulation 2003 Jun 17; 107 (23 Suppl. 1): I22-30
6. Barritt DW, Jordan SC. Anticoagulant drugs in the treatment of pulmonary embolism: a controlled trial. Lancet 1960 Jun 18; 1: 1309-12
7. Price GC, Thompson SA, Kam PC. Tissue factor and tissue factor pathway inhibitor. Anaesthesia 2004 May; 59 (5): 483-92
8. Herbert JM, Petitou M, Lormeau JC, et al. SR 90107A/Org 31540, a novel anti-factor Xa antithrombotic agent. Cardiovasc Drug Rev 1997; 15 (1): 1-26
9. US Department of Health and Human Services. Authorisation letter: Arixtra® (fondaparinux sodium) [online]. Available from URL: http://www.fda.gov/ cder/foi/appletter/2004/21345se1-004,005ltr.pdf [Accessed 2005 Mar 22]
10. European Medicines Authority. European public assessment report: (Arixtra®) abstract [online]. Available from URL: http://www.emea.eu.int/ humandocs/Humans/EPAR/arixtra/arixtra.htm [Accessed 2005 Mar 22]
11. GlaxoSmithKline. Arixtra® (fondaparinux sodium): prescribing information [on-line]. Available from URL: http://www.fda.gov/cder/foi/label/ 2005/021345s010lbl.pdf [Accessed 2005 May 30]
12. Reynolds NA, Perry CM, Scott LJ. Fondaparinux sodium: a review of its use in the prevention of venous thromboembolism following major orthopaedic surgery. Drugs 2004; 64 (14): 1575-96
13. GlaxoSmithKline. GlaxoSmithKline receives authorisation from European Commission for use of Arixtra® in medical patients [online]. Available from URL: http://www.gsk.com/media/archive.htm [Accessed 2005 Apr 3]
14. GlaxoSmithKline. European Commission approves new use of Arixtra® for prevention of venous thromboembolic events in abdominal surgery [online]. Available from URL: http://www.gsk.com/media/archive.htm [Accessed 2005 Jul 12]
15. US Department of Health and Human Services. Authorisation letter: Arixtra® (fondaparinux sodium) [online]. Available from URL: http://www.fda.gov/cder/foi/appletter/2005/021345s010ltr.pdf [Accessed 2005 May 30]
16. Walenga JM, Jeske WP, Bara L, et al. Biochemical and pharmacologic rationale for the development of a synthetic heparin pentasaccharide. Thromb Res 1997; 86 (1): 1-36
17. Bauer KA. New pentasaccharides for prophylaxis of deep vein thrombosis: phar-macology. Chest 2003 Dec; 124 (6 Suppl.): 364S-70S
18. de Moerloose P, Boehlen F. Two new antithrombotic agents (fondaparinux and ximelagatran) and their implications in anesthesia. Can J Anaesth 2002 Jun-Jul; 49 (6): S5-10
19. Olson ST, Swanson R, Raub-Segall E, et al. Accelerating ability of synthetic oligosaccharides on antithrombin inhibition of proteinases of the clotting and fibrinolytic systems: comparison with heparin and low-molecular-weight heparin. Thromb Haemost 2004 Nov; 92 (5): 929-39
20. Olson ST, Bjork I, Sheffer R, et al. Role of the antithrombin-binding pentasaccharide in heparin acceleration of antithrombin-proteinase reactions: resolution of the antithrombin conformational change contribution to heparin rate enhancement. J Biol Chem 1992 Jun 25; 267 (18): 12528-38
21. Weitz JI, Hirsh J, Samama MM. New anticoagulant drugs: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest 2004 Sep; 126 (3 Suppl.): 265S-86S
22. Pasi J. The coagulation cascade: old and new. CME Bull Haematol 1997; 1 (1): 3-4
23. Gerotziafas GT, Elalamy I, Depasse F, et al. On the mechanism of inhibition of tissue factor pathway by the synthetic pentasaccharide during coagulation of human plasma. Blood Coagul Fibrinolysis 2003 Oct; 14 (7): 633-8
24. Petitou M, Duchaussoy P, Jaurand G, et al. Synthesis and pharmacological properties of a close analogue of an antithrombotic pentasaccharide (SR 90107A/ORG 31540). J Med Chem 1997 May 23; 40 (11): 1600-7
25. Lormeau JC, Hérault JP, Gaich C, et al. Determination of the anti-factor Xa activity of the synthetic pentasaccharide SR 90107A/ORG 31540 and of two structural analogues. Thromb Res 1997 Jan 1; 85 (1): 67-75
26. Herbert JM, Hérault JP, Bernat A, et al. Biochemical and pharmacological properties of SANORG 34006, a potent and long-acting synthetic pentasaccharide. Blood 1998 Jun; 91 (11): 4197-205
27. Bendetowicz AV, Bara L, Samama MM. The inhibition of intrinsic prothrombinase and its generation by heparin and four derivatives in prothrombin poor plasma. Thromb Res 1990; 58: 445-54
28. 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
29. Gerotziafas GT, Bara L, Bloch MF, et al. Comparative effects of synthetic pentasaccharide, low-molecular-weight heparin, unfractionated heparin and recombinant hirudin on the generation of factor VIIa and prothrombin activation after coagulation of human plasma. Blood Coagul Fibrinolysis 1998; 9 (7): 571-80
30. Lormeau JC, Hérault JP, Herbert JM. Antithrombin-mediated inhibition of factor VIIa-tissue factor complex by the synthetic pentasaccharide representing the heparin binding site to antithrombin. Thromb Haemost 1996 Jul; 76 (1): 5-8
31. Samama MM, Bara L, Walenga J. Comparative mechanism of action and pharmacokinetics of pentasaccharide and LMW heparins. Reprinted from State of the Art book. 16th International Congress on Thrombosis; 2000 May 5-8; Porto, 99-102
32. Pieters J, Lindhout T, Willems G. Heparin-stimulated inhibition of factor IXa generation and factor IXa neutralization in plasma. Blood 1990 Aug 1; 76 (3): 549-54
33. Wiebe EM, Stafford AR, Fredenburgh JC, et al. Mechanism of catalysis of inhibition of factor IXa by antithrombin in the presence of heparin or pentasaccharide. J Biol Chem 2003 Sep 12; 278 (37): 35767-74
34. Hérault JP, Gaich C, Bono F, et al. The structure of synthetic oligosaccharides in relation to factor IXa inhibition. Thromb Haemost 2002; 88 (3): 432-5
35. Pieters J, Willems G, Hemker HC, et al. Inhibition of factor IXa and factor Xa by antithrombin III/heparin during factor X activation. J Biol Chem 1988 Oct 25; 263 (30): 15313-8
36. Lormeau JC, Hérault JP. The effect of the synthetic pentasaccharide SR 90107/ORG 31540 on thrombin generation ex vivo is uniquely due to ATIII-mediated neutralization of factor Xa. Thromb Haemost 1995; 74 (6): 1474-7
37. Walenga JM, Fareed J. Relative contribution of factor Xa and factor IIa. Inhibition in the mediation of the antithrombotic actions of LMWHs and synthetic heparin pentasaccharides. Thromb Haemorrh Disord 1991; 3 (2): 53-9
38. Carrie D, Caranobe C, Saivin S, et al. Pharmacokinetic and antithrombotic properties of two pentasaccharides with high affinity to antithrombin III in the rabbit: comparison with CY216. Blood 1994; 84 (8): 2571-7
39. Messmore HL, Griffin B, Fareed J, et al. In vitro studies of the interaction of heparin, low molecular weight heparin and heparinoids with platelets. Ann NY Acad Sci 1989; 556: 217-31
40. Amiral J, Lormeau JC, Marfaing-Koka A, et al. Absence of cross-reactivity of SR90107A/ORG31540 pentasaccharide with antibodies to heparin-PF4 complexes developed in heparin-induced thrombocytopenia. Blood Coagul Fibrinolysis 1997; 8 (2): 114-7
41. Ahmad S, Jeske WP, Walenga JM, et al. Synthetic pentasaccharides do not cause platelet activation by antiheparin-platelet factor 4 antibodies. Clin App Thromb Hemost 1999; 5 (4): 259-66
42. Walenga JM, Petitou M, Lormeau JC, et al. Antithrombotic activity of a synthetic heparin pentasaccharide in a rabbit stasis thrombosis model using different thrombogenic challenges. Thromb Res 1987; 46: 187-98
43. Pottier P, Planchon B, Truchaud F, et al. Efficacy of pentasaccharide on a prethrombosis model based on a calibrated stasis by the increase in up-stream venous pressure. Blood Coagul Fibrinolysis 2003; 14 (6): 587-91
44. Boneu B, Necciari J, Cariou R, et al. Pharmacokinetics and tolerance of the natural pentasaccharide (SR90107/ORG31540) with high affinity to antithrombin III in man. Thromb Haemost 1995; 74 (6): 1468-73
45. Warkentin TE, Crowther MA. Reversing anticoagulants both old and new. Can J Anaesth 2002 Jun-Jul; 49 (6): S11-25
46. Bijsterveld NR, Moons AH, Boekholdt SM, et al. Ability of recombinant factor VIIa to reverse the anticoagulant effect of the pentasaccharide fondaparinux in healthy volunteers. Circulation 2002; 106 (20): 2550-4
47. Daud AN, Ahsan A, Iqbal O, et al. Synthetic heparin pentasaccharide depolymerization by heparinase I: molecular and biological implications. Clin Appl Thromb Hemost 2001 Jan; 7 (1): 58-64
48. Donat F, Duret JP, Santoni A, et al. The pharmacokinetics of fondaparinux sodium in healthy volunteers. Clin Pharmacokinet 2002; 41 Suppl. 2: 1-9
49. Lieu C, Shi J, Donat F, et al. Fondaparinux sodium is not metabolised in mammalian liver fractions and does not inhibit cytochrome P450-mediated metabolism of concomitant drugs. Clin Pharmacokinet 2002; 41 Suppl. 2: 19-26
50. Paolucci F, Claviés MC, Donat F, et al. Fondaparinux sodium mechanism of action: identification of specific binding to purified and human plasma-derived proteins. Clin Pharmacokinet 2002; 41 Suppl. 2: 11-8
51. Lagrange F, Vergnes C, Brun JL, et al. Absence of placental transfer of pentasaccharide (fondaparinux, Arixtra®) in the dually perfused human cotyledon in vitro. Thromb Haemost 2002; 87 (5): 831-5
52. Rembrandt Investigators. Treatment of proximal deep vein thrombosis with a novel synthetic compound (SR90107A/ORG31540) with pure anti-factor Xa activity: a phase II evaluation. Circulation 2000 Nov 28; 102: 2726-31
53. National Guideline Clearinghouse Summary. Anticoagulation therapy supplement [online]. Available from URL: http://www.guideline.gov [Accessed 2005 Apr 11]
54. European Medicines Authority. European public assessment report: (Quixidar®) summary of product characteristics [online]. Available from URL: http://www.emea.eu.int/humandocs/Humans/EPAR/quixidar/quixidar.htm [Accessed 2005 Mar 22]
55. Faaij RA, Burggraaf J, Schoemaker RC, et al. Absence of an interaction between the synthetic pentasaccharide fondaparinux and oral warfarin. Br J Clin Pharmacol 2002; 54 (3): 304-8
56. Ollier C, Faaij RA, Santoni A, et al. Absence of interaction of fondaparinux sodium with aspirin and piroxicam in healthy male volunteers. Clin Pharmacokinet 2002; 41 Suppl. 2: 31-7
57. Mant T, Fournié P, Ollier C, et al. Absence of interaction of fondaparinux sodium with digoxin in healthy volunteers. Clin Pharmacokinet 2002; 41 Suppl. 2: 39-45
58. Büller HR, Davidson BL, Decousus H, et al. for the MATISSE Investigators. Fondaparinux or enoxaparin for the initial treatment of symptomatic deep venous thrombosis: a randomized trial. Ann Intern Med 2004; 140 (11): 867-73
59. Büller HR, Davidson BL, Decousus H, et al. for the MATISSE Investigators. Subcutaneous fondaparinux versus intravenous unfractionated heparin in the initial treatment of pulmonary embolism [published erratum appears in N Engl J Med 2004; 350 (4): 423]. N Engl J Med 2003 Oct 30; 349 (18): 1695-702
60. Levine M, Gent M, Hirsh J, et al. A comparison of low-molecular-weight heparin administered primarily at home with unfractionated heparin administered in the hospital for proximal deep-vein thrombosis. N Engl J Med 1996 Mar 14; 334 (11): 677-81
61. European Medicines Authority. European public assessment report (Quixidar®): scientific discussion [online]. Available from URL: http://www.emea.eu.int/humandocs/PDFs/EPAR/arixtra/011502en6.pdf [Accessed 2005 Mar 22]
62. Büller HR, Agnelli G, Hull RD, et al. Antithrombotic therapy for venous thromboembolic disease: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest 2004 Sep; 126 (3 Suppl.): 401S-28S
63. Guidelines on diagnosis and management of acute pulmonary embolism. Task Force on Pulmonary Embolism, European Society of Cardiology. Eur Heart J 2000 Aug; 21 (16): 1301-36
64. Dager WE, Andersen J, Nutescu E. Special considerations with fondaparinux therapy: heparin-induced thrombocytopenia and wound healing. Pharmacotherapy 2004 Jul; 24 (7 Pt. 2): 88S-94S
65. Groce JB. Treatment of deep vein thrombosis using low-molecular-weight heparins. Am J Manag Care 2001 Nov; 7 (17 Suppl.): S510-23
66. Weitz JI. New anticoagulants for treatment of venous thromboembolism. Circulation 2004 Aug 31; 110 (9 Suppl. 1): I19-26
67. Wells PS. Outpatient treatment of patients with deep-vein thrombosis or pulmona-ry embolism. Curr Opin Pulm Med 2001 Sep; 7 (5): 360-4
68. Gould MK, Dembitzer AD, Doyle RL, et al. Low-molecular-weight heparins compared with unfractionated heparin for treatment of acute deep venous thrombosis: a meta-analysis of randomized, controlled trials. Ann Intern Med 1999 May 18; 130 (10): 800-9
69. Rosenberg RD. Redesigning heparin. N Engl J Med 2001 Mar 1; 344: 673-5
70. Lindhoff-Last E, Nakov R, Misselwitz F, et al. Incidence and clinical relevance of heparin-induced antibodies in patients with deep vein thrombosis treated with unfractionated or low-molecular-weight heparin. Br J Haematol 2002 Sep; 118 (4): 1137-42
71. Vun CM, Evans S, Chong BH. Cross-reactivity study of low molecular weight heparins and heparinoid in heparin-induced thrombocytopenia. Thromb Res 1996 Mar 1; 81 (5): 525-32
72. Bjorvatn A, Kristiansen F. Fondaparinux sodium compared with enoxaparin sodium: a cost-effectiveness analysis. Am J Cardiovasc Drugs 2005; 5 (2): 121-30
73. U.S. National Institutes of Health. FOndaparinux in ST elevation Myocardial Infarction [online]. Available from URL: http://www.clinicaltrials. gov [Accessed 2005 Apr 6]
74. Simoons ML, Bobbink IW, Boland J, et al. A dose-finding study of fondaparinux in patients with non-ST-segment elevation acute coronary syndromes: the Pentasaccharide in Unstable Angina (PENTUA) study. J Am Coll Cardiol 2004 Jun 16; 43 (12): 2183-90
75. Mehta SR, Steg PG, Granger CB, et al. Randomized, blinded trial comparing fondaparinux with unfractionated heparin in patients undergoing contemporary percutaneous coronary intervention: Arixtra Study in Percutaneous Coronary Intervention. A randomized evaluation (ASPIRE) pilot trial. Circulation 2005 Mar 22; 111 (11): 1390-7