Apixaban in the prevention of stroke and systemic embolism in nonvalvular atrial fibrillation

Drugs of Today

Volumn 49, Issue 7, 2013, Pages 425-436

  Pujadas Mestres, L ^a   Escolar, G ^b   Arellano Rodrigo, E ^b   Galan A M ^b  

^a BRISTOL MYERS SQUIBB   (United States)

^b UNIVERSITY OF BARCELONA   (Spain)

Author keywords

Anticoagulants; Apixaban; Atrial fibrillation; Coagulation factor Xa inhibitors; Stroke

Indexed keywords

ACETYLSALICYLIC ACID; AMIODARONE; ANTIVITAMIN K; APIXABAN; CYTOCHROME P450 1A2; CYTOCHROME P450 2J2; CYTOCHROME P450 3A4; DABIGATRAN; ENOXAPARIN; ITRACONAZOLE; KETOCONAZOLE; PHENOBARBITAL; PHENYTOIN; POSACONAZOLE; RIFAMPICIN; RITONAVIR; RIVAROXABAN; VORICONAZOLE; WARFARIN;

ANTICOAGULANT THERAPY; ARTICLE; BLOOD CLOTTING TEST; BRAIN HEMORRHAGE; CEREBROVASCULAR ACCIDENT; CHRONIC KIDNEY DISEASE; COMPARATIVE STUDY; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG METABOLISM; HEART ATRIUM FIBRILLATION; HUMAN; IC 50; IN VITRO STUDY; KIDNEY CLEARANCE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PHASE 3 CLINICAL TRIAL (TOPIC); PROTHROMBIN TIME; SMALL INTESTINE ABSORPTION; THROMBIN TIME; THROMBOCYTE AGGREGATION; TIME TO MAXIMUM PLASMA CONCENTRATION; VEIN THROMBOSIS; VENOUS THROMBOEMBOLISM;

ANTICOAGULANTS; APIXABAN; ATRIAL FIBRILLATION; COAGULATION FACTOR XA INHIBITORS; STROKE;

ANIMALS; ATRIAL FIBRILLATION; CLINICAL TRIALS, PHASE III AS TOPIC; FIBRINOLYTIC AGENTS; HUMANS; PYRAZOLES; PYRIDONES; STROKE; VENOUS THROMBOEMBOLISM;

EID: 84882358721     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2013.49.7.1980498     Document Type: Article

References (59)

1. Lip, g.Y., Brechin, C.M., Lane, D.a. The global burden of atrial fibrillation and stroke: a systematic review of the epidemiology of atrial fibrillation in regions outside North America and Europe. Chest 2012, 142(6): 1489-98.
2. heeringa, J., van der Kuip, D.a., hofman, a. et al. Prevalence, incidence and lifetime risk of atrial fibrillation: the Rotterdam study. Eur heart J 2006, 27(8): 949-53.
3. alberts, M.J., Eikelboom, J.W., hankey, g.J. Antithrombotic therapy for stroke prevention in non-valvular atrial fibrillation. Lancet neurol 2012, 11(12): 1066-81.
4. Menke, J., Luthje, L., Kastrup, a., Larsen, J. Thromboembolism in atrial fibrillation. am J Cardiol 2010, 105(4): 502-10.
5. Fuster, V., ryden, L.E., Cannom, D.S. et al. 2011 ACCF/AHA/HRS focused updates incorporated into the ACC/AHA/ESC 2006 guidelines for the management of patients with atrial fibrillation: a report of the American College of Cardiology Foundation/American Heart Association Task Force on practice guidelines. Circulation 2011, 123(10): e269-367.
6. Watson, T., Shantsila, E., Lip, g.Y. Mechanisms of thrombogenesis in atrial fibrillation: Virchow's triad revisited. Lancet 2009, 373(9658): 155-66.
7. n?strom, E., Escolar, g. Natural anticoagulants and thrombophilia. In:Vol. Blood and Bone Marrow pathology 2nd Edition. a. porwit, J. McCullough, W.n. Erber (Eds.). Elsevier: 2011, 569-81.
8. roberts, h.r., hoffman, M., Monroe, D.M. A cell-based model of thrombin generation. Semin Thromb hemost 2006, 32(Suppl. 1): 32-8.
9. Ben-hadj-Khalifa, S., hezard, n., almawi, W.Y., remy, M.g., Florent, B., Mahjoub, T., nguyen, p. Differential coagulation inhibitory effect of fondaparinux, enoxaparin and unfractionated heparin in cell models of thrombin generation. Blood Coagul Fibrinolysis 2011, 22(5): 369-73.
10. hirsh, J. New anticoagulants. am heart J 2001, 142(2 Suppl): S3-8.
11. Weitz, J.I., hirsh, J., Samama, M.M. New anticoagulant drugs: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest 2004, 126(3 Suppl): 265S-86S.
12. Weitz, J.I., Bates, S.M. New anticoagulants. J Thromb haemost 2005, 3(8): 1843-53.
13. Bauer, K.a. New anticoagulants. hematology am Soc hematol Educ program 2006: 450-6.
14. pinto, D.J., orwat, M.J., Koch, S. et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6, 7-tetrahydro-1H -pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. J Med Chem 2007, 50(22): 5339-56.
15. Bates, S.M., Weitz, J.I., Serradell, n., rosa, E., Bolos, J. Apixaban. Factor Xa inhibitor, anticoagulant. Drugs Fut 2008, 33(4): 293-301.
16. Wong, p.C., pinto, D.J., Zhang, D. Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor. J Thromb Thrombolysis 2011, 31(4): 478-92.
17. he, K., Luettgen, J.M., Zhang, D. et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor. Eur J Drug Metab pharmacokinet 2011, 36(3): 129-39.
18. Luettgen, J.M., Wang, Z., Seiffert, D.a., rendina, a.r., Knabb, r.M., ogletree, M.L. Inhibition of measured thrombin generation in human plasma by apixaban: a predictive mathematical model based on experimentally determined rate constants. 21st Congr Int Soc Thromb haemost (ISTh) (July 6-12, geneva) 2007, abst p-T-633
19. Wong, p.C., Crain, E.J., Watson, C.a., Xin, B. Favorable therapeutic index of the direct factor Xa inhibitors, apixaban and rivaroxaban, compared with the thrombin inhibitor dabigatran in rabbits. J Thromb haemost 2009, 7(8): 1313-20.
20. Jiang, X., Crain, E.J., Luettgen, J.M., Schumacher, W.a., Wong, p.C. Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro. Thromb haemost 2009, 101(4): 780-2.
21. Wong, p.C., Jiang, X. Apixaban, a direct factor Xa inhibitor, inhibits tissue-factor induced human platelet aggregation in vitro: comparison with direct inhibitors of factor VIIa, XIa and thrombin. Thromb haemost 2010, 104(2): 302-10.
22. Samama, M.M., guinet, C. Laboratory assessment of new anticoagulants. Clin Chem Lab Med 2011, 49(5): 761-72.
23. Becker, r.C., Yang, h., Barrett, Y., Mohan, p., Wang, J., Wallentin, L., alexander, J.h. Chromogenic laboratory assays to measure the factor Xa-inhibiting properties of apixaban-an oral, direct and selective factor Xa inhibitor. J Thromb Thrombolysis 2011, 32(2): 183-7.
24. Escolar, g., areiiano-rodrigo, E., reverter, J.C. et al. Coagulation factor concentrates restore alterations in hemostasis induced by a high dose of apixaban: Studies in vitro with circulating human blood. 54th annu Meet am Soc hematol (Dec 8-11, atlanta) 2012, abst 2263
25. Wang, L., raghavan, n., he, K. et al. Sulfation of o-demethyl apixaban: enzyme identification and species comparison. Drug Metab Dispos 2009, 37(4): 802-8.
26. raghavan, n., Frost, C.E., Yu, Z. et al. Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos 2009, 37(1): 74-81.
27. Frost, C., Wang, J., nepal, S. et al. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects. Br J Clin pharmacol 2013, 75(2): 476-87.
28. Frost, C., Yu, Z., Moore, K., et al. Apixaban, an oral direct factor Xa inhibitor: Multiple-dose safety, pharmacokinetics, and pharmacodynamics in healthy subjects. 21st Congr Int Soc Thromb haemost (ISTh) (July 6-12, geneva) 2007, abst p-M-664
29. prom, r., Spinler, S.a. The role of apixaban for venous and arterial thromboembolic disease. ann pharmacother 2011, 45(10): 1262-83.
30. ELIQUIS prescribing information. http://packageinserts. bms.com/pi/pi-eliquis.pdf. accessed
31. Flaker, g.C., hohnloser, S., Wojdyla, D. et al. Apixaban is efficacious and safe in patients with atrial fibrillation using concomitant amiodarone: An analysis from the ARISTOTLE trial. 62nd annu Sci Sess am Coll Cardiol (aCC) (March 9-11, San Francisco) 2013, abst 914-6.
32. Leil, T.a., Feng, Y., Zhang, L., paccaly, a., Mohan, p., pfister, M. Quantification of apixaban's therapeutic utility in prevention of venous thromboembolism: selection of phase III trial dose. Clin pharmacol Ther 2010, 88(3): 375-82.
33. Lassen, M.r., raskob, g.E., gallus, a., pineo, g., Chen, D., portman, r.J. Apixaban or enoxaparin for thromboprophylaxis after knee replacement. n Engl J Med 2009, 361(6): 594-604.
34. Lassen, M.r., raskob, g.E., gallus, a., pineo, g., Chen, D., hornick, p. Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2): a randomised double-blind trial. Lancet 2010, 375(9717): 807-15.
35. Lassen, M.r., gallus, a., raskob, g.E., pineo, g., Chen, D., ramirez, L.M. Apixaban versus enoxaparin for thromboprophylaxis after hip replacement. n Engl J Med 2010, 363(26): 2487-98.
36. Lassen, M.r. Practical use of apixaban in the prevention of venous thromboembolism after total knee or hip replacement. Drugs Today (Barc) 2012, 48(4): 249-58.
37. Eikelboom, J.W., o'Donnell, M., Yusuf, S. et al. Rationale and design of AVERROES: apixaban versus acetylsalicylic acid to prevent stroke in atrial fibrillation patients who have failed or are unsuitable for vitamin K antagonist treatment. am heart J 2010, 159(3): 348-53 e1.
38. Lopes, r.D., alexander, J.h., al-Khatib, S.M. et al. Apixaban for reduction in stroke and other ThromboemboLic events in atrial fibrillation (ARISTOTLE) trial: design and rationale. am heart J 2010, 159(3): 331-9.
39. Connolly, S.J., Eikelboom, J., Joyner, C. et al. Apixaban in patients with atrial fibrillation. n Engl J Med 2011, 364(9): 806-17.
40. granger, C.B., alexander, J.h., McMurray, J.J. et al. Apixaban versus warfarin in patients with atrial fibrillation. n Engl J Med 2011, 365(11): 981-92.
41. Cowper, p.a., pan, W., anstrom, K., et al. Apixaban reduces hospitalization in patients with atrial fibrillation: An analysis of the effect of apixaban therapy on resource use in the apixaban for reduction in stroke and other thromboembolic events in atrial fibrillation trial. 62nd annu Sci Sess am Coll Cardiol (aCC) (March 9-11, San Francisco) 2013, abst 1245-108.
42. Bristol-Myers Squibb and Pfizer announce U.S. FDA approval of ELIQUIS(R) (apixaban) [news release]. Bristol-Myers Squibb, December 28, 2012. accessed July 23, 2013.
43. ELIQUIS(R) (apixaban) approved in Europe for prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation [news release]. Bristol-Myers Squibb, november 20, 2012. accessed July 23, 2013.
44. Coresh, J., Selvin, E., Stevens, L.a. et al. Prevalence of chronic kidney disease in the United States. JaMa 2007, 298(17): 2038-47.
45. Soliman, E.Z., prineas, r.J., go, a.S. et al. Chronic kidney disease and prevalent atrial fibrillation: the Chronic Renal Insufficiency Cohort (CRIC). am heart J 2010, 159(6): 1102-7.
46. alonso, a., Lopez, F.L., Matsushita, K. et al. Chronic kidney disease is associated with the incidence of atrial fibrillation: the Atherosclerosis Risk in Communities (ARIC) study. Circulation 2011, 123(25): 2946-53.
47. piccini, J.p., hernandez, a.F., Zhao, X., patel, M.r., Lewis, W.r., peterson, E.D., Fonarow, g.C. Quality of care for atrial fibrillation among patients hospitalized for heart failure. J am Coll Cardiol 2009, 54(14): 1280-9.
48. Marinigh, r., Lane, D.a., Lip, g.Y. Severe renal impairment and stroke prevention in atrial fibrillation: implications for thromboprophylaxis and bleeding risk. J am Coll Cardiol 2011, 57(12): 1339-48.
49. Eikelboom, J.W., Connolly, S.J., gao, p. et al. Stroke risk and efficacy of apixaban in atrial fibrillation patients with moderate chronic kidney disease. J Stroke Cerebrovasc Dis 2012, 21(6): 429-35.
50. hohnloser, S.h., hijazi, Z., Thomas, L. et al. Efficacy of apixaban when compared with warfarin in relation to renal function in patients with atrial fibrillation: insights from the ARISTOTLE trial. Eur heart J 2012, 33(22): 2821-30.
51. Diener, h.C., Eikelboom, J., Connolly, S.J. et al. Apixaban versus aspirin in patients with atrial fibrillation and previous stroke or transient ischaemic attack: a predefined subgroup analysis from AVERROES, a randomised trial. Lancet neurol 2012, 11(3): 225-31.
52. Easton, J.D., Lopes, r.D., Bahit, M.C. et al. Apixaban compared with warfarin in patients with atrial fibrillation and previous stroke or transient ischaemic attack: a subgroup analysis of the ARISTOTLE trial. Lancet neurol 2012, 11(6): 503-11.
53. Camm, a.J., Lip, g.Y., De Caterina, r. et al. 2012 focused update of the ESC Guidelines for the management of atrial fibrillation: an update of the 2010 ESC Guidelines for the management of atrial fibrillation-developed with the special contribution of the European Heart Rhythm Association. Europace 2012, 14(10): 1385-413.
54. Lip, g.Y., Frison, L., halperin, J.L., Lane, D.a. Comparative validation of a novel risk score for predicting bleeding risk in anticoagulated patients with atrial fibrillation: the HASBLED (Hypertension, Abnormal Renal/Liver Function, Stroke, Bleeding History or Predisposition, Labile INR, Elderly, Drugs/Alcohol Concomitantly) score. J am Coll Cardiol 2011, 57(2): 173-80.
55. Flaker, g.C., Eikelboom, J.W., Shestakovska, o. et al. Bleeding during treatment with aspirin versus apixaban in patients with atrial fibrillation unsuitable for warfarin: the apixaban versus acetylsalicylic acid to prevent stroke in atrial fibrillation patients who have failed or are unsuitable for vitamin K antagonist treatment (AVERROES) trial. Stroke 2012, 43(12): 3291-7.
56. Lip, g.Y., Connolly, S., Yusuf, S. et al. Modification of outcomes with aspirin or apixaban in relation to CHADS(2) and CHA(2)DS(2)-VASc scores in patients with atrial fibrillation: a secondary analysis of the AVERROES study. Circ arrhythm Electrophysiol 2013, 6(1): 31-8.
57. Lopes, r.D., al-Khatib, S.M., Wallentin, L. et al. Efficacy and safety of apixaban compared with warfarin according to patient risk of stroke and of bleeding in atrial fibrillation: a secondary analysis of a randomised controlled trial. Lancet 2012, 380(9855): 1749-58.
58. agnelli, g., Buller, h. r., Cohen, a. et al. Oral apixaban for the treatment of acute venous thromboembolism. n Engl J Med 2013, advance publication.
59. agnelli, g., Buller, h. r., Cohen, a. et al. Apixaban for extended treatment of venous thromboembolism. n Engl J Med 2013, 368(8): 699-708.