645
Views
1
CrossRef citations to date
0
Altmetric
Drug Evaluation

Pharmacodynamics, pharmacokinetics and clinical efficacy of apixaban in the treatment of thrombosis

, &
Pages 575-580 | Received 30 Nov 2015, Accepted 08 Mar 2016, Published online: 01 Apr 2016

References

  • Tagalakis V, Patenaude V, Kahn SR, et al. Incidence of and mortality from venous thromboembolism in a real-world population: the Q-VTE study cohort. Am J Med. 2013;126:832.e13–21. DOI:10.1016/j.amjmed.2013.02.024.
  • Kearon C. Natural history of venous thromboembolism. Circulation. 2003;107:22–30.
  • Barritt DW, Jordan SC. Anticoagulant drugs in the treatment of pulmonary embolism: a controlled trial. Lancet. 1960;1:1309–1312.
  • Carrier M, Le Gal G, Wells PS, et al. Systematic review: case-fatality rates of recurrent venous thromboembolism and major bleeding events among patients treated for venous thromboembolism. Ann Intern Med. 2010;152:578–589.
  • Heit JA, Silverstein MD, Mohr DN, et al. Predictors of survival after deep vein thrombosis and pulmonary embolism: a population-based, cohort study. Arch Intern Med. 1999;159:445–453.
  • Duxbury BM, Poller L. The oral anticoagulant saga: past, present, and future. Clin Appl Thromb Hemost. 2001;7:269–275.
  • Garcia D, Libby E, Crowther MA. The new oral anticoagulants. Blood. 2010;115:15–20.
  • Gallus AS, Baker RI, Chong BH, et al. Consensus guideline for warfarin therapy. Recommendations from the Australasian Society of Thrombosis and Haemostasis. Med J Aust. 2000;172:600–605.
  • Bristol-Myers Squibb Company. Eliquis (apixaban) tablets for oral use: US prescribing information; 2012 [cited 2015 Oct 16]. Available from: http://packageinserts.bms.com/pi/pi_eliquis.pdf
  • Wong PC, Pinto DJP, Zhang D. Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor. J Thromb Thrombolysis. 2011;31:478–492.
  • Pinto DJ, Orwat MJ, 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;50:5339–5356.
  • Jiang X, Crain EJ, Luettgen JM, et al. Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro. Thromb Haemost. 2009;101:780–782.
  • Wong PC, Crain EJ, Xin B, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thomb Haemost. 2008;6:820–829.
  • Barrett YC, Wang J, Knabb R, et al. Apixaban decreases coagulation activity in patients with acute deep-vein thrombosis. Thromb Haemost. 2011;105:181–189.
  • Becker RC, Alexabder JH, Newby LK, et al. Effect of apixaban, an oral and direct factor Xa inhibitor, on coagulation activity biomarkers following acute coronary syndrome. Thromb Haemost. 2010;104:976–983.
  • Wong PC, Jiang X. Apixaban, a direct factor Xa inhibitor, inhibits tissue-factor induced human platelet aggregation in vitro: comparison with direct inhibitiors of factor VIIa, XIa and thrombin. Thromb Haemost. 2010;104:302–310.
  • Barrett YC, Wang Z, Frost C, et al. Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay. Thromb Haemost. 2010;104:1263–1271.
  • Douxfils J, Chatelain C, Chatelain B, et al. Impact of apixaban on routine and specific coagulation assays: a practical laboratory guide. Thromb Haemost. 2013;110:283–294.
  • Beyer J, Trujillo T, Fisher S, et al. Evaluation of a heparin-calibrated anti-Xa assay for measuring the anticoagulant effect of oral direct Xa inhibitors. Clin Appl Thromb Hemost. 2016. doi:10.1177/1076029616629759. [Epub ahead of print].
  • Freyburger G, Macouillard G, Khennoufa K, et al. Rivaroxaban and apixaban in orthopaedics: is there a difference in their plasma concentrations and anticoagulant effects? Blood Coagul Fibrinolysis. 2015;26:925–933.
  • Frost C, Nepal S, Wang J, et al. Safety, pharmacokinetics and pharmacodynamics of multiple oral doses of apixaban, a factor Xa inhibitor, in healthy subjects. Br J Clin Pharmacol. 2013;76:776–786.
  • Zhang D, He K, Raghavan N, et al. Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans. Drug Metab Dispos. 2009;37:1738–1748.
  • European Medicines Agency. Eliquis (apixaban) film-coated tablets: EU summary of product characteristics; 2012 [cited 2015 Oct 18]. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002148/WC500107728.pdf
  • Raghavan N, Frost CE, Yu Z, et al. Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009;37:74–81.
  • Frost CE, Yu Z, Wang J, et al. Single-dose safety and pharmacokinetics of apixaban in subjects with mild or moderate hepatic impairment. Clin Pharmacol Ther. 2009;85(suppl 1):S34. [Abstract].
  • Keating GM. Apixaban: a review of its use for reducing the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. Drugs. 2013;73:825–843.
  • Zhang D, He K, Herbst JJ, et al. Charaterization of efflux transporters involved in distribution and disposition of apixaban. Drug Metab Dispos. 2013;41:827–835.
  • Frost CE, Yan S, Shenker A, et al. Effects of age and gender on the single-dose pharmacokinetics and pharmacodynamics of apixaban. Clin Pharmacokinet. 2015;54:651–662.
  • FDA approved drug product: all approval. 2014 Aug [cited 2015 Oct 20]. Available from: http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Reports.MonthlyApprovalsAll
  • Summary for ARTG entry: 193474 ELIQUIS apixaban 5mg film-coated tablet blister pack. [cited 2015 Oct 20]. Available from: https://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=193474&agid=(PrintDetailsPublic)&actionid=1
  • Kearon C, Akl EA, Comerota AJ, et al. Antithrombotic therapy for VTE disease: antithrombotic therapy and prevention of thrombosis, 9th ed: American College of Chest Physicians evidence-based clinical practice guideline. Chest. 2012;141(2_suppl):e419S–e494S. DOI:10.1378/chest.11-2301.
  • Agnelli G, Buller HR, Cohen A, et al. Oral apixaban for the treatment of acute venous thromboembolism. N Engl J Med. 2013;369:799–808.
  • Agnelli G, Buller HR, Cohen A, et al. Apixaban for extended treatment of venous thromboembolism. N Engl J Med. 2013;368:699–708.
  • The Hokusai-VTE Investiators. Edoxan versus warfarin for the treatment of symptomatic venous thromboembolism. N Engl J Med. 2013;369:1406–1415.
  • The Einstein-PE investigators. Oral rivaroxaban for the treatment of symptomatic pulmonary embolism. N Engl J Med. 2012;366:1287–1297.
  • Schulman S, Kakkar A, Goldhaber SZ, et al. Treatment of acute venous thromboembolism with dabigatran or warfarin and pooled analysis. Circulation. 2014;129:764–772.
  • Granger CB, Alexander JH, McMurray JJV, et al. Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011;365:981–992.
  • Timp Timp JF, Braekkan SK, Versteeg HH, et al. Epidemiology of cancer-associated venous thrombosis. Blood. 2013;122:1712–1723.
  • Mateo J, Oliver A, Borrell M, et al. Laboratory evaluation and clinical characteristics of 2,132 consecutive unselected patients with venous thromboembolism – results of the Spanish multicentric study on thrombophilia (EMET-Study). Thromb Haemost. 1997;77(3):444.
  • Linkins LA, Dans AL, Moores LK, et al. Treatment and prevention of heparin-induced thrombocytopenia. Chest. 2012;141(2_suppl):e495S–530S. DOI:10.1378/chest.11-2303.
  • Barnett AE, Mahan CE, Vazquez SR, et al. Guidance for the practical anticoagulants (DOACs) in VTE treatment. J Thromb Thrombolysis. 2016;41:206–232.
  • Lee AYY, Levine MN, Baker RI, et al Low-molecularweight heparin versus T a coumarin for the prevention of recurrent venous thromboembolism in patients with cancer. N Engl J Med. 2003;349:146–153.
  • Meyer G, Marjanovic Z, Valcke J, et al. Comparison of low molecular weight heparin and warfarin for the secondary prevention of venous thromboembolism in patient wit caner: a randomized controlled study. Arch Inern Med. 2002;162:1729–1735.
  • Hull RD, Pineo GF, Brant RF, et al. Long-term low-molecular-weight heparin versus usual care in proximal-vein thrombosis patients with cancer. Am J Med. 2006;119(12):1062–1072.
  • Cuker A, Siegal DM, Crowther MA, et al. Laboratory measurement of the anticoagulant activity of the target-specific oral anticoagulants: a systemic review. J Am Coll Cardiol. 2014;64:1128–1139.
  • Tran H, Joseph J, Young L, et al. New oral anticoagulants: a practical guide on prescription, laboratory testing and peri-procedural/bleeding management. IMJ. 2014;44:525–536.
  • Siegal DM, Garcia DA, Crowther MA. How I treat target-specific oral anticoagulant-associated bleeding. Blood. 2014;123:1152–1158.
  • Lu G, DeGuzman FR, Hollenbach SJ, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013;19:446–451.
  • Crowther M, Crowther MA. Antidotes for novel oral anticoagulants: current status and future potential. Arterioscler Thromb Vasc Biol. 2015;35:1736–1745.
  • Siegal DM, Curnutte JT, Connolly SJ, et al. Andexanet alfa for the reversal of factor Xa inhibitor activity. N Engl J Med. 2015;373:2413–2424.
  • Liu X, Johnson M, Mardekian J, et al. Apixaban reduces hospitalizations in patients with VTE: an analysis of the AMPLIFY Trial. J Am Coll Cardiol. 2014;63(Suppl 12):A2024. [Abstract].
  • Liu X, Thompson J, Phatak H, et al. Apixaban reduces hospitalization in patients with venous thromboembolism: an analysis of the AMPLIFY-EXT trial. Blood. 2013;122:3638. [Abstract].

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.