Skip to main content

Advertisement

SpringerLink
Log in

Apixaban: an emerging oral factor Xa inhibitor

  • Published:
Journal of Thrombosis and Thrombolysis Aims and scope Submit manuscript

Abstract

Apixaban, an oral direct factor Xa inhibitor, is currently in late stage clinical development for the prevention and treatment of thromboembolic diseases. In comparison with current treatment standards for venous thromboembolism (VTE) prophylaxis, apixaban has shown decreased rates of clinically significant bleeding with mixed results in terms of non-inferiority for VTE events. Secondary treatment of VTE with apixaban is currently in phase III clinical study after earlier trials showed comparable safety and efficacy outcomes. The APPRAISE-1 trial, a phase II investigation of apixaban versus placebo following acute coronary syndrome showed a higher risk of clinically significant bleeding in addition to a trend toward decreased ischemic events. A large, international phase III clinical study (APPRAISE-2) of apixaban following acute coronary syndrome is currently underway. Large, phase III studies testing apixaban for the prevention of vascular events in subjects with non-valvular atrial fibrillation are also ongoing.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1

References

  1. Eriksson BI et al (2008) Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost 6(3):457–463

    Article  CAS  PubMed  Google Scholar 

  2. Luettgen JM et al (2006) In vitro evaluation of apixaban, a novel, potent, selective and orally bioavailable factor Xa inhibitor. Blood (ASH Annual Meeting Abstracts) 108(11):4130

    Google Scholar 

  3. Jiang X et al (2009) Apixaban, an oral direct factor Xa inhibitor, inhibits human clot-bound factor Xa activity in vitro. Thromb Haemost 101(4):780–782

    CAS  PubMed  Google Scholar 

  4. Raghavan N et al (2009) Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos 37(1):74–81

    Article  CAS  PubMed  Google Scholar 

  5. He K et al (2006) Preclinical pharmacokinetic and metabolism of apixaban, a potent and selective factor Xa inhibitor. Blood (ASH Annual Meeting Abstracts) 108(11):910

    Google Scholar 

  6. Wong PC et al (2008) Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost 6(5):820–829

    Article  CAS  PubMed  Google Scholar 

  7. Dahl OE et al (2008) Major joint replacement. A model for antithrombotic drug development: from proof-of-concept to clinical use. Int Angiol 27(1):60–67

    CAS  PubMed  Google Scholar 

  8. Lassen MR et al (2007) The efficacy and safety of apixaban, an oral, direct factor Xa inhibitor, as thromboprophylaxis in patients following total knee replacement. J Thromb Haemost 5(12):2368–2375

    Article  CAS  PubMed  Google Scholar 

  9. Geerts WH et al (2008) Prevention of venous thromboembolism: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Chest 133(6 Suppl):381S–453S

    Article  CAS  PubMed  Google Scholar 

  10. Lassen MR et al (2009) Apixaban or enoxaparin for thromboprophylaxis after knee replacement. N Engl J Med 361(6):594–604

    Article  CAS  PubMed  Google Scholar 

  11. Lassen MR, Gallus AS, Pineo GF, Raskob GE (2009) The ADVANCE-2 study: a randomized double-blind trial comparing apixaban with enoxaparin for thromboprophylaxis after total knee replacement. In: International society on thrombosis and haemostasis, Boston, MA

  12. Yoshitake S et al (1985) Nucleotide sequence of the gene for human factor IX (antihemophilic factor B). Biochemistry 24(14):3736–3750

    Article  CAS  PubMed  Google Scholar 

  13. Buller H et al (2008) Efficacy and safety of the oral direct factor Xa inhibitor apixaban for symptomatic deep vein thrombosis. The Botticelli DVT dose-ranging study. J Thromb Haemost 6(8):1313–1318

    Article  CAS  PubMed  Google Scholar 

  14. Alexander JH et al (2009) Apixaban, an oral, direct, selective factor Xa inhibitor, in combination with antiplatelet therapy after acute coronary syndrome: results of the Apixaban for Prevention of Acute Ischemic and Safety Events (APPRAISE) trial. Circulation 119(22):2877–2885

    Article  PubMed  Google Scholar 

  15. Pinto DJ et al (2007) 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 50(22):5339–5356

    Article  CAS  PubMed  Google Scholar 

  16. Eriksson BI, Quinlan DJ, Weitz JI (2009) Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor Xa inhibitors in development. Clin Pharmacokinet 48(1):1–22

    Article  CAS  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Medicine, Duke University Medical Center, Duke University School of Medicine, Durham, NC, USA

    Christopher Roser-Jones

  2. Advanced Biomarkers Program, Duke Clinical Research Institute, Durham, NC, USA

    Christopher Roser-Jones & Richard C. Becker

  3. Divisions of Cardiovascular Medicine and Hematology, Department of Medicine, Duke University Medical Center, Duke University School of Medicine, Durham, NC, USA

    Richard C. Becker

Authors
  1. Christopher Roser-Jones
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Richard C. Becker
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Richard C. Becker.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Roser-Jones, C., Becker, R.C. Apixaban: an emerging oral factor Xa inhibitor. J Thromb Thrombolysis 29, 141–146 (2010). https://doi.org/10.1007/s11239-009-0421-4

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11239-009-0421-4

Keywords

Search

Navigation