Switch Language
Alt tag

Never miss out on the latest news!

Sign up to the Thrombosis Adviser newsletter.

 

Subscribe

See Also

Peripheral Artery Disease: causes and consequences

Coronary Artery Disease: causes and consequences

Factor Xa Inhibitors

This section covers the role of Factor Xa in coagulation, and discusses the use of direct and indirect Factor Xa inhibitors as anticoagulants

Coagulation is initiated when small amounts of thrombin are generated in response to vascular injury and platelets become activated1,2

  • Factor Xa is central to the propagation of coagulation1,2
  • In combination with co-factors bound to activated platelets, Factor Xa amplifies coagulation by converting prothrombin to thrombin1,2
Alt tag

Factor Xa is central to the propagation of coagulation1,2

Activated Factor X, bound as part of the prothrombinase complex on the surface of activated platelets, converts large amounts of prothrombin to thrombin, stimulating the so-called ‘thrombin burst’

 

PL, phospholipid

Factor Xa is positioned at the start of the common pathway of coagulation. As the amount of serine protease is amplified at each step of the cascade, it has been hypothesized that the selective inhibition of coagulation factors above thrombin might be a highly effective antithrombotic strategy.
 

Sylvia Haas, MD

Professor of Medicine and former Director of the Haemostasis and Thrombosis Research Group at the Institute for Experimental Oncology and Therapy Research, Technical University of Munich, Germany
  • Fondaparinux is a synthetic indirect inhibitor of Factor Xa
    • Its chemical structure is based on the natural pentasaccharide contained within heparin and LMWHs3
    • Potentiates the rate of neutralization of Factor Xa by antithrombin and, unlike heparin, does not inactivate thrombin4
    • Does not inhibit Factor Xa bound in the prothrombinase complex; therefore, does not completely inhibit Factor Xa3
    • Administered via subcutaneous injection, limiting long-term use3,4
  • Rivaroxaban, apixaban and edoxaban directly engage the active site of the Factor Xa molecule3,4
    • Inhibit both free Factor Xa in plasma and Factor Xa attached to the prothrombinase complex3,4
    • Administered orally
  • Rivaroxaban, apixaban, and edoxaban have many of the properties of an ideal anticoagulant:5,6
    • Oral administration
    • Fixed-dose regimens
    • Rapid onset and offset of action
    • Show consistent, dose-dependent plasma levels across a range of patient populations
Approved indications in Europe (unless otherwise stated) of the direct Factor Xa inhibitors in adults7-9
  Rivaroxaban Apixaban Edoxaban
Prevention of VTE in patients undergoing elective hip or knee replacement surgery
(Japan only)
Treatment of DVT and PE and prevention of recurrent DVT and PE a a
Prevention of stroke and systemic embolism in patients with NVAF with ≥1 risk factors
Secondary prevention of ACS b x x
Prevention of atherothrombotic events in adult patients with CAD or symptomatic PAD at high risk of ischaemic eventsc x x

aCan be used without pre-treatment with parenteral anticoagulant; bIn patients with elevated cardiac biomarkers and no prior stroke or TIA, and co-administered with ASA or ASA plus clopidogrel or ticlopidine; cco-administered with ASA

References

Never miss out on the latest news!

Sign up to the Thrombosis Adviser newsletter.