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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
In this section:
The role of Factor Xa in coagulation
Coagulation is initiated when small amounts of thrombin are generated in response to vascular injury and platelets become activated1,2
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.
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
Indirect Factor Xa inhibitors
- 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
Direct Factor Xa inhibitors
- Rivaroxaban, apixaban and edoxaban directly engage the active site of the Factor Xa molecule3,4
- 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
| 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
- Perzborn E., Roehrig S., Straub A. et al. The discovery and development of rivaroxaban, an oral, direct Factor Xa inhibitor. Nat Rev Drug Discov 2011;10(1):61–75. Return to content
- Hoffman M, Monroe DM. Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am 2007;21:1–11. Return to content
- Turpie AGG. Oral, direct Factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases. Arterioscler Thromb Vasc Biol 2007;27:1238–1247. Return to content
- Weitz JI, Bates SM. New anticoagulants. J Thromb Haemost 2005;3:1843–1853. Return to content
- Bauer KA. Pros and cons of new oral anticoagulants. Hematology Am Soc Hematol Educ Program 2013;2013:464–470. Return to content
- King CS, Holley AB, Moores LK. Moving toward a more ideal anticoagulant: the oral direct thrombin and factor Xa inhibitors. Chest 2013;143:1106–1116. Return to content
- Bayer AG. Xarelto® (rivaroxaban) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000944/WC500057108.pdf [accessed 17 September 2018]. Bayer AG. Xarelto® (rivaroxaban) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000944/WC500057108.pdf [accessed 17 September 2018]. Return to content
- Eliquis® (apixaban). Summary of Product Characteristics. Eliquis® (apixaban). Summary of Product Characteristics. Return to content
- Daiichi Sankyo Europe GmbH. Lixiana® (edoxaban) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002629/WC500189045.pdf [accessed 22 August 2018]. Daiichi Sankyo Europe GmbH. Lixiana® (edoxaban) Summary of Product Characteristics. 2018. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002629/WC500189045.pdf [accessed 22 August 2018]. Return to content
See Also
Peripheral Artery Disease: causes and consequences
See Also
Coronary Artery Disease: causes and consequences
