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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
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 |
Approved indications in Europe (unless otherwise stated) of the direct Factor Xa inhibitors in adults7-10
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
- Hoffman M, Monroe DM. Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am 2007;21:1–11. Return to content
- 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;10:61–75. 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. 2020. Available at: https://www.ema.europa.eu/documents/product-information/xarelto-epar-product-information_en.pdf [accessed 30 July 2020]. Bayer AG. Xarelto® (rivaroxaban) Summary of Product Characteristics. 2020. Available at: https://www.ema.europa.eu/documents/product-information/xarelto-epar-product-information_en.pdf [accessed 30 July 2020]. Return to content
- Bristol Myers Squibb, Pfizer Inc. Eliquis® (apixaban) Summary of Product Characteristics. 2020. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002148/WC500107728.pdf [accessed 30 July 2020]. Bristol Myers Squibb, Pfizer Inc. Eliquis® (apixaban) Summary of Product Characteristics. 2020. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002148/WC500107728.pdf [accessed 30 July 2020]. Return to content
- Daiichi Sankyo Europe GmbH. Lixiana® (edoxaban) Summary of Product Characteristics. 2020. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002629/WC500189045.pdf [accessed 8 September 2020]. Daiichi Sankyo Europe GmbH. Lixiana® (edoxaban) Summary of Product Characteristics. 2020. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002629/WC500189045.pdf [accessed 8 September 2020]. Return to content
- Daiichi Sankyo Co Ltd. Lixiana OD tablets 15 mg, OD tablets 30 mg, OD tablets 60 mg. 2020. Available at: https://www.medicallibrary-dsc.info/di/lixiana_od/?product=lixiana_od_tablets_30mg [accessed 6 November 2020]. Daiichi Sankyo Co Ltd. Lixiana OD tablets 15 mg, OD tablets 30 mg, OD tablets 60 mg. 2020. Available at: https://www.medicallibrary-dsc.info/di/lixiana_od/?product=lixiana_od_tablets_30mg [accessed 6 November 2020]. Return to content
See Also
Peripheral Artery Disease: causes and consequences
See Also
Coronary Artery Disease: causes and consequences
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Updated date 26/01/2021
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