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Rivaroxaban
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| Systematic (IUPAC) name | |
| 5-chloro-N-[[2-oxo-3-[4-(3-oxomorpholin-4-yl) phenyl]oxazolidin-5-yl]methyl] thiophene-2-carboxamide |
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| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C19H18ClN3O5S |
| Mol. mass | 435.882 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 5.7-9.2 |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
?? |
| Legal status |
?? |
| Routes | oral |
Rivaroxaban (BAY 59-7939) is an oral anticoagulant under development by Bayer; it will be marketed as Xarelto. It acts by inhibiting the active form of coagulation factor X (factor Xa).
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Development
Rivaroxaban is an oxazolidinone derivative optimised for binding with factor Xa.[1] If marketed, it will be a joint product by Bayer and Ortho-McNeil Pharmaceutical.[2]
Uses
Expected
Due to the decreased need for monitoring, rivaroxaban is likely to be used to replace warfarin for a number of indications, such as atrial fibrillation.[3]
Trial results
In phase IIb trials it was effective in reducing thromboembolic complications (deep vein thrombosis and pulmonary embolism) after orthopedic surgery[4] and it is under investigation for the prevention of DVT and PE and for anticoagulation in atrial fibrillation.[3] Advantages are the oral administration (a benefit over low molecular weight heparins, which require subcutaneous injections) and no need for monitoring (an advantage over warfarin). In studies, dosages of 2.5-10 mg once or twice daily were used.[4]
Bayer-sponsored phase 3 clinical trials showed that once-daily rivaroxaban achieved superior efficacy and similar safety in the prevention of venous thromboembolism (VTE) in patients undergoing knee replacement or hip arthroplasty surgery in comparison with enoxaparin, a LMWH.[5][6]
Related drugs
Ximelagatran, a direct thrombin inhibitor, was not marketed further due to its potential side-effects; the related compound dabigatran was recently approved in the European Union. Together with rivaroxaban, the related factor Xa-inhibitor apixaban (Bristol-Myers-Squibb) and LY517717 (Lilly) are under development as non-monitored antithrombotic drugs.[7]
References
- ^ Roehrig S, Straub A, Pohlmann J, et al (2005). "Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor". J. Med. Chem. 48 (19): 5900–8. doi:. PMID 16161994.
- ^ Pharmabiz.com. "Bayer, Ortho-McNeil to co-develop key thrombosis drug". Retrieved on 2007-12-03.
- ^ a b Clinical trial NCT00403767
- ^ a b Eriksson BI, Borris L, Dahl OE, et al (2006). "Oral, direct Factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement". J. Thromb. Haemost. 4 (1): 121–8. doi:. PMID 16409461.
- ^ Eriksson BI, Borris LC, Friedman RJ et al (2008). "Rivaroxaban versus enoxaparin for thromboprophylaxis after hip arthroplasty". N. Engl. J. Med. 358: 2765–75. doi:.
- ^ Lassen MR, Ageno W, Borris LC et al (2008). "Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty". N. Engl. J. Med. 358: 2776–2786. doi:.
- ^ Hampton T (2006). "New oral anticoagulants show promise.". JAMA 295 (7): 743–4. doi:. PMID 16478891.
External links
- Xarelto.com (presently redirects to Bayer's main page)
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Wikipedia content modification information:
- This page was last modified on 12 August 2008, at 20:45.
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