Chemistry:Betrixaban

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Betrixaban (trade name Bevyxxa) is an oral anticoagulant drug which acts as a direct factor Xa inhibitor.[1] Betrixaban is FDA approved for venous thrombosis prevention in adults hospitalized for an acute illness who are at risk for thromboembolic complications.[2] Compared to other directly acting oral anticoagulants betrixaban has relatively low renal excretion and is not metabolized by CYP3A4.[3]

History

Betrixaban was originally developed by Millennium Pharmaceuticals. Portola Pharmaceuticals acquired rights for betrixaban in 2004 and co-developed it with Merck. In 2011 Merck discontinued joint development.[4]

The drug has undergone clinical trials for prevention of embolism after knee surgery[5] and for prevention of stroke following non-valvular atrial fibrillation.[6][7] Betrixaban was also studied in a large phase III clinical trial for extended duration thromboprophylaxis in acute ill patients.[8] Previously apixaban and rivaroxaban have failed to show positive risk/benefit ratio in this indication compared to enoxaparin.[9][10][non-primary source needed] APEX trial compared betrixaban with enoxaparin and included 7513 patients. Lower rate of VTE events was found in betrixaban arm with no increase in major bleedings compared to enoxaparin.[11] Based on these results betrixaban was approved by FDA on June 23, 2017, becoming the first DOAC approved for extended prophylaxis in hospitalized patients.[12]

Betrixaban has been also reviewed by EMA but didn't receive marketing approval in EU mainly due to concerns of increased bleeding risk and absence of reversal agent.[13]

See also

References

  1. ↑ "Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development". Clinical Pharmacokinetics 48 (1): 1–22. 2009. doi:10.2165/0003088-200948010-00001. PMID 19071881. 
  2. ↑ "Approved Drugs - FDA approved betrixaban (BEVYXXA, Portola) for the prophylaxis of venous thromboembolism (VTE) in adult patients" (in en). Center for Drug Evaluation and Research (CDER). U.S. Food and Drug Administration. https://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm564422.htm. 
  3. ↑ "Pharmacological properties of betrixaban". European Heart Journal Supplements 20 (Suppl E): E12–E15. May 2018. doi:10.1093/eurheartj/suy016. PMID 29977164. 
  4. ↑ "Merck Abandons Development of Factor Xa Inhibitor Betrixaban". CardioBrief. 24 March 2011. http://cardiobrief.org/2011/03/24/merck-abandons-development-of-factor-xa-inhibitor-betrixaban/. 
  5. ↑ "A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT)". Thrombosis and Haemostasis 101 (1): 68–76. January 2009. doi:10.1160/th08-07-0460. PMID 19132191. 
  6. ↑ "Oral factor Xa inhibitors for the prevention of stroke in atrial fibrillation". Current Opinion in Cardiology 25 (4): 312–320. July 2010. doi:10.1097/HCO.0b013e32833a524f. PMID 20520539. 
  7. ↑ "New anticoagulants for atrial fibrillation". Seminars in Thrombosis and Hemostasis 35 (5): 515–524. July 2009. doi:10.1055/s-0029-1234147. PMID 19739042. 
  8. ↑ "The design and rationale for the Acute Medically Ill Venous Thromboembolism Prevention with Extended Duration Betrixaban (APEX) study". American Heart Journal 167 (3): 335–341. March 2014. doi:10.1016/j.ahj.2013.11.006. PMID 24576517. 
  9. ↑ "Rivaroxaban for thromboprophylaxis in acutely ill medical patients" (in EN). The New England Journal of Medicine 368 (6): 513–523. February 2013. doi:10.1056/nejmoa1111096. PMID 23388003. 
  10. ↑ "Apixaban versus enoxaparin for thromboprophylaxis in medically ill patients" (in EN). The New England Journal of Medicine 365 (23): 2167–2177. December 2011. doi:10.1056/nejmoa1110899. PMID 22077144. 
  11. ↑ "Extended Thromboprophylaxis with Betrixaban in Acutely Ill Medical Patients" (in EN). The New England Journal of Medicine 375 (6): 534–544. August 2016. doi:10.1056/nejmoa1601747. PMID 27232649. 
  12. ↑ "FDA approved betrixaban (BEVYXXA, Portola) for the prophylaxis of venous thromboembolism (VTE) in adult patients". https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm564422.htm. 
  13. ↑ "Refusal of the marketing authorisation for Dexxience (betrixaban): Outcome of re-examination". Committee for Medicinal Products for Human Use (CHMP). European Medicines Agency. 27 July 2018. https://www.ema.europa.eu/documents/smop-initial/questions-answers-refusal-marketing-authorisation-dexxience-betrixaban_en.pdf. 



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