|Systematic (IUPAC) name|
|Legal status||POM (UK)|
|Excretion||75% biliary, 25% renally|
|Mol. mass||459.497 g/mol|
|(what is this?)|
Apixaban (BMS-562247-01, tradename Eliquis) is an anticoagulant for the treatment of venous thromboembolic events. It is a direct factor Xa inhibitor. Apixaban has been available in Europe since May 2012. In the United States, it is undergoing phase III trials for the prevention of venous thromboembolism. An FDA decision on apixaban which was expected on June 28, 2012 was delayed. It is being developed in a joint venture by Pfizer and Bristol-Myers Squibb.
A 2007 trial showed that apixaban was equivalent to enoxaparin/open-label heparin in preventing thrombosis in patients who had undergone a knee replacement. A 2010 trial showed that apixaban was superior to enoxaparin in preventing thrombosis in patients undergoing elective hip replacement surgery, with similar bleeding rates.
A 2011 trial showed that in patients with atrial fibrillation who have failed or are not candidates for vitamin K antagonist therapy, apixaban, as compared with aspirin, reduced the risk of stroke or systemic embolism in patients experiencing atrial fibrillation by more than 50% (from 3.7% per year with aspirin to 1.6% per year with Apixaban). Difference in death rates did not reach statistical significance. A 2011 trial showed that patients receiving apixaban after acute coronary syndrome experienced an increased rate of major bleeding episodes without a significant reduction in recurrent ischemic events. For this reason, the trial was terminated early.
In a head-to-head study of apixaban versus warfarin, apixaban met both its primary endpoint (“noninferiority” to warfarin in preventing strokes) and a key secondary endpoint (superior compared to warfarin in avoiding major bleeding).
- "ELIQUIS® (apixaban) Approved In Europe For Preventing Venous Thromboembolism After Elective Hip Or Knee Replacement" (Press release). Pfizer. April 20, 2012. Retrieved 2012-05-29.
- Turpie AG (June 2007). "Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases". Arterioscler. Thromb. Vasc. Biol. 27 (6): 1238–47. doi:10.1161/ATVBAHA.107.139402. PMID 17379841.
- Huston, Larry (February 29, 2012). "Decision on Apixaban (Eliquis) Pushed Back By Three Months". Forbes. Retrieved 2012-05-29.
- Husten, Larry. "FDA Once Again Delays Approval Of Apixaban (Eliquis)". Forbes. Retrieved 17 July 2012.
- "Bristol-Myers Squibb News Release 26 April 2007". Archived from the original on 11 September 2007. Retrieved 2007-09-15.
- Nainggolan, Lisa. "Apixaban better than European enoxaparin regimen for preventing VTE". Retrieved 2011-04-01.
- Lassen MR, Davidson BL, Gallus A, Pineo G, Ansell J, Deitchman D (2007). "The efficacy and safety of apixaban, an oral, direct factor Xa inhibitor, as thromboprophylaxis in patients following total knee replacement". J. Thromb. Haemost. 5 (12): 2368–75. doi:10.1111/j.1538-7836.2007.02764.x. PMID 17868430.
- Lassen MR, Gallus A, Raskob GE, Pineo G, Chen D, Ramirez LM, ADVANCE-3 Investigators (December 2010). "Apixaban versus enoxaparin for thromboprophylaxis after hip replacement". N. Engl. J. Med. 363 (26): 2487–98. doi:10.1056/NEJMoa1006885. PMID 21175312.
- Nainggolan L. "Apixaban better than European enoxaparin regimen for preventing VTE". theheart.org by WebMD. Retrieved 2011-04-01.
- "Apixaban in patients with atrial fibrillation". N. Engl. J. Med. 364 (9): 806–817. March 2011. doi:10.1056/NEJMoa1007432. PMID 21309657.
- Alexander JH, Lopes RD, James S, et al. (August 2011). "Apixaban with antiplatelet therapy after acute coronary syndrome". N. Engl. J. Med. 365 (8): 699–708. doi:10.1056/NEJMoa1105819. PMID 21780946.
- "Apixaban for the Prevention of Stroke in Subjects With Atrial Fibrillation (ARISTOTLE)". NCT00412984. ClinicalTrials.gov. Retrieved 2011-06-23.
- Granger CB, Alexander JH, McMurray JJV, et al. (August 2011). "Apixaban versus Warfarin in Patients with Atrial Fibrillation". New England Journal of Medicine 365. doi:10.1056/NEJMoa1107039.
- Husten L (2011-06-22). "ELIQUIS® (apixaban) Meets Primary and Key Secondary Endpoints in Phase 3 ARISTOTLE Study". CardioBrief. WordPress.com. Retrieved 2011-06-23.