andexanet
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Indications
- antidote to factor-Xa inhibitors apixaban, edoxaban, & rivaroxaban
- decreases hematoma expansion in factor-Xa inhibitor-associated intracerebral hemorrhage[5]*
* thrombotic events including ischemic stroke were increased,
- 30-day functional outcomes were unchanged[5]
Dosage
Pharmacokinetics
- >90% decline in anti-Xa activity of either apixaban or rivaroxaban within 2-5 minutes after 400 mg IV of andexanet
at 12 hours after infusion, 82% of patients with good or excellent hemostasis[4]
Adverse effects
- infusion-associated urticaria
- thrombosis within 39 days 10%[4]
Mechanism of action
- recombinant modified human factor Xa decoy protein
- reverses inhibition of factor Xa by factor Xa inhibitors[2]
More general terms
References
- ↑ Siegal DM, Curnutte JT, Connolly SJ et al. Andexanet alfa for the reversal of factor Xa inhibitor activity. N Engl J Med 2015 Nov 11 PMID: https://www.ncbi.nlm.nih.gov/pubmed/26559317 Free full text
Connors JM. Antidote for factor Xa anticoagulants. N Engl J Med 2015 Nov 11 PMID: https://www.ncbi.nlm.nih.gov/pubmed/26559124 Free full text - ↑ 2.0 2.1 Connolly SJ, Milling TJ, Eikelboom JW et al. Andexanet alfa for acute major bleeding associated with factor Xa inhibitors. N Engl J Med 2016 Aug 30 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27573206 <Internet> http://www.nejm.org/doi/10.1056/NEJMoa1607887
- ↑ Susman E Novel Drug Reverses Anticoagulation in Emergencies. Andexanet stops 90% of action of factor Xa inhibitors. MedPage Today. March 13, 2018 https://www.medpagetoday.com/meetingcoverage/acc/71736
Connolly S, et al Report on the ANNEXA-4 study: Andexanet for reversal of anticoagulation in factor Xa-associated acute major bleeding. American College of Cardiology (ACC) 2018; Abstract 409-14 - ↑ 4.0 4.1 4.2 Connolly SJ, Crowther M, Eikelboom JW et al Full Study Report of Andexanet Alfa for Bleeding Associated with Factor Xa Inhibitors. N Engl J Med. Feb 7, 2019 PMID: https://www.ncbi.nlm.nih.gov/pubmed/30730782 https://www.nejm.org/doi/full/10.1056/NEJMoa1814051
- ↑ 5.0 5.1 5.2 Connolly SJ et al. Andexanet for factor Xa inhibitor-associated acute intracerebral hemorrhage. N Engl J Med 2024 May 16/23; 390:1745 https://www.nejm.org/doi/10.1056/NEJMoa2313040
Smith WS, Hemphill JC. Reversing oral anticoagulation in intracerebral hemorrhage. N Engl J Med 2024 May 16/23; 390:1815 https://www.nejm.org/doi/10.1056/NEJMe2403726