Apixaban


Description

Apixaban is an oral, direct, and highly selective factor Xa (FXa) inhibitor of both free and bound FXa, as well as prothrombinase, independent of antithrombin III for the prevention and treatment of thromboembolic diseases[Label,

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Pharmacology

Indication

Apixaban is indicated for reducing the risk of stroke and systemic embolism in patients who have non... Read more

Pharmacodynamic

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III... Read more

Mechanism of action

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III... Read more

Absorption

Apixaban is approximately 50% bioavailable[Label] though other studies report 43-46% oral bioavailab... Read more

Protein binding

92-94%[Label].

Volume of distribution

Approximately 21L[Label].

Clearance

3.3L/h[Label] though other studies report 4876mL/h[ Read more

Half life

12.7±8.55h[Label, Read more

Route of elimination

56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered... Read more

Toxicity

Animal studies have shown an increased risk of maternal bleeding during pregnancy but no increase in... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
All bleeding event US
  • Kind: experimental
    • Percent: 11-15%
  • Kind: placebo
    • Percent: 9%
  • Kind: comparator
    • Percent: 25%
  • Clinical Trial
    All bleeding event US
  • Kind: experimental
    • Percent: 11-15%
  • Kind: placebo
    • Percent: 9%
  • Kind: comparator
    • Percent: 25%
  • Clinical Trial
    Minor bleeding event US
  • Kind: experimental
    • Percent: 9-12%
  • Kind: placebo
    • Percent: 7%
  • Kind: comparator
    • Percent: 19%
  • Clinical Trial
    Minor bleeding event US
  • Kind: experimental
    • Percent: 9-12%
  • Kind: placebo
    • Percent: 7%
  • Kind: comparator
    • Percent: 19%
  • Clinical Trial
    Any bleeding event US
  • Kind: experimental
    • Percent: 5-12%
  • Kind: comparator
    • Percent: 7-13%
  • Clinical Trial
    Any bleeding event US
  • Kind: experimental
    • Percent: 5-12%
  • Kind: comparator
    • Percent: 7-13%
  • Clinical Trial
    Major and clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 3%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Major and clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 3%
  • Kind: comparator
    • Percent: 10%
  • Clinical Trial
    Clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 8%
  • Clinical Trial
    Clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 8%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Major or clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-5%
  • Kind: comparator
    • Percent: 4-5%
  • Clinical Trial
    Major or clinically relevant nonmajor bleeding event US
  • Kind: experimental
    • Percent: 3-5%
  • Kind: comparator
    • Percent: 4-5%
  • Clinical Trial
    Contusion US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Hematuria US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Hematuria US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Contusion US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Major bleeding event US
  • Kind: experimental
    • Percent: 2.13
  • Kind: comparator
    • Percent: 3.09
  • Clinical Trial
    Hematoma US
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Hematoma US
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Anemia US
  • Kind: experimental
    • Percent: 3%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Anemia US
  • Kind: experimental
    • Percent: 3%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Major bleeding event US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Major bleeding event US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Contusion US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Contusion US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Operative Hemorrhage US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Operative Hemorrhage US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Wound secretion US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Wound secretion US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Incision-site hemorrhage US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Incision-site hemorrhage US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Incision-site hematoma US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Incision-site hematoma US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Hemoptysis US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Hemoptysis US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Menorrhagia US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Menorrhagia US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Decreases in hemoglobin US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 0-1%
  • Clinical Trial
    Bleeding at critical site US
  • Kind: experimental
    • Percent: <1%
  • Kind: comparator
    • Percent: <1%
  • Clinical Trial
    Bleeding at critical site US
  • Kind: experimental
    • Percent: <1%
  • Kind: comparator
    • Percent: <1%
  • Clinical Trial
    Hemorrhage US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Hemorrhage US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Postprocedural hemorrhage US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Aspartate aminotransferase increased US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Aspartate aminotransferase increased US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Postprocedural hemorrhage US
  • Kind: experimental
    • Percent: 1%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Hypersensitivity:
      • True
    • Sex Group: all
    • Regions: US
    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Regions: US
    • Patient Conditions:
        • Name: Active pathological bleeding
        • Drugbank Id: DBCOND0107496

    Food Interactions

    • Alfalfa, Anise, Bilberry may increase the adverse effects of apixaban.
    • Grapefruit juice may increase apixaban serum concentration.
    • St. John's wort will likely decrease apixaban serum concentration. Avoid combination if possible.

    Interactions

    Type in a drug name to check for interaction with Apixaban

    The therapeutic efficacy of Apixaban can be increased when used in combination with (1,2,6,7-3H)Testosterone.
    Apixaban may increase the anticoagulant activities of (R)-warfarin.
    Apixaban may increase the anticoagulant activities of (S)-Warfarin.
    The therapeutic efficacy of Apixaban can be increased when used in combination with 1-Testosterone.
    The therapeutic efficacy of Apixaban can be increased when used in combination with 18-methyl-19-nortestosterone.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Apixaban.
    3,5-Diiodotyrosine may increase the anticoagulant activities of Apixaban.
    Apixaban may increase the anticoagulant activities of 4-hydroxycoumarin.
    The therapeutic efficacy of Apixaban can be increased when used in combination with 4-Hydroxytestosterone.
    The metabolism of Apixaban can be decreased when combined with 5-androstenedione.
    The therapeutic efficacy of Apixaban can be increased when used in combination with 5beta-dihydrotestosterone.
    The metabolism of Apixaban can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Apixaban.
    The metabolism of Apixaban can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Apixaban.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Apixaban.
    The metabolism of Apixaban can be increased when combined with Abatacept.
    Apixaban may increase the anticoagulant activities of Abciximab.
    The serum concentration of Apixaban can be increased when it is combined with Abemaciclib.
    The metabolism of Apixaban can be decreased when combined with Abiraterone.

    References

    • 1 . Raghavan N, Frost CE, Yu Z, He K, Zhang H, Humphreys WG, Pinto D, Chen S, Bonacorsi S, Wong PC, Zhang D: Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009 Jan;37(1):74-81. doi: 10.1124/dmd.108.023143. Epub 2008 Oct 2. [PubMed: 18832478]
    • 2 . Granger CB, Alexander JH, McMurray JJ, Lopes RD, Hylek EM, Hanna M, Al-Khalidi HR, Ansell J, Atar D, Avezum A, Bahit MC, Diaz R, Easton JD, Ezekowitz JA, Flaker G, Garcia D, Geraldes M, Gersh BJ, Golitsyn S, Goto S, Hermosillo AG, Hohnloser SH, Horowitz J, Mohan P, Jansky P, Lewis BS, Lopez-Sendon JL, Pais P, Parkhomenko A, Verheugt FW, Zhu J, Wallentin L: Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011 Sep 15;365(11):981-92. doi: 10.1056/NEJMoa1107039. Epub 2011 Aug 27. [PubMed: 21870978]
    • 3 . FDA Drug Approval Package: Apixaban [Link]

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