Factor Xa inhibitors in clinical practice: Comparison of pharmacokinetic profiles

The anticoagulant actions of oral direct factor Xa (FXa) inhibitors can be inferred from their observed plasma concentrations; however, the steady-state pharmacokinetics (PK) of different FXa inhibitors have not been compared in clinically. The sensitivity of the rivaroxaban, apixaban, and edoxaban...

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Bibliographic Details
Published in:Drug metabolism and pharmacokinetics 2020-02, Vol.35 (1), p.151-159
Main Authors: Goto, Eri, Horinaka, Shigeo, Ishimitsu, Toshihiko, Kato, Toru
Format: Article
Language:English
Subjects:
anti-FXa activity
Apixaban
Atrial fibrillation
Edoxaban
Plasma concentration
Population pharmacokinetics
Rivaroxaban
Venous thromboembolism
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Summary:The anticoagulant actions of oral direct factor Xa (FXa) inhibitors can be inferred from their observed plasma concentrations; however, the steady-state pharmacokinetics (PK) of different FXa inhibitors have not been compared in clinically. The sensitivity of the rivaroxaban, apixaban, and edoxaban in the STA-Liquid Anti-FXa assay were compared, and the anti-FXa plasma concentrations were measured for PK assessments. Nonlinear mixed-effects modeling was used to assess population PK in 329 patients with nonvalvular atrial fibrillation or venous thromboembolism. Patients were followed up for an average of 3.6 years. Sensitivity was similar among the three drugs in this assay, which could directly compare plasma concentrations instead of anti-FXa activities. Overall exposure was greatest in 5 mg BID apixaban relative to other drugs (p 
ISSN:1347-4367
1880-0920
DOI:10.1016/j.dmpk.2019.10.005