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. 2021 May 21;38(6):2891–2907. doi: 10.1007/s12325-021-01769-9

Table 1.

Pharmacokinetic characteristics of direct oral anticoagulants

Drug Dabigatran Rivaroxaban Apixaban Edoxaban
Target Thrombin FXa FXa FXa
Bioavailability (%) 6.5 80 50 60
Prodrug Yes No No No
Active metabolites No No No Yes
Vd (L) 60–70 50 21 > 300
Plasma protein binding (%) 35 > 90 87 40–59
Cmax (h) 1–3 2–4 3–4 2
Elimination half-life (h) 12–17 5–9 8–15 8–11
Metabolism (CYP) No 3A4, 2J2 3A4 (25% elimination) 3A4 (< 4% elimination)
P-gp substrate Yes Yes Yes Yes
Other transporters Not known BCRP/ABCG2 BCRP/ABCG2 No
Renal elimination (%) 80 65 27 35
Renal clearance (mL/min) 80 58 15 183
Posology BID OD BID OD
Expected range of plasma levels at peak for std. dose (ng/mL) 64–443 184–343 69–321 91–321
Expected range of plasma levels at trough for std. dose (ng/mL) 31–225 12–137 34–230 31–230