Skip to main content

Advertisement

Table 1 Pharmacokinetic properties of direct oral anticoagulants[2025]

From: Pharmacokinetic and pharmacodynamic evaluation of rivaroxaban: considerations for the treatment of venous thromboembolism

  Rivaroxaban Apixaban Edoxaban Dabigatran
Mechanism of action Direct Factor Xa inhibitor Direct Factor Xa inhibitor Direct Factor Xa inhibitor Direct thrombin inhibitor
Prodrug No No No Dabigatran etexilate
Oral bioavailability (%) 80–100 ~66 ~50 6.5
Fraction unbound in plasma (%) ~5–10 13 ~41–60 ~65–70
tmax (h) 2.0–4.0 1.0–3.0 1.0–2.0 1.25–3.0
t½ (h) 5–13 8–15 6–11 12–14
Elimination 36% unchanged via active renal secretion; 30% renal excretion of inactive metabolites; 34% hepatobiliary (7% unchanged) ~25% renal; ~75% hepatobiliary ~35–39% renal; ~61–65% hepatobiliary 80% renal; 20% hepatobiliary
Metabolism CYP3A4, CYP2J2 and CYP-independent mechanisms; P-gp substrate CYP3A4; P-gp substrate CYP3A4; P-gp substrate P-gp substrate
  1. CYP, cytochrome P450; P-gp, P-glycoprotein; t½, half-life; tmax, time to maximum concentration.