Update on Edoxaban for the Prevention and Treatment of Thromboembolism: Clinical Applications Based on Current Evidence
Table 1
Edoxaban pharmacodynamics and pharmacokinetics [16–21].
Drug/mechanism of action
Edoxaban/direct oral factor Xa inhibitor (FXa-I) without antithrombin III
Indication and dosing guidelines
(1) Treatment of nonvalvular atrial fibrillation (NVAF) (i) 60 mg orally daily for CrCl greater than 50 to less than or equal to 95 mL/min (ii) 30 mg orally daily for CrCl 15–50 mL/min (iii) Do not use if CrCl is greater than 95 mL/min (Black Box Warning) (2) Treatment of venous thromboembolism (VTE) (i) 60 mg orally daily (ii) 30 mg orally daily if CrCl is 15–50 mL/min or body weight is less than 60 Kg or patient is on P-gp inhibitor
Protein binding/removed by dialysis
55%/No
(%)
62% absorption in gastrointestinal tract Food does not affect the systemic exposure No data available for administration via feeding tube
(h)
1-2
Vd (L)
19.9
(h)
10–14 with steady state reached in 72 hours
Metabolism
Minimal hepatic, undergoes biotransformation to various metabolites, the most abundant of which [M4] is formed through hydrolysis
Effect of P-gp/ABCG2 on metabolism
Minimal
Renal excretion (%)
50%
Biliary-intestinal excretion (%)
50%
Pregnancy category
C
Bioavailability, ; creatinine clearance, cytochrome P450 3A4 (CYP3A4/5), CrCl; half-life, ; P-glycoprotein/ABCG2, P-gp/ABCG2; volume of distribution, Vd, time to reach maximum concentration in hours (h), .
