Table 1.
Factor-Xa inhibitor’s pharmacokinetic and pharmacodynamic characteristics
| Rivaroxaban | Apixaban | Edoxaban | |
|---|---|---|---|
| VTE dose | 15 mg BID ×3 weeks, then 20 mg once daily | 10 mg BID ×7 days, then 5 mg BID | 60 mg QD after 7–10 days heparin |
| Renal dose adjustment | Yes, CrCl <30 mL/min | Yes, CrCl <25 mL/min or Scr >2.5 | Assumed 50% reduction if CrCl <50 mL/min |
| Tmax (h) | 2–4 | 3–4 | 1–2 |
| VD (L) | 50 | ~23* | >300 |
| Half-life (h) | 5–9 | 9–14 | 10–14 |
| Bioavailability | >80% | >50% | 62% |
| Protein binding | 92%–95% | 87% | 40%–59% |
| Metabolism | CYP3A4, CYP2J2 | CYP3A4 | CYP3A4 |
| Elimination | 33% renal | 25% renal | 35% renal |
| Effects of food | Cmax and AUC increased; take with food | Cmax and AUC unchanged | Cmax and AUC unchanged |
| CYP3A4 substrate | Yes | Yes | Yes |
| P-gp substrate | Yes | Yes | Yes |
Notes:
*
VD =0.3 L/kg and assuming a 75 kg patient. The HOKUSAI-VTE trial20 reduced dose by 50% in those patients with a CrCl of 30 to 50 mL/min, or a body weight ≤60kg, or in patients receiving concomitant treatment with potent P-gp inhibitor.
Abbreviations: AUC, area under the curve; BID, twice daily; Cmax, maximum peak concentration; CrCl, creatinine clearance; CYP, cytochrome P450; h, hours; min, minutes; P-gp, P-glycoprotein; QD, every day; Scr, serum creatine; Tmax, time to maximum concentration; VD, volume of distribution; VTE, venous thromboembolism.