Table 1.
Pharmacological properties of non-vitamin K antagonist oral anticoagulants (NOACs).
| Dabigatran | Apixaban | Edoxaban | Rivaroxaban | |
|---|---|---|---|---|
| Target | Thrombin | Factor Xa | Factor Xa | Factor Xa |
| Bioavailability, % | 3–7% | 50% | 62% | 15 mg/20 mg: 66% without food, 80–100% with food |
| Plasma protein binding | 35% | 87% | 55% | 95% |
| Prodrug | Yes | No | No | No |
| Clearance non-renal/renal of absorbed dose | 20%/80% | 73%/27% | 50%/50% | 65%/35% |
| Dialysability | 50–60% (in part dialysable) | 14% (not dialysable) | NA (not dialysable) | NA (not dialysable) |
| Time to peak levels (h) | 3 | 3 | 2–4 | 2–4 |
| Elimination half-life (h) | 12–17 | 12 | 10–14 | 5–9 (young) 11–13 (elderly) |
| Metabolism | Glucuronic acid conjugation | CYP3A4 (25%), CYP1A2, CYP2J2, CYP2C8, CYP2C9, CYP2C19 |
CYP3A4 (<4% of elimination) | CYP2A4 (18%), CYP2J2 |
| Absorption with food | No effect | No effect | 6–22% more; minimal effect on exposure | +39% more |
| Absorption with H2B/PPI | −12% to 30% (not clinically relevant) | No effect | No effect | No effect |
| Drug interactions | Inhibitors and inducers of P-gp | Dual inhibitors and inducers of CYP3A4 and P-gp | Inhibitors and inducers of P-gp | Dual inhibitors and inducers of CYP3A4 and P-gp |