eTable. Pharmacokinetics and pharmacodynamics of the direct or non-vitamin-K-dependent oral anticoagulants currently on the market (data from [5] and summaries of product characteristics).
| Apixaban | Rivaroxaban | Edoxaban | Dabigatran | |
|---|---|---|---|---|
| Point of action | Factor Xa | Factor Xa | Factor Xa | Factor IIa (thrombin) |
| Prodrug | No | No | No | Yes |
| Time to Cmax (h) | 1–3 (4) | 2–4 | 1–2 | 2–3 |
| CYP metabolism | 15% | 32% | <4% | 0% |
| Bioavailability | (50% ?) 66% | 80% | 62% | 3–7% |
| Transport | P-gp | P-gp/BCRP | P-gp | P-gp |
| Protein binding | 87% | > 90% | 55% | 35% |
| Half-life (h) | 8–15 | (5–7 ?) 9–13 | 10–14 | (8?)12–14(15?) |
| Renal elimination | 27% | 33% (65%)* | 50% | 80% |
*Approximately half eliminated unchanged in the urine
BCRP. breast cancer resistant protein; Cmax. maximal concentration (peak level); CYP. cytochrome P450; P-gp. P-glycoprotein.
The question marks indicate uncertainty.