Table 2.
Pharmacokinetic parameters of edoxaban and its metabolites
| Parameter | Edoxaban | M4 | M6 | |||
|---|---|---|---|---|---|---|
| Edoxaban alone, N = 34 | Edoxaban with rifampin, N = 32 | Edoxaban alone, N = 34 | Edoxaban with rifampin, N = 32 | Edoxaban alone, N = 34 | Edoxaban with rifampin, N = 32 | |
| C max, ng/mL | 243 ± 100 | 257 ± 61.8 | 23.1 ± 13.2 | 108 ± 33.0 | 8.55 ± 4.10 | 44.5 ± 12.3 |
| t max, h | 1.08 (0.50–4.00) | 1.00 (0.50–3.00) | 1.81 (1.00–3.05) | 2.00 (1.00–3.00) | 1.49 (0.983–3.00) | 1.00 (0.617–3.00) |
| AUC∞, ng·h/mL | 1835 ± 442 | 1192 ± 214 | 161 ± 69.8 | 449 ± 140 | 91.1 ± 28.2 | 261 ± 57.4 |
| t ½, h | 13.6 ± 6.06 | 6.54 ± 4.24 | 14.3 ± 6.0 | 4.23 ± 3.78 | 14.3 ± 5.58 | 10.0 ± 3.81 |
| CL/F, L/h | 34.8 ± 9.22 | 52.0 ± 9.76 | NC | NC | NC | NC |
| Metabolite to parent exposure ratio (%) | 8.89 ± 3.22 | 38.1 ± 11.8 | 5.09 ± 1.44 | 22.2 ± 4.35 | ||
Data are presented as arithmetic mean ± standard deviation, except for t max values, which are presented as median (range)
AUC ∞ area under the plasma concentration–time curve from time zero extrapolated to infinity, CL/F apparent total body clearance, C max maximum plasma concentration, NC not calculated, t ½ apparent terminal half-life, t max time to C max