Table 1.
Plasma pharmacokinetics of oral tedizolid phosphatea
| Data sourceb | Cmax (μg/ml) | Tmax (h) | Total drug AUC (μg · h/ml) | VSS/F (liters) | CL/F (liters/h) | t1/2 (h) |
|---|---|---|---|---|---|---|
| BAL study (day 3) | 2.4 (0.4) | 2 (0.5–4) | 25.1 (5.8) | 108 (21) | 8.4 (2.2) | 9.2 (2.0) |
| Bien (single dose) (1) | 2.0 (0.4) | 3 (1–4) | 25.4 (4.6) | 128 (31)c | 8.1 (1.5) | 11.2 (3.6) |
| Prokocimer (multiple dose, day 1) (23) | 1.8 (1.2) | 3 (1.5–4) | 21.6 (6.5) | 155 (29)c | 10.0 (2.8) | 11.1 (1.2) |
| Prokocimer (multiple dose, steady state) (23) | 1.8 (0.4) | 3 (2–4) | 22.5 (6.5) | 143 (51)c | 9.5 (2.7) | 10.2 (2.0) |
a
Data are means (SD) except Tmax, which are means (range). Cmax, maximum drug concentration; Tmax, time to Cmax; AUC, area under the curve from time zero to infinity (for single dose) or for the 0- to 24-h dosing interval (for multiple doses); VSS/F, volume of distribution at steady-state; CL/F, total body clearance; t1/2, elimination half-life.
b
Drug for the BAL was 200 mg tedizolid phosphate (containing 164 mg of the active compound, tedizolid); drug for the other studies was 200 mg tedizolid phosphate disodium (containing 150 mg of tedizolid).
c
VZ/F (volume of distribution).