TABLE 2.
PK parameters after single ascending i.v. doses of eravacycline
| Parametera | Values after the following dosesb: |
||||||
|---|---|---|---|---|---|---|---|
| 0.1 mg/kg | 0.25 mg/kg | 0.5 mg/kg | 1 mg/kg | 1.5 mg/kg | 2 mg/kg | 3 mg/kg | |
| AUC0–t (ng · h/ml) | 428.0 (21.2) | 1,153.9 (16.5) | 2,502.9 (25.9) | 5,297.9 (22.2) | 8,495.6 (17.3) | 11,972.1 (14.3) | 22,443.5 (20.7) |
| AUC0–inf (ng · h/ml) | 554.2 (23.2) | 1,309.1 (16.2) | 2,678.7 (25.6) | 5,511.1 (21.3) | 8,856.8 (18.3) | 12,347.5 (15.4) | 23,145 (20.7) |
| Cmax (ng/ml) | 227.0 (24.5) | 466.5 (22.7) | 993.5 (17.5) | 1,888.3 (27.8) | 3,233.3 (22.6) | 4,916.7 (17.0) | 9,793.3 (16.4) |
| Tmax (h) | 0.5 (0.5–0.6) | 0.5 (0.3–0.6) | 0.5 (0.5–0.6) | 0.5 (0.5–0.7) | 0.5 (0.5–0.5) | 0.5 (0.5–0.5) | 0.5 (0.5–0.6) |
| t1/2 (h) | 12.7 (23.9) | 16.5 (13.3) | 19.6 (28.0) | 20.2 (28.0) | 22.7 (18.0) | 22.3 (12.4) | 25.6 (9.7) |
| CL (liter/h/kg) | 0.19 (21.3) | 0.20 (17.1) | 0.20 (24.6) | 0.19 (19.8) | 0.17 (19.1) | 0.17 (14.9) | 0.14 (24.5) |
| Vss (liters/kg) | 2.5 (14.8) | 3.3 (11.6) | 3.6 (13.5) | 3.4 (20.4) | 3.5 (15.4) | 3.1 (9.4) | 2.3 (26.4) |
a
AUC0–t, area under the plasma concentration-time curve from 0 h to time t; AUC0–inf, area under the plasma concentration-time curve from 0 h to infinity; Cmax, maximum plasma concentration; Tmax, time to maximum plasma concentration; t1/2, terminal elimination half-life; CL, clearance; Vss, volume of distribution at steady state.
b
Values represent the mean (coefficient of variation [in percent]) for all parameters except Tmax, for which the values are the median (range).