TABLE 3.
PK parameters after multiple ascending i.v. doses of eravacycline on day 1 and day 10
| Day and parametera | Values after the following regimensb: |
|||
|---|---|---|---|---|
| 0.5 mg/kg over 30 min q24h | 1.5 mg/kg over 30 min q24h | 1.5 mg/kg over 60 min q24h | 1.0 mg/kg over 60 min q12h | |
| Day 1 | ||||
| AUC0–24 (ng · h/ml) | 2,096 (20.9) | 6,003 (8.8) | 7,171 (15.3) | |
| AUC0–12 (ng · h/ml) | 4,305 (13.8) | |||
| AUCinf (ng · h/ml) | 2,639 (28.5) | 7,015 (10.7) | 8,385 (15.9) | 5,630 (16.1) |
| Cmax (ng/ml) | 1,078 (18.0) | 3,447 (7.1) | 2,785 (22.0) | 2,125 (15.3) |
| Tmax (h) | 0.5 (0.5–0.5) | 0.5 (0.5–0.5) | 1.0 (1.0–1.0) | 1.0 (1.0–1.0) |
| t1/2 (h) | 12.7 (22.6) | 11.0 (11.9) | 11.4 (23.4) | 8.6 (20.5) |
| Day 10 | ||||
| AUC0–24 (ng · h/ml) | 2,902 (30.4) | 8,051 (19.1) | 7,592 (11.8) | |
| AUC0–12 (ng · h/ml) | 6,309 (15.0) | |||
| Cmax (ng/ml) | 931 (16.6) | 3,403 (9.3) | 1,892 (10.3) | 1,825 (15.5) |
| Tmax (h) | 0.5 (0.5–0.5) | 0.5 (0.5–0.5) | 1.0 (0.5–1.0) | 1.0 (1.0–1.0) |
| t1/2 (h) | 35.8 (48.5) | 29.1 (14.0) | 30.2 (17.0) | 38.7 (32.4) |
| CL (liter/h/kg) | 0.19 (31.6) | 0.19 (18.2) | 0.20 (12.8) | 0.16 (17.0) |
| Vss (liter/kg) | 5.0 (20.2) | 4.0 (18.1) | 4.7 (7.7) | 4.0 (15.0) |
a
AUC0–24, area under the plasma concentration-time curve from 0 h to 24 h; AUC0–12, area under the plasma concentration-time curve from 0 h to 12 h; AUCinf, area under the plasma concentration-time curve at 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. AUC0–24 was used for the 24-h regimens, and AUC0–12 was used for the 12-h regimen.
b
Values represent the mean (coefficient of variation [in percent]) for all parameters except Tmax, for which the values are the median (range).