Table 3.
Main PK and PK/PD characteristics, by dosing group, including protein-binding-adjusted (PBA) parameters. -: not applicable.
| Intensive PK Study | |||||
|---|---|---|---|---|---|
| Variable | Overall | Group 0 | Group 1 | Group 2 | Group 3 |
| Cmax I dose (mg/L) | 342.8 [290.5–424.0] |
419.6 [306.8–477.0] |
347.0 [292.4–479.2] |
323.3 [305.8–385.4] |
383.8 [335.5–383.8] |
| Cmax II dose (mg/L) | 379.5 [321.3–448.8] |
420.6 [380.6–469.8] |
337.0 [290.7–424.0] |
432.440 [372.2–432.4] |
|
| AUC0–1w (mg/L·h) | - | 26,693 [20,842–28,630] |
25,623 [23,335–28,347] |
23,924 [20,685–26,501] |
28,489 [25,573–28,489] |
| AUC0–2w (mg/L·h) | - | 34,168 [25,336–37,301] |
- | 31,686 [26,281–33,914] |
35,912 [32,891–35,912] |
| AUC0–3w (mg/L·h) | - | 39,270 [28,876–43,971] |
- |
- | 39,985 [37,045–39,985] |
| Cumul. AUC0–4w (mg/L·h) | - | 41,681 [32,055–48,180] |
79,486 [71,849–95,210] |
62,432 [55,860–74,010] |
68,835 [66,005–68,835] |
| PBA AUC0–1w/MIC | - | 14,946 [11,670–16,030] |
14,341 [13,065–15,872] |
13,395 [11,582–14,838] |
15,951 [14,318–15,951] |
| PBA AUC0–2w/MIC | - | - | - | 17,741 [14,715–18,989] |
20,107 [18,416–20,107] |
| PBA AUC0–3w/MIC | - | - | - | - | 22,388 [20,741–22,388] |
| PBA Cumul. AUC0–4w /MIC (mg/L·h) | - | 23,338 [17,948–26,976] |
44,505 [40,229–53,309] |
34,956 [31,277–41,439] |
38,541 [36,957–38,541] |
| Terminal half-life | - | 508 | 633 | 413 | 437 |