Table 5.
Summary of pharmacokinetic parameters
| Cohort | Day | Cmax (ng/mL) geometric mean (% CV) |
Tmax (h) median (min, max) |
AUC0-8h (ng*h/mL) geometric mean (% CV) | RCmax geometric mean (% CV) | RAUC geometric mean (% CV) |
|---|---|---|---|---|---|---|
| 1 | Cycle 1 day 1 (n = 3) | 3050 (40) | 2.1 (1.8–8.0) | 12,800 (34) | – | – |
| Cycle 1 day 15 (n = 3) | 8420 (16) | 1.0 (0.0–2.0) | 48,900 (35) | 2.8 (47) | 3.8 (67) | |
| 2 | Cycle 1 day 1 (n = 8) | 3460 (39) | 2.0 (0.8–4.0) | 15,900 (30) | – | – |
| Cycle 1 day 15 (n = 7)a | 10,400 (31) | 1.8 (0.0–2.1) | 62,900 (26) | 3.2 (57) | 4.1 (52) |
AUC0-8h, area under the plasma concentration-time curve from 0 to 8 h; Cmax, maximum plasma concentration; % CV, percent geometric coefficient of variation; RAUC, ratio of AUC0-8h on cycle 1 day 15 to AUC0-8h on cycle 1 day 1; RCmax, ratio of Cmax on cycle 1 day 15 to Cmax on cycle 1 day 1; Tmax, time to reach Cmax
aOne patient from cohort 2 was excluded from the pharmacokinetic analysis because of a lack of measurements