Table 4.
Summary of pharmacokinetic parameters following Day 5 administration of CPX-351
| Cytarabine | Ara-U | Daunorubicin | Daunorubicinol | |
|---|---|---|---|---|
| Mean Cmax (SD), µg/mL | 62.2 (20.9) | 1.24 (0.25) | 26.0 (8.5) | 0.147 (0.52) |
| Median Tmax (range), h | 2.00 (0.75–8.33) | 8 (5.78–8.33) | 2.0 (0.75–6.02) | 26.2 (1.5–48.0) |
| Mean AUC0-48 h (SD), µg × h/mL | 1900 (844) | 44 (11.3) | 637 (244) | 6.24 (2.27) |
| Mean CLss (SD), L/h | 0.131 (0.0791) | 0.163 (0.087) | ||
| Mean Vz (SD), L | 7.11 (3.50) | 6.64 (2.44) | ||
| Mean t1/2 (SD), h | 40.4 (9.77) | 60.3 (15.6) | 31.5 (9.0) | 43.9 (10.7) |
| M:P ratio (%) | 3.22 (1.47) | 1.79 (0.443) | ||
| Mean cumulative dose recovered (SD), % | 1.11 (0.35) | 69.6 (33.9) | 3.19 (0.91) | 5.80 (2.49) |
| Mean CLr (SD), L/h | 0.00167 (0.00102) | 3.81 (2.02) | 0.0061 (0.0028) | 1.13 (0.74) |
| Total drug in urine,a % | 70.7 (33.8)a | 9.00 (3.21)a | ||
Cmax maximum observed concentration, SD standard deviation, Tmax time of maximum observed concentration, AUC area under the concentration–time curve, CLss total body clearance, Vz volume of distribution based on the terminal elimination phase, t1/2 terminal phase half-life, M:P ratio metabolite to parent ratio, CLr renal clearance
aPercent of drug recovered in urine was the sum of parent and metabolite in urine during the 48-h interval following Day 5 administration of CPX-351