Table 2.
Pharmacokinetic parameters following dosing of different enzalutamide formulations (50 mg/kg oral dose).
| Formulation | AUC0–inf (µg h/mL) | Cmax (µg/mL) | Tmax (h) | t1/2 (h) | t1/2abs (h) | Fa |
|---|---|---|---|---|---|---|
| Crystalline Slurry | 43.1 (4.6) | 1.04 (0.03) | 5.0 (1.0) | 22.2 | 1.9 | 3.6 (0.3)% |
| 50:50 CA Sub | 45 (14) | 1.44 (0.34) | 12.0 (6.2) | 12.1 | 3.6 | 4.3 (2.4)% |
| SEDDS | 283 (11) | 9.34 (0.42) | 4.0 (1.0) | 20.7 | 1.1 | 31.5 (3.3)% |
| 50:50 CPHPC-106 | 305 (19) | 11.7 (0.3) | 3.0 (0.0) | 14.7 | 0.9 | 28.4 (2.2)% |
| 10:90 CPHPC-106 | 516 (137) | 15.3 (2.1) | 2.7 (0.3) | 15.1 | 1.0 | 46.0 (18.6)% |
Values in parentheses are standard deviations, n = 3.
aF, absolute bioavailability, was estimated from intraveneous bolus dosed at 10 mg/kg AUC0–inf.