Table 4.
Pharmacokinetic parameters of enzalutamide in castration-resistant prostate cancer patients after multiple oral dose administration
| Study | Dose (mg/day)a | Subjects (n) | C max (μg/mL)b | AUCτ (μg·h/mL)b | t max (h)c | CL/F (L/h)b |
|---|---|---|---|---|---|---|
| Dose escalationd | 30 | 3 | 2.8 ± 0.6 | 61 ± 12 | 2.1 [1.0–3.9] | 0.51 ± 0.11 |
| 60 | 21 | 5.7 ± 1.5 | 115 ± 34 | 1.1 [0.5–23.7] | 0.58 ± 0.25 | |
| 150 | 23 | 14.5 ± 3.3 | 300 ± 68 | 1.0 [0.0–25.8] | 0.53 ± 0.15 | |
| 240 | 29 | 19.5 ± 5.0 | 410 ± 112 | 1.1 [0.0–26.2] | 0.63 ± 0.18 | |
| 360 | 16 | 25.1 ± 5.2 | 502 ± 119 | 1.6 [0.5–24.1] | 0.76 ± 0.18 | |
| 480 | 1 | 27.9 | 463 | 0.0e | 1.1 | |
| All doses combined | 93 | NC | NC | 1.1 [0.0–26.2] | 0.61 ± 0.20 | |
AUC τ area under the plasma concentration–time curve for one 24-h dosing interval at steady state, CL/F apparent oral clearance, C max maximum plasma concentration, NC not calculated, t max time to reach C max
aEnzalutamide was administered by once-daily dosing in all dose groups except for 480 mg/day, in which it was administered as a divided dose (240 mg twice daily), with approximately 12 h between the two doses
bValues are expressed as mean ± standard deviation
cValues are expressed as median [range]
dDose-escalation study, multiple-dose period [5]; pharmacokinetics were assessed after approximately 3 months of dosing
e t max was observed in the predose sample