Table 3.
Pharmacokinetic Parameters for ARN-509 at Steady-State
| Dose Group (mg) | Tmax (hours) | Cmax (μg/mL) | AUC0-24 h (h × μg/mL) | T1/2eff (hours) |
|---|---|---|---|---|
| 30 (n = 3) | ||||
| Mean | 0.7 | 0.841 | 14.7 | 104.0 |
| CV, % | 43.3 | 16.1 | 13.6 | 58.9 |
| 60 (n = 2 or 3) | ||||
| Mean | 2.0 | 1.60 | 29.7 | 96.0 |
| CV, % | 86.6 | 11.0 | 21.6 | 23.7 |
| 90 (n = 3) | ||||
| Mean | 1.2 | 2.53 | 38.3 | 86.8 |
| CV, % | 65.5 | 6.9 | 9.8 | 29.6 |
| 120 (n = 2 or 3) | ||||
| Mean | 9.3 | 3.30 | 59.4 | 108.0 |
| CV, % | 136.0 | 16.4 | 18.2 | 38.8 |
| 180 (n = 3) | ||||
| Mean | 1.0 | 5.98 | 93.7 | 72.0 |
| CV, % | 0.0 | 20.7 | 29.1 | 15.1 |
| 240 (n = 2 or 3) | ||||
| Mean | 3.5 | 7.55 | 127.0 | 86.2 |
| CV, % | 112.0 | 15.3 | 28.7 | 18.0 |
| 300 (n = 4 or 5) | ||||
| Mean | 6.1 | 7.08 | 134.0 | 72.6 |
| CV, % | 164.0 | 31.0 | 27.9 | 26.7 |
| 390 (n = 3) | ||||
| Mean | 1.0 | 8.91 | 140.0 | 74.8 |
| CV, % | 50.0 | 11.2 | 15.7 | 22.0 |
| 480 (n = 3) | ||||
| Mean | 1.2 | 11.2 | 202.0 | 86.1 |
| CV, % | 49.5 | 4.2 | 4.8 | 6.8 |
Abbreviations: AUC0-24 h, area under plasma concentration-time curve over 0 to 24 hours; Cmax, maximum observed plasma; CV, coefficient of variation; T1/2eff, effective half-life; Tmax, time of maximum observed plasma.