Table 1. Summary of apremilast, M12, and M14 plasma pharmacokinetic parameters on day 5 following multiple oral doses of apremilast (geometric mean, geometric CV%).
| Apremilast 30 mg b.i.d. | Apremilast 50 mg b.i.d. | |||||
|---|---|---|---|---|---|---|
| Apremilast n = 53 |
M12 n = 53 |
M14 n = 53 |
Apremilast n = 55 |
M12 n = 55 |
M14 n = 55 |
|
| tmax a (h) | 2.0 (0.5 – 6.0) | 3.0 (1.0 – 12.0) | 3.0 (0.5 – 12.0) | 2.0 (0.6 – 6.0) | 3.0 (0.5 – 6.0) | 3.0 (0.5 – 6.0) |
| Cmax (ng/mL) | 351.8 (37.1) | 44.2 (27.7) | 41.8 (41.1) | 507.2 (32.3) | 659.1 (21.0) | 62.2 (35.3) |
| AUC0–τ (ng×h/mL) | 2,260 (36.1) | 3,930 (23.9) | 363.8 (35.9) | 3,451 (38.6) | 5,968 (20.0) | 544.9 (33.9) |
| t1/2 (h) | 6.41 (24.3)b | 12.18 (25.9)c | 19.20 (49.0)d | 7.28 (29.1) | 12.79 (29.0)e | 20.31 (57.1)f |
aThe tmax is summarized by median and range (minimum–maximum); bn = 52 for half-life calculations; cn = 35 for half-life calculations; dn = 10 for half-life calculations; en = 46 for half-life calculations; fn = 19 for half-life calculations. b.i.d. = twice daily; CV% = coefficient of variation; Cmax = maximum plasma concentration; tmax = time to maximum plasma concentration; t1/2 = estimate of the terminal elimination half-life in plasma; AUC0–τ = area under the plasma concentration-time curve from time 0 to the dosing interval τ (the dosing interval is 12 hours).