Table 5.
Pharmacokinetic parameters of ABT-288 (mean ± SD) after administration of escalating single oral doses to healthy young adults
| Parameter | 0.1 mg (n = 6)* | 0.3 mg (n = 6) | 1 mg (n = 6) | 3 mg (n = 6) | 10 mg (n = 6) | 20 mg (n = 6) | 40 mg (n = 6) |
|---|---|---|---|---|---|---|---|
| Cmax (ng ml−1) | 0.06 ± 0.01 | 0.14 ± 0.05 | 0.58 ± 0.10 | 1.62 ± 0.46 | 6.80 ± 1.52 | 13.2 ± 2.19 | 26.5 ± 4.25 |
| tmax (h)† | 4 (3–6) | 5 (4–6) | 4 (2–4) | 4 (4–6) | 3 (2–4) | 4 (3–6) | 4 (2–6) |
| t1/2 (h)‡ | ND | 56 ± 11 | 61 ± 15 | 43 ± 10 | 47 ± 5 | 41 ± 9 | 49 ± 11 |
| AUC(0,tlast) (ng h ml−1) | 1.1 ± 0.5 | 5.1 ± 1.4 | 19 ± 2.9 | 55 ± 10 | 230 ± 62 | 440 ± 79 | 970 ± 220 |
| AUC(0,∞) (ng h ml−1) | ND | 7.3 ± 1.6 | 28 ± 7.2 | 70 ± 9.1 | 270 ± 74 | 480 ± 96 | 1130 ± 340 |
| CL/F (l h−1) | ND | 43 ± 7.8 | 37 ± 9.1 | 44 ± 6.3 | 40 ± 9.6 | 43 ± 7.6 | 38 ± 11 |
*
The concentrations of ABT-288 at the 0.1 mg level were close to or below the LLOQ. Consequently robust estimates of t1/2, and AUC(0,∞) could not be obtained.
†
Median and range (minimum-maximum) are presented.
‡
Harmonic mean ± pseudo-standard deviation is presented. ND, Not determined.