Table 1. Summary of pharmacokinetic data for abiraterone acetate when given orally in single and multiple dose studies.
Patient | Dose (mg m−2) | AUC (μM h−1) | Cmax (μM) | Tmax (h) | T1/2α (h) | T1/2β (h) | Kabs (h) |
---|---|---|---|---|---|---|---|
1 | 10 | ND | ND | ND | ND | ND | ND |
2 | 10 | ND | 0.001 | 2 | ND | ND | ND |
3 | 10 | ND | 0.018 | 11 | ND | ND | ND |
4 | 30 | ND | ND | ND | ND | ND | ND |
5 | 30 | ND | 0.004 | 4 | ND | ND | ND |
6 | 30 | ND | 0.006 | 1 | ND | ND | ND |
7 | 100 | 0.15 | 0.012 | 13 | 6.5 | ND | 6.5 |
8 | 100 | 0.09 | 0.011 | 0.16 | 0.97 | 26.5 | 0.03 |
9 | 100 | 0.12 | 0.019 | 3.7 | 2.0 | 28 | 1.8 |
10 | 200 | 0.39 | 0.061 | 2.8 | 1.59 | 25.8 | 3.87 |
11 | 500 | 0.25 | 0.063 | 0.8 | 0.28 | 29 | 0.01 |
12 | 500 | 1.68 | 0.139 | 3.7 | 1.83 | 21 | 1.8 |
13 | 500 | 0.73 | 0.06 | 3.6 | 1.73 | 74 | 1.71 |
14 | 500 | 0.67 | 0.066 | 4 | 1.43 | 18 | 1.41 |
15 | 500 | 0.42 | 0.077 | 2 | 0.29 | 13.4 | 1.00 |
16 | 500 | 1.38 | 0.167 | 2.7 | 0.05 | 13.3 | 1.15 |
17 | 200 | 0.23 | 0.037 | 0.69 | 1.49 | 28 | 0.03 |
18 | 500 | 1.23 | 0.054 | 1.7 | 0.19 | 14.6 | 0.3 |
19 | 500 | 1.101 | 0.183 | 1.51 | 0.71 | 14 | 0.7 |
20 | 500 | 2.08 | 0.30 | 1.41 | 1.59 | 24 | 0.12 |
21 | 500 | 3.54 | 0.62 | 1.70 | 1.07 | 23.2 | 0.82 |
22 | 500 | 0.34 | 0.07 | 2.30 | 0.79 | 12.0 | 0.80 |
23 | 500 | NE | NE | NE | NE | NE | NE |
24 | 800 | 11.66 | 1.19 | 3.02 | 1.32 | 87 | 1.34 |
25 | 800 | 2.32 | 0.43 | 1.20 | 0.45 | 19.9 | 0.45 |
26 | 800 | 2.84 | 0.18 | 3.10 | 1.73 | 26.2 | 1.82 |
Details of subjects: PT 1–16: single dose study in castrate males; PT 17–20: single dose in noncastrate males; PT 21–26: multidose study in noncastrate males. NE=not evaluated due to problems with the assay; ND=not detectable, plasma concentrations too allow to permit estimation of the pharmacokinetic behaviour of the drug; AUC=area under the concentration time curve; Cmax=maximum concentration, Tmax=time to maximum concentration; T1/2α=initial half-life; T1/2β=terminal half-life; Kabs=absorption rate constant.