Table 4.
First-dose pharmacokinetic parameters for PF-06263507a
| Dose (mg/kg) | N | Cmax (μg/mL) | AUCinf (μg × d/mL) | Terminal t1/2 (days) | Vss (L) | CL (L/day) |
|---|---|---|---|---|---|---|
| 0.05 | 2 | 0.8 (−) | 1.8 (−) | 3.0 (−) | 9.5 (−) | 3.4 |
| 0.10 | 2 | 2.4 (−) | 4.7 (−) | 1.5 (−) | 3.5 (−) | 1.7 |
| 0.19 | 2 | 4.0 (−) | 10.4 (−) | 4.5 (−) | 6.2 (−) | 1.5 |
| 0.37 | 2 | 9.5 (−) | 24.2 (−) | 3.5 (−) | 6.3 (−) | 1.5 |
| 0.73 | 2 | 21.2 (−) | 52.3 (−) | 4.4 (−) | 5.0 (−) | 1.0 |
| 1.42 | 2 | 45.5 (−) | 90.4 (−) | 3.8 (−) | 5.5 (−) | 1.3 |
| 2.78 | 2 | 65.7 (−) | 123.7 (−) | 4.2 (−) | 4.2 (−) | 0.9 |
| 4.34 | 6 | 102.9 (22%) | 418.3 (12%) | 6.0 (15%) | 5.3 (16%) | 0.7 (22%) |
| 5.42 | 3 | 142.0 (48%) | 332.7 (19%) | 5.4 (9%) | 5.6 (21%) | 1.0 (23%) |
| 6.50 | 3 | 109.1 (40%) | 486.2 (−) | 5.5 (−) | 7.4 (−) | 1.1 |
C max maximum concentration, AUC inf area under the curve from 0 to infinity, t 1/2 terminal half-life, V ss volume of distribution at steady state, CL clearance
aData are presented as geometric mean (% coefficient of variation), with the exception of t1/2, which is presented as arithmetic mean (% coefficient of variation). Summary statistics are not presented if fewer than three patients had reportable parameter values