Table 3.
Summary of secondary PK parameters of everolimus by treatment (PK population, N=22)
| Everolimus treatment | Statistics | AUCall (ng · h/mL) |
AUC0–144h (ng · h/mL) |
Tmax (h) |
Lambda_z (1/h) |
CL/F (L/h) |
T1/2 (h) |
|---|---|---|---|---|---|---|---|
| 1×5 mg | Mean (SD) | 238 (60.7) | 238 (60.5) | N/A | 0.0227 (0.00366) | 21.2 (5.19) | 31.2 (4.79) |
| CV% mean | 25.5 | 25.5 | N/A | 16.1 | 24.5 | 15.4 | |
| Geometric mean | 231 | 230 | N/A | 0.0225 | 20.6 | 30.9 | |
| CV% geometric mean | 25.5 | 25.4 | N/A | 15.7 | 25.0 | 15.7 | |
| Median | 219 | 218 | 1.01 | 0.0224 | 21.7 | 31.0 | |
| Min, max | 142, 375 | 142, 373 | 0.500, 2.48 | 0.0163, 0.0331 | 12.9, 33.7 | 21.0, 42.6 | |
| 5×1 mg | Mean (SD) | 260 (75.5) | 260 (75.3) | N/A | 0.0228 (0.00351) | 19.7 (5.79) | 31.1 (4.84) |
| CV% mean | 29.0 | 29.0 | N/A | 15.4 | 29.4 | 15.6 | |
| Geometric mean | 250 | 250 | N/A | 0.0225 | 19.0 | 30.7 | |
| CV% geometric mean | 30.2 | 30.1 | N/A | 15.6 | 29.0 | 15.6 | |
| Median | 263 | 263 | 0.500 | 0.0226 | 18.3 | 30.7 | |
| Min, max | 135, 450 | 135, 449 | 0.500, 1.02 | 0.0173, 0.0289 | 10.7, 34.7 | 24.0, 40.0 |
Notes: For Tmax, only median and range are presented. CV% = SD/mean ×100. CV% geometric mean = sqrt (exp [variance for log-transformed data] − 1) ×100.
Abbreviations: AUC0–144h, area under the concentration–time curve from time zero to the 144-hour concentration sampling time; AUCall, area under the concentration– time curve from time zero to time of last observation time point, regardless of whether the last concentration is quantifiable; CL/F, systemic clearance; CV%, coefficient of variation (%); Lambda_z, terminal slope of elimination phase; N/A, not applicable; PK, pharmacokinetics; SD, standard deviation; sqrt, square root; T1/2, terminal half-life; Tmax, time taken to reach maximum blood concentration; min, minimum; max, maximum.