Table 2.
Pharmacokinetic properties of everolimus in various patient populations
| Patient population | Tmax (h) | Cmax (ng/mL) | AUC (ng/mL · h) 0–∞ | Half-life (h) |
|---|---|---|---|---|
| Healthy subjectsa (n = 24) 2.0 mg dose54 |
0.5 (0.5–2.0) | 17.9 ± 5.9 | 122 ± 52 | 31.5 ± 6.4 |
| Healthy subjectsa (n = 12) 4.0 mg dose66 |
0.5 (0.5–1.0) | 44.2 ± 13.3 | 219 ± 69 | 32.2 ± 6.1 |
| Refractory advanced solid tumor patients aged ≥18 years (n = 4)a 5.0 mg dose53 |
1 (1) | 32 ± 9 | 238 ± 77 | — |
| Refractory or recurrent solid tumor patients aged ≥3 years to <22 years (n = 6)b 2.1 mg/m2 67 |
1 (0.5–1.2) | 21.5 (16.1–78.5) | 139.8 (94.6–197.7) | 18.0 (15.2–19.9) |
| Refractory or recurrent solid tumor patients aged ≥3 years to <22 years (n = 8)b 3.0 mg/m2 67 |
1.1 (0.6–2.3) | 43.5 (18–58) | 197.6 (59.6–249.4) | 15.9 (13.9–22.5) |
Notes:
a
Values are mean ± standard deviation, except for Tmax, which is median (range)
b
all values are median (range).
Abbreviations: AUC, area under the concentration–time curve from zero to infinity; Cmax, maximum concentration; Tmax, time to reach maximum concentration.