Table 1. Pharmacokinetic parameters for everolimusa in humans and mice.
Dose | Species | t½ (hr) | AUC0→t (ng·hr/mL) | Cmax (ng/mL) | Cmin (ng/mL) | Ref. | |
Everolimus a | |||||||
10 mg | Human | – | 514±231 | 61±17b | 13.3b | [25] | |
10 mg | Human | – | 711±113 | 66±1.4b | ∼20bd | [26] | |
5 mg | Human | – | 238±77 | 32±9b | †5.4 | [25] | |
5 mg | Human | – | 543±189 | 58±18b | ∼12–14bd | [26] | |
10 mg/kg | Mouse | 5.0 | 11592 | 1684±277b | 59±5b | ||
2.5 mg/kg | Mouse | 6.0 | 1921 | 350±230b | 12±6b | ||
5 mg/kge | Mouse | 5.7 | 3716 | 561bc | 21b |
All PK data obtained for everolimus is for daily oral administration.
Steady-state parameter.
Value of Cmax for simulated data is taken at 0.5 h for comparison to data measured at this time.
Data estimated from graph in references.
Data for 5 mg/kg RAD001 is based on simulations.