Pharmacokinetic variables of temsirolimus on day 5, mean ± SD (no. patients)
| Dose group (mg/m2) | Cmax (ng/mL) | tmax (h) | t1/2 (h) | AUC (cycle 1; ng h/mL) | AUC (cycle 3; ng h/mL) | CLc (L/h) | Vdss (L) | AR | B/Pratio (day 1) |
|---|---|---|---|---|---|---|---|---|---|
| 0.75 | 72 ± 16 (3) | 0.67 ± 0.29 (3) | 24.8 ± 7.5 (2) | 1,355 ± 732 (2) | — | 6.2 ± 3.3 (2) | 132.1 ± 14.2 (2) | 2.2 ± 1.1 (3) | 10.9 ± 13.9 (2) |
| 1.25 | 133 ± 64 (3) | 0.46 ± 0.28 (30) | 12.6 ± 5.1 (3) | 2,502 ± 1,531 (3) | 2,812 (1) | 5.2 ± 2.7 (3) | 57.1 ± 21.7 (3) | 1.0 ± 0.6 (3) | 10.4 ± 3.2 (4) |
| 2.16 | 186 ± 51 (5) | 0.59 ± 0.24 (5) | 16.4 ± 6.9 (5) | 3,896 ± 986 (5) | 4,705 ± 1,781 (3) | 5.5 ± 1.4 (5) | 81.5 ± 23.7 (5) | 1.3 ± 0.4 (5) | 9.1 ± 6.3 (6) |
| 4.5 | 331 ± 72 (4) | 0.46 ± 0.11 (4) | 13.9 ± 2.6 (4) | 5,350 ± 792 (4) | 5,439 ± 2,223 (3) | 7.6 ± 1.5 (4) | 111.1 ± 8.7 (4) | 1.1 ± 0.2 (4) | 3.7 ± 1.7 (4) |
| 15 | 503 ± 293 (5) | 0.26 ± 0.18 (5) | 20.0 ± 22.0 (5) | 8,619 ± 2,188 (5) | 7,756 (1) | 16.5 ± 5.3 (5) | 232.5 ± 110.9 (5) | 0.7 ± 0.4 (4) | 1.5 ± 0.9 (6) |
| 19 | 796 ± 226 (12) | 0.41 ± 0.13 (12) | 15.4 ± 15.6 (12) | 9,838 ± 3,504 (12) | 9,353 ± 1,053 (4) | 19.9 ± 7.5 (12) | 239.2 ± 116.0 (12) | 0.8 ± 0.1 (11) | 1.5 ± 0.6 (12) |
Abbreviations: Cmax, peak observed concentration; tmax, time to Cmax; t1/2, terminal half-life; AUC, area under the concentration versus time curve; CLc, central clearance; Vdss, steady-state volume of distribution; AR, accumulation ratio of day 5 to day 1; B/Pratio, blood-to-plasma concentration ratio.