Table 3.

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)ARB/Pratio (day 1)
0.7572 ± 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)
1.25133 ± 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)
2.16186 ± 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)
4.5331 ± 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)
15503 ± 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)
19796 ± 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.