Table 4.

Pharmacokinetic variables of sirolimus 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)ARAUCratioAUCsum (ng h/mL)
0.759.3 ± 4.1 (3)25.9* ± 37.5 (3)102.0 ± 46.3 (3)1,866 ± 1,324 (3)1,929 ± 1,132 (2)1.8 ± 0.5 (2)1.2 ± 0.8 (2)3,194 ± 2,603 (2)
1.2527.3 ± 7.6 (3)3.6 ± 2.2 (3)80.3 ± 15.5 (3)4,186 ± 1,293 (3)3,688 (1)1.3 (1)1.7 ± 1.5 (2)7,144 ± 182 (2)
2.1634.3 ± 21.2 (5)3.6 ± 2.1 (5)49.4 ± 27.2 (6)3,240 ± 2,463 (6)5,309 ± 90 (3)1.2 ± 0.4 (3)0.9 ± 0.4 (5)7,740 ± 2,977 (5)
4.548.7 ± 16.7 (4)2.8 ± 2.3 (4)50.3 ± 6.8 (4)5,583 ± 2,728 (4)4,815 ± 1,488 (3)1.1 ± 0.3 (3)1.0 ± 0.4 (4)10,934 ± 3,384 (4)
15.057.8 ± 24.3 (5)1.8 ± 1.5 (5)39.9 ± 1.3 (2)4,729 ± 545 (2)2,958 (1)0.6 ± 0.2 (2)12,687 ± 4,050 (2)
19.1133.9 ± 70.3 (12)2.0 ± 1.5 (12)52.3 ± 14.5 (11)15,503 ± 8,573 (11)11,857 ± 4,724 (4)0.5 ± 0.3 (3)1.8 ± 1.2 (11)2,4781 ± 8,956 (11)
  • Abbreviations: AUCratio, uncorrected ratio of sirolimus to temsirolimus AUC; AUCsum, arithmetic sum of temsirolimus and sirolimus AUC.

  • * One of three patients exhibited an abnormally prolonged tmax.