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. 2008 Sep 1;26(25):4172–4179. doi: 10.1200/JCO.2008.16.2347

Table 3.

Pharmacokinetic Parameters of Rapamycin

Dose (mg) Day Pharmacokinetic Parameters
Tmax (hours)
Cmax (ng/mL)
Vz/F (L)
Cls/F (L/h)
T1/2,z (hours)
AUC (ng · h/mL)
Css,min (ng/mL)
Median Range No. Mean SD No. Mean SD No. Mean SD No. Mean SD No. Mean SD No. Mean SD No.
2 1 2.02 1.98-3.00 4 7.0 2.7* 4 354.7 371.5 2 29.0 30.6 2 11.13 3.15 4 65.3 69.1* 2 6.6 6.6 4
2 28 2.00 1.07-4.05 3 9.2 1.8* 3 277.5 473.2 2 16.3 0.8 3 11.23 1 122.7 5.6* 3
3 1 2.00 1.00-3.92 3 8.2 2.4* 3 231.9 1 17.5 1 9.20 16.57 2 171.6* 1 7.3 2.8 3
3 28 1.93 1.00-2.00 3 19.3 5.6* 3 541.5 228.4 3 13.1 5.1 3 29.04 9.92 3 254.1 98.7* 3
6 1 2.00 1.00-6.00 9 21.3 8.1* 9 356.1 33.8 3 22.3 2.6 3 14.46 3.11 9 272.1 33.2* 3 12.7 7.1 9
6 28 1.98 1.00-5.12 9 27.6 15.0* 9 562.5 367.6 3 20.5 14.7 9 28.52 8.19 3 445.2 318.1* 9
9 1 2.00 1.00-2.08 5 28.4 13.1* 5 173.8 1 38.2 1 11.44 6.05 4 235.7* 1 23.6 7.4 5
9 28 2.00 4.00 2 37.9 50.8* 2 217.3 395.4 2 12.3 15.2 2 12.21 18.05 2 592.7 729.5* 2
All 1 2.00 1.00-6.00 21 314.3 80.6 7 26.0 7.1 7 12.95* 3.99 19
28 2.00 1.00-8.08 18 467.6 240.8 10 17.7 11.1 17 23.79* 10.03 9

NOTE. When n ≤ 2, individual values are reported. AUCinf is reported for all dose levels for day 1; AUC0-24 hours is reported for all dose levels for day 28.

Abbreviations: AUC, area under the concentration-time curve; Cmax, maximal plasma concentration; Cls/F, apparent systemic clearance; Css,min, steady state plasma concentration at trough; NR, not reportable; Tmax, time of the maximal plasma concentration; T1/2,z, terminal half-life; Vz/F, apparent volume of distribution; SD, standard deviation.

*

P < .05 using a Wilcoxon matched pairs signed-rank test.