Table 3.

Pharmacokinetic analysis (noncompartmental analysis) of sirolimus with or without ketoconazole or grapefruit juice

Sirolimus dose, mg, nKeto 0 = non 1 = KetoGFJ 0 = non 1 = GFJCmax (ng/mL)aCmax CV%aAUC∞ (ng-h/mL)aAUC∞ CV%aT1/2 (h)T1/2 CV%CL/F (l/h)aCL/F CV%a
1 (6)05.431.41861028215610.387.2
125.436.89353050471.243.7
2 (6)09.959.62717445419.537.8
133.247.81,3473152281.858.5
3 (6)017.454.94002635368.027.3
149.262.22,44873841011.643.8
4 (6)021.335.745642363510.037.4
166.871.92,8977961502.153.5
5 (6)025.843.26764635279.049.9
171.270.13,1447257352.881.5
6 (3)015.055.551063787615.662.0
174.692.72,6203862602.645.3
8 (1)025.24201819.1
185.21,624344.9
16 (2)047.415.81,45617257911.217.1
1123.07.65,00733263.23.2
15 (5)050.328.185837367120.552.4
1127.952.04,3615246415.9109.4
20 (5)045.673.086382264436.971.6
1105.365.82,79762535211.579.1
25 (4)084.768.01,44977304732.6102.4
1173.955.34,5388040299.279.5
30 (5)068.536.11,81448303718.739.9
182.137.52,41917352112.614.7
35 (8)068.162.31,79972435829.464.0
1129.765.36,655835610312.8135.3
  • aP < 0.05 for combined dose levels.