Table 1

Concentrations of CPT-11 and its metabolites after three i.v. infusions of 90 min a

Time (h)Concentration (nm) CPT-11Concentration (nm) SN-38
LactoneCarboxLactoneCarboxSN-38 glu
Cycle 1
−0.10.00.00.00.00.0
1.51338.21214.722.620.6206.9
1.6708.8956.423.420.4219.7
1.7603.71025.722.121.0241.1
2.0574.61182.122.523.4243.5
2.5468.11139.622.022.8291.7
3.5365.11129.015.722.2344.5
5.5292.5970.912.916.1369.7
9.6239.6801.311.014.7414.6
25.587.3287.38.510.6321.8
50.043.2137.16.611.5330.3
74.024.975.25.510.9282.5
148.05.817.24.29.1100.6
167.65.013.33.58.797.5
191.4n.d.4.6n.d.b5.979.1
412.9n.d.n.d.n.d.n.d.5.9
435.1n.d.n.d.n.d.n.d.6.1
506.6n.d.n.d.n.d.n.d.4.2
Cycle 2
1.5202.2296.012.120.277.5
9.271.0180.84.112.4193.1
24.824.664.7n.d.4.9173.4
47.710.830.53.23.7149.9
73.24.612.3n.d.n.d.72.6
124.2n.d.n.d.n.d.n.d.24.6
163.9n.d.n.d.n.d.n.d.15.1
Cycle 3
1.5268.5298.717.917.696.8
24.220.861.33.15.5165.2
46.36.624.42.74.195.4
70.7n.d.13.0n.d.3.366.8
118.7n.d.3.9n.d.n.d.44.4
  • a In cycles 1, 2, and 3, the patient received CPT-11 at a dose of 100, 30, and 30 mg/m2, respectively. After 96 h and 120 h, and between 144 and 168 h, transfusion of 1050 ml of red cells was given.

  • b n.d., signals below lower limit of quantification of 3 nm.