Summary of mean ± SD CPT-11, SN-38, and SN-38G pharmacokinetic parameters
| Dose (mg/m2) | |||||||
|---|---|---|---|---|---|---|---|
| 240 (n = 3) | 290 (n = 12) | 320 (n = 13) | 340 (n = 6) | ||||
| CPT-11 | |||||||
| t1/2 (h) | 12.9 ± 3.6 | 12.8 ± 1.8 | 11.9 ± 1.7 | 12.2 ± 1.6 | |||
| Cmax (ng/ml) | 2810 ± 314 | 3418 ± 975 | 3432 ± 587 | 3392 ± 874 | |||
| AUC (ng/ml·h) | 18091 ± 1657 | 22270 ± 5882 | 22695 ± 8546 | 22998 ± 7336 | |||
| CL (liters/h/m2) | 11.6 ± 1.0 | 12.1 ± 3.8 | 13.6 ± 4.3 | 12.1 ± 3.8 | |||
| Vz (liters/m2) | 215 ± 60 | 229 ± 91 | 240 ± 95 | 229 ± 91 | |||
| Vss (liters/m2) | 120 ± 13 | 122 ± 52 | 122 ± 35 | 122 ± 52 | |||
| SN-38 | |||||||
| Tmax (h)a | 1.55 ± 0.05 | 1.84 ± 0.72 | 2.15 ± 0.83 | 2.02 ± 0.40 | |||
| Cmax (ng/ml) | 41 ± 2 | 68 ± 40 | 68 ± 27 | 56 ± 28 | |||
| AUC (ng/ml·h) | 638 ± 124 | 797 ± 405 | 712 ± 276 | 714 ± 415 | |||
| t1/2 (h) | 27.1 ± 12.5 | 21.5 ± 5.7 | 19.3 ± 7.0 | 21.0 ± 8.2 | |||
| SN-38G | |||||||
| Tmax (h)a | 1.83 ± 0.14 | 2.07 ± 0.40 | 2.37 ± 0.61 | 1.84 ± 0.35 | |||
| Cmax (ng/ml) | 109 ± 30 | 160 ± 61 | 198 ± 81 | 168 ± 69 | |||
| AUC (ng/ml·h) | 1710 ± 465 | 2421 ± 1347 | 2663 ± 1413 | 2329 ± 1199 | |||
| t1/2z (h) | 20.3 ± 3.8 | 19.7 ± 7.0 | 17.0 ± 4.5 | 17.2 ± 3.6 | |||
| AUC ratiosb | |||||||
| SN-38/CPT-11 | 5.0 ± 0.5 | 5.2 ± 2.2 | 4.8 ± 2.1 | 4.3 ± 1.8 | |||
| SN-38G/CPT-11 | 13.7 ± 4.6 | 15.4 ± 7.2 | 16.8 ± 8.4 | 14.1 ± 4.9 | |||
a Time relative to the start of the infusion.
b Ratio of SN-38 or SN-38G to CPT-11 AUC, expressed as a percentage.