Table S1.
Noncompartmental pharmacokinetic parameters for DTS-108, SN-38, and SN-38G
| Dose (mg/m2) | DTS-108
|
SN-38
|
SN-38G
|
AUCSN-38/AUCDTS-108 (×10−3) | AUCSN-38G/AUCSN-38 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cmax (ng/mL) | Tmax (hours) | AUCinf (h·ng/mL) | CV (%) | Cmax (ng/mL) | Tmax (hours) | AUCinf (h·ng/mL) | CV (% | Cmax (ng/mL) | Tmax (hours) | AUCinf (h·ng/mL) | CV (%) | |||
| 3 | 1.004 | 0.25 | 1.702 | – | 6 | 0.25 | 24 | – | 9 | 2.00 | 39 | – | 14.2 | 1.61 |
| 6 | 0.967 | 1.00 | 1.185 | – | 11 | 1.00 | 17 | – | – | – | – | – | 14.3 | – |
| 12 | 4.741 | 0.97 | 10.616 | – | 30 | 1.50 | 136 | – | 10 | 8.00 | – | – | 12.8 | – |
| 24 | 6.887 | 0.98 | 13.845 | – | 54 | 0.98 | 168 | – | 18 | 8.00 | – | – | 12.2 | – |
| 32 | 15.289 | 1.11 | 42.616 | 25.2 | 98 | 0.94 | 528 | 28.4 | 38 | 5.69 | 853 | 43.1 | 12.1 | 1.18 |
| 42 | 21.299 | 1.32 | 56.071 | 15.9 | 109 | 1.52 | 570 | 18.0 | 57 | 6.00 | 801 | 54.4 | 12.1 | 1.48 |
| 56 | 12.773 | 0.96 | 38.578 | 39.0 | 154 | 1.36 | 1,076 | 11.1 | 86 | 6.58 | 1.077 | 57.9 | 29.2 | 1.07 |
| 75 | 22.667 | 1.44 | 58.889 | 16.8 | 227 | 1.28 | 738 | 17.1 | 45 | 6.76 | 583 | 28.1 | 12.6 | 0.78 |
| 100 | 30.283 | 1.31 | 93.433 | 29.0 | 182 | 1.86 | 792 | 9.5 | 113 | 7.36 | 1.456 | 33.3 | 9.4 | 1.80 |
| 133 | 56.269 | 0.99 | 153.763 | 20.0 | 310 | 1.21 | 1,724 | 54.0 | 163 | 7.02 | 3.792 | 98.4 | 11.7 | 1.69 |
| 177 | 60.346 | 1.45 | 220.265 | 13.8 | 652 | 2.34 | 2,653 | 26.5 | 131 | 5.35 | 1.985 | 38.6 | 12.1 | 0.74 |
| 235a | 63.926 | 1.27 | 239.567 | 23.6 | 757 | 2.02 | 3,642 | 66.0 | 339 | 4.54 | 4.148 | 73.7 | 15.2 | 1.48 |
| 313a | 116.067 | 1.68 | 439.293 | 17.6 | 202 | 1.96 | 1,992 | 30.0 | 310 | 6.73 | 4.538 | 51.5 | 4.5 | 2.38 |
| 416a | 134.333 | 2.47 | 566.735 | 13.1 | 225 | 2.79 | 2,059 | 18.8 | 381 | 6.82 | 5.681 | 51.5 | 3.6 | 2.63 |
Note:
a
Samples were processed using the revised procedure and were analyzed at MicroConstant Inc.
Abbreviations: CV, coefficient of variation of Cmax; SN-38, 7-ethyl-10-hydroxycampthotecin; SN-38G, SN-38 glucuronide; AUCinf, area under the plasma concentration–time curve to infinity; Cmax, the peak of the concentration.