Table 4.
Plasma pharmacokinetic parameters for S-1 components and paclitaxel
| Dose level | FT | 5-FU | CDHP | Oxo | Paclitaxel | |||||
|---|---|---|---|---|---|---|---|---|---|---|
| Mean | SD | Mean | SD | Mean | SD | Mean | SD | Mean | SD | |
| Level 1 and 2a (n = 6) | ||||||||||
| tmax, h | 1.3 | 0.5 | 2.3 | 0.8 | 1.5 | 0.5 | 1.7 | 0.5 | 0.5 | 0.0 |
| Cmax, ng/mL | 1901 | 310 | 148.9 | 65.0 | 417.0 | 69.9 | 53.51 | 77.41 | 4778 | 343 |
| AUC0–t, ng/h/mL | 12 201 | 3119 | 695.4 | 276.3 | 1463 | 360 | 230.5 | 409.8 | 4583 | 479 |
| AUCinf, ng/h/mL | 21 998 | 8800 | 718.6 | 271.7 | 1567 | 422 | 1217 | NA | 4806 | 490 |
| t1/2, h | 8 | 1.8 | 1.6 | 0.5 | 2.5 | 0.2 | 3.4 | NA | 26.2 | 3.9 |
| Level 2b and 3 (n = 6) | ||||||||||
| tmax, h | 1.3 | 0.5 | 2.3 | 0.8 | 1.2 | 0.4 | 1.7 | 0.5 | 0.5 | 0.0 |
| Cmax, ng/mL | 2768 | 432 | 193.9 | 83.1 | 452.6 | 97.5 | 80.19 | 63.11 | 5689 | 1056 |
| AUC0–t, ng/h/mL | 16 057 | 3697 | 903.5 | 310.4 | 1648 | 175 | 275.8 | 201.7 | 4876 | 1007 |
| AUCinf, ng/h/mL | 29 732 | 12 675 | 933.7 | 300.9 | 1772 | 119 | 411.5 | 258.6 | 5087 | 1066 |
| t1/2, h | 8.3 | 2.4 | 1.7 | 0.4 | 2.7 | 0.7 | 2.7 | 2.0 | 25.2 | 2.6 |
AUC, area under the curve; AUCinf, AUC from time zero extrapolated to infinity; AUC0–t, AUC from time zero to t; CDHP, 5-chloro-2.4-dihydrooxypyridine; Cmax, maximum plasma concentration; FT, tegafur; 5-FU, 5-fluorouracil; NA, not applicable; Oxo, oteracil potassium; t1/2, half-life time; tmax, maximum concentration time.