Table 2.
Summary of pharmacokinetic data of 5-FU in plasma and ECF of tumor tissue
| Parameter | Patient 1 | Patient 3 | Patient 4 | Patient 5 | Patient 6 | Patient 7 |
|---|---|---|---|---|---|---|
| Dose 5-fluorouracil (mg/day) | 2300 | 1890 | 1700 | 2000 | 1650 | 1500 |
| Plasma unbound | ||||||
| Fraction unbound (%)a | 87 ± 3.2 | 93 ± 11 | 97 ± 9.1 | 86 ± 8.5 | 83 ± 4.7 | 88 ± 2.7 |
| AUC0-120 (μg*h/ml)a | 50.8 | 62.7 | 54.6 | 33.6 | 38.6 | NA |
| AUC0-24 (μg*h/ml)b | 8.79 | 11.1 | 7.39 | 7.22 | 6.25 | 6.56 |
| AUC24-48 (μg*h/ml)b | 10.6 | 11.4 | 9.83 | 7.05 | 6.58 | 7.94 |
| AUC48-72 (μg*h/ml)b | 10.2 | 11.8 | 12.4 | 6.74 | 7.39 | NA |
| AUC72-96 (μg*h/ml)b | 10.8 | 14.4 | 13.2 | 5.75 | 8.71 | NA |
| AUC96-120 (μg*h/ml)b | 10.4 | 14.1 | 11.8 | 6.79 | 9.62 | NA |
| ECF tumor tissue | ||||||
| Probe recovery (%)a | 40 ± 4.5 | 89 ± 3.4 | 89 ± 2.7 | 92 ± 2.4 | 63 ± 1.2 | 92 ± 1.2 |
| AUC0–120 (μg*h/ml)b,c | 11.0 (0.22) | NA | 13.0 (0.24) | 13.6 (0.41) | 6.38 (0.17) | 19.3 (NA) |
| AUC0–24 (μg*h/ml)b,c | 1.31 (0.15) | 1.69 (0.15) | 0.92 (0.12) | 2.09 (0.29) | 0.94 (0.15) | 2.61 (0.40) |
| AUC24–48 (μg*h/ml)b,c | 1.70 (0.16) | 2.59 (0.23) | 2.03 (0.21) | 2.43 (0.35) | 1.13 (0.17) | 3.51 (0.44) |
| AUC48–72 (μg*h/ml)b,c | 2.23 (0.22) | 2.60 (0.22) | 2.49 (0.20) | 2.96 (0.44) | 1.24 (0.17) | 5.05 (NA) |
| AUC72–96 (μg*h/ml)b,c | 2.73 (0.25) | NA | 3.82 (0.29) | 2.85 (0.50) | 1.50 (0.17) | 4.28 (NA) |
| AUC96–120 (μg*h/ml)b,c | 3.03 (0.29) | NA | 3.69 (0.31) | 3.26 (0.48) | 1.58 (0.16) | 3.87 (NA) |
AUC area under the concentration time curve, ECF extracellular fluid, NA not available
a Mean ± SD
bCalculated using data observed during a timeframe after start of the infusion with subscript numbers referring to start and endpoint of timeframe
cAUC ratio ECFtumor/Plasmaunbound