Table 3

Metabolites of capecitabine in urine from rats or mice collected over 72 h after administration of capecitabine at a dose of 80 mg/kg B.W. for rat and LD mice groups and 500 mg/kg B.W. for the HD mice group

0–6 h6–24 h24–48 h48–72 hOver 72 h
CAP
 Rat3.5  ± 0.70.79  ± 0.440.02  ± 0.034.3  ± 1.0
 LD mice10  ± 33-150 1.4  ± 0.43-150 0.09  ± 0.083-150 0.04  ± 0.0612  ± 23-150
 HD mice3.3  ± 3.83-151 3.5  ± 0.63-151 0.73  ± 0.263-151 0.19  ± 0.177.7  ± 2.63-151
5′-DFCR
 Rat 37  ± 15 25  ± 6 2.9  ± 1.0 0.58  ± 0.70 65  ± 11
 LD mice14  ± 23-150 1.7  ± 0.83-150 0.09  ± 0.083-150 0.08  ± 0.073-150 16  ± 13-150
 HD mice5.4  ± 5.43-151 6.9  ± 1.93-151 1.3  ± 0.73-151 0.47  ± 0.373-151 14  ± 2
5′-DFUR
 Rat1.9  ± 1.61.2  ± 0.30.16  ± 0.090.06  ± 0.103.3  ± 2.1
 LD mice 23  ± 23-150 6.2  ± 1.73-150 0.45  ± 0.263-150 0.27  ± 0.34 30  ± 13-150
 HD mice 6.1  ± 5.13-151 13  ± 33-151 3.5  ± 1.93-151 0.88  ± 0.6823  ± 23-151
5-FU
 Rat0.01  ± 0.020.01  ± 0.020.02  ± 0.030.06  ± 0.100.10  ± 0.12
 LD mice0.02  ± 0.030.10  ± 0.180.01  ± 0.020.06  ± 0.070.19  ± 0.24
 HD mice0.01  ± 0.010.08  ± 0.020.03  ± 0.010.02  ± 0.010.14  ± 0.02
5-FUH2
 Rat
 LD mice0.12  ± 0.110.07  ± 0.060.19  ± 0.17
 HD mice0.05  ± 0.060.15  ± 0.020.06  ± 0.040.26  ± 0.08
FUPA + FBAL3-a
 Rat1.5  ± 0.52.4  ± 1.10.35  ± 0.120.10  ± 0.174.4  ± 1.3
 LD mice11  ± 13-150 11  ± 0.53-150 1.2  ± 0.43-150 0.69  ± 0.91 24  ± 23-150
 HD mice3.0  ± 2.83-151 14  ± 23-151 6.2  ± 2.93-151 1.2  ± 0.6 24  ± 1
5-FC + 5-FCOH
 Rat0.14  ± 0.040.47  ± 0.350.61  ± 0.42
 LD mice0.06  ± 0.080.22  ± 0.170.28  ± 0.22
 HD mice0.07  ± 0.040.50  ± 0.073-151 0.19  ± 0.080.01  ± 0.010.77  ± 0.193-151
F−
 Rat0.64  ± 0.261.8  ± 0.41.8  ± 1.3 1.5  ± 0.5 5.7  ± 1.3
 LD mice0.64  ± 0.371.0  ± 0.43-150 1.2  ± 0.7 0.64  ± 0.693-150 3.4  ± 0.73-150
 HD mice0.05  ± 0.063-151 0.73  ± 0.250.48  ± 0.153-151 0.48  ± 0.061.7  ± 0.23-151
Total
 Rat45  ± 1731  ± 85.3  ± 1.72.3  ± 0.784  ± 10
 LD mice59  ± 622  ± 33.0  ± 0.71.8  ± 1.286  ± 1
 HD mice18  ± 173-151 39  ± 43-151 13  ± 63-151 3.3  ± 1.973  ± 63-151

Data are expressed as % a.d. Data in bold characters represent the main metabolite in each urine fraction or in total collection.

  • ↵3-a  CFBAL and FHPA included when detected.

  • ↵3-150  Significant difference between rat and LD mice groups (p < 0.05).

  • ↵3-151  Significance difference between LD mice and HD mice groups (p < 0.05).