First-order rate constants for glucuronidation of SN-38 lactone and carboxylate in microsomes and recombinant isoforms
Numbers in parentheses indicate the parameter coefficient of variance (%).
Matrix | kgluc, lactone | kgluc, carboxylate |
|---|---|---|
| min-1 | min-1 | |
| Human UGT1A1 | 5.17 × 10-4(3.51) | 0.855 × 10-4(11.5) |
| Human UGT1A7 | 8.52 × 10-4(4.62) | 2.73 × 10-4(12.4) |
| Human UGT1A8 | 0.0526 × 10-4(10.3) | 0.0940 × 10-4(4.11) |
| Human UGT1A9 | 0.427 × 10-4(4.13) | 0.121 × 10-4(3.51) |
| Human hepatic microsomes | 68.0 × 10-4(4.23) | 15.4 × 10-4(12.5) |
| Human intestinal microsomes | 9.54 × 10-4(3.51) | 2.73 × 10-4(11.1) |
| Rat UGT1A1 | 8.23 × 10-4(8.05) | 4.49 × 10-4(12.7) |
| Rat UGT1A7 | 81.2 × 10-4(10.0) | 23.6 × 10-4(20.1) |
| Rat UGT1A8 | 27.9 × 10-4(3.51) | 5.06 × 10-4(30.6) |