Apparent kinetic parameters of raloxifene glucuronidation to M1 and M2 in human liver microsomes genotyped for UGT1A1*28 polymorphism and calculated microsomal intrinsic and tissue intrinsic clearances
Data are presented as mean (S.E.).
| Vmax | Km | Ksi | Clint | Clint,o | |
|---|---|---|---|---|---|
| nmol · min−1 · mg−1 | μM | μl · min−1 · mg−1 | ml · min−1 · kg−1 | ||
| M1 | |||||
| UGT1A1 *1/*1 | 8.72 (0.07) | 149.4 (0.14) | n.d. | 58.4 (0.16) | 52.5 (0.16) |
| UGT1A1 *1/*28 | 3.40 (0.10) | 130.2 (0.19) | n.d. | 26.1 (0.22) | 23.5 (0.22) |
| UGT1A1 *28/*28 | 1.98 (0.07) | 150.0 (0.13) | n.d. | 13.2 (0.14) | 11.9 (0.14) |
| M2 | |||||
| UGT1A1 *1/*1 | 9.86 (0.31) | 158.7 (0.35) | 493.1 (0.98) | 62.1 (0.47) | 55.9 (0.47) |
| UGT1A1 *1/*28 | 10.7 (0.38) | 181.2 (0.49) | 146.5 (0.86) | 58.9 (0.62) | 53.0 (0.62) |
| UGT1A1 *28/*28 | 1.85 (0.27) | 161.0 (0.41) | 541 (0.81) | 11.5 (0.49) | 10.4 (0.49) |
n.d., not determined.