Compound | fm, UGTa | ||||
---|---|---|---|---|---|
Mouse | Rat | Monkey | Dog | Humanb | |
Ketoprofen | 0.010 | 0.853 | 0.350 | 0.163 | 0.900 |
Imipramine | ND | 0.014 | 0.040 | 0.005 | 0.100 |
Lorazepam | 0.436 | 0.085 | 0.530 | 0.785 | 0.810 |
Levofloxacin | 0.229 | 0.644 | 0.820 | 0.061 | <0.015 |
Zidovudine | 0.034 | 0.020 | 0.080 | 0.134 | 0.850 |
Diclofenac | 0.261 | 0.065 | 0.290 | 0.522 | 0.150 |
Furosemide | 0.005 | 0.052 | 0.671 | 0.170 | 0.140 |
Raloxifene | 0.243 | 0.214 | 0.380 | 0.196 | 0.900 |
Gemfibrozil | 0.173 | 0.366 | 0.350 | 0.690 | 0.400 |
Mycophenolic acid | 0.966 | 0.096 | 0.540 | 0.990 | 0.900 |
Indomethacin | 0.001 | 0.004 | 0.940 | 0.010 | 0.217 |
Telmisartan | 0.118 | 0.396 | 0.470 | 0.990 | NA |
Percentage of compounds within | |||||
2-fold | 30 | 20 | 40 | 40 | |
3-fold | 40 | 40 | 70 | 40 | |
4-fold | 60 | 40 | 70 | 50 |
NA, not available; ND, not detected.
↵a Preclinical fm,UGT values were derived from the recovery of glucuronide excreted in bile and urine (n = 2–3).
↵b Clinical fm,UGT values were obtained from the literature as follows: ketoprofen, zidovudine, and gemfibrozil (Kilford et al., 2009); imipramine and furosemide (Soars et al., 2002); lorazepam (Greenblatt, 1981); levofloxacin (Fish and Chow, 1997); diclofenac (Stierlin et al., 1979); raloxifene and mycophenolic acid (Cubitt et al., 2009); and indomethacin (Duggan et al., 1972).