Biliary and renal CL of BCRP substrates in bile duct-catheterized rats after intravenous administration
Values are mean ± S.D. for n = 3; individual value is reported for n = 2.
| Compound | Dose | Abcg2(+/+) | Abcg2(−/−) | ||||
|---|---|---|---|---|---|---|---|
| Biliary CL | Dose as Parent in Urine | Renal CL | Biliary CL | Dose as Parent in Urine | Renal CL | ||
| mg/kg | l/h/kg | % | l/h/kg | % | l/h/kg | ||
| Nitrofurantoin | 5 | 0.04, 0.05 | 19.7, 16.7 | 0.42, 0.63 | 0.002 ± 0.000 | 27.6 ± 16.2 | 0.45 ± 0.33 |
| Sulfasalazine | 1 | 0.75, 0.40 | 1.5, 2.4 | 0.022, 0.023 | 0.04, 0.03 | 0.3, <0.1 | 0.001, <0.001 |
| Compound A | 1 | 0.89 ± 0.65 | N.D. | N.D. | 0.09 ± 0.06** | N.D. | N.D. |
| Compound A | 5 | 0.23 ± 0.17 | <0.1 | <0.001 | 0.07 ± 0.01** | <0.1 | <0.001 |
Biliary CL, CL × [percentage of the dose excreted into bile as parent]; Renal CL, CL × [percentage of the dose excreted into urine as parent]; N.D., not determined.
↵** p < 0.01, unpaired t test between Abcg2(+/+) and Abcg2(−/−) rats, one-tailed.