Pharmacokinetic parameters of CPFX, GPFX, OFX, and UFX after a single i.v. administration at a dose of 1 mg/kg
Data are taken from Fig. 3. Each value represents the mean ± S.E. of four mice.
CLtotala | CLbile, plasmab | Kplasma, liver c | Kplasma, kidney d | Kplasma, brain e | ||
|---|---|---|---|---|---|---|
| ml/min/kg | ||||||
| CPFX | ||||||
| Wild-type | 22.0 ± 1.2 | 3.65 ± 0.83 | 5.32 ± 0.14 | 5.79 ± 0.57 | 0.14 ± 0.01 | |
| Bcrp(−/−) | 31.2 ± 4.3 | 1.30 ± 0.11* | 6.19 ± 1.41 | 20.8 ± 2.1** | 0.32 ± 0.15 | |
| GPFX | ||||||
| Wild-type | 6.82 ± 0.02 | 0.61 ± 0.04 | 1.99 ± 0.18 | 3.19 ± 0.33 | 0.11 ± 0.01 | |
| Bcrp(−/−) | 7.63 ± 0.01 | 0.30 ± 0.02** | 2.10 ± 0.22 | 4.72 ± 0.20** | 0.13 ± 0.01 | |
| OFX | ||||||
| Wild-type | 28.1 ± 6.8 | 1.98 ± 0.51 | 3.03 ± 0.79 | 10.9 ± 6.4 | 0.26 ± 0.07 | |
| Bcrp(−/−) | 18.8 ± 1.7 | 0.76 ± 0.04 | 1.45 ± 0.15 | 8.02 ± 1.77 | 0.15 ± 0.02 | |
| UFX | ||||||
| Wild-type | 16.6 ± 4.6 | 3.07 ± 0.60 | 2.86 ± 0.56 | 15.7 ± 6.1 | N.D. | |
| Bcrp(−/−) | 21.2 ± 8.1 | 0.50 ± 0.09** | 4.21 ± 1.84 | 15.1 ± 7.2 | N.D. | |
N.D., not detected.
↵ a Total body clearance obtained by dividing the dose by the AUC0-∞.
↵ b Biliary clearance obtained by dividing the cumulative biliary excretion by the AUC0-120.
↵ c Plasma/liver concentration ratio at 120 min.
↵ d Plasma/kidney concentration ratio at 120 min.
↵ e Plasma/brain concentration ratio at 120 min.
↵* P < 0.05 versus control values.
↵** P < 0.01.