TABLE 4

Pharmacokinetic parameters of radioactivity after i.v. administration of [14C]S-8921G in wild-type and Bcrp–/– mice The pharmacokinetic parameters were calculated by WinNonlin using the plasma concentrations shown in Fig. 6. Data represent the mean ± S.D. of three mice.


PK Parameters

Wild-Type Mice

Bcrp–/– Mice
AUC0→120m (μg · min/ml) 113 ± 23 75.0 ± 24.1
CLtot, p (ml/min/kg) 9.10 ± 1.72 14.5 ± 4.8
fe, bile (% of dose) 92.0 ± 6.4 93.9 ± 2.6
CLbile, p (ml/min/kg)
8.44 ± 2.10
13.6 ± 4.5
  • AUC0→120m, the area under the plasma concentration-time curve from 0 to 120 min after dosing; fe, bile, the fraction of cumulative biliary excretion of radioactivity within 120 min of dosing; CLtot, p, the total body clearance based on the plasma concentration obtained by dividing dose (1 mg/kg) by AUC0→120m; CLbile, p, the biliary clearance obtained by dividing the amount excreted in the bile (fe, bile multiplied by dose) by AUC0→120m