TABLE 3

Pharmacokinetic parameters of pitavastatin (0.3 mg/kg) after single intravenous and oral administration to male cynomolgus monkeys in combination with CsA and RIF

Each value represents the mean ± S.D. of four monkeys. CsA or RIF was administered 4 hours and 1 hour before intravenous and oral administration of pitavastatin, respectively. AUC′, CLtotal′, and FH′ refer to the parameters in the presence of a perpetrator.

ControlCsA, p.o.RIF, p.o.
Pitavastatin, i.v.Pitavastatin, p.o.Pitavastatin, i.v.Pitavastatin, p.o.Pitavastatin, i.v.Pitavastatin, p.o.
CLtotal (ml/h/kg)756 ± 156258 ± 104b249 ± 109b
Vss (ml/kg)607 ± 169388 ± 179431 ± 181
t1/2 (h)3.4 ± 0.62.5 ± 0.62.4 ± 0.83.2 ± 1.32.7 ± 0.94.5 ± 1.2a
Cmax (ng/ml)15.0 ± 19.7135 ± 113b314 ± 456c
Tmax (h)2.3 ± 1.34.0 ± 1.61.9 ± 1.5
AUC (ng·h/ml)412 ± 4872 ± 701394 ± 776b725 ± 651c1578 ± 1151b1089 ± 1129c
FH0.62 ± 0.080.87 ± 0.05b0.88 ± 0.05b
AUCpo′/AUCpo10.6 ± 1.414.8 ± 2.4
CLtotal/CLtotal3.2 ± 0.93.6 ± 1.6
FH′/FH1.4 ± 0.11.4 ± 0.1
(FH′/FH)·(CLtotal/CLtotal′)4.5 ± 1.15.0 ± 2.0
  • a P < 0.05, compared with the control values obtained before CsA or RIF treatment.

  • b P < 0.01.

  • c P < 0.001.