TABLE 2

Pharmacokinetic parameters of ATV and 2-hydroxy-ATV after single intravenous (1 mg/kg) or oral (5 mg/kg) administration of ATV to cynomolgus monkeys with and without oral administration of RIF (18 mg/kg)

Each value represents mean ± S.E. from four monkeys.

CompoundATV i.v.ATV PO
ControlRIF PORatioControlRIF PORatio
ATV
 CLtotal (l/h/kg)2.69 ± 0.391.66 ± 0.270.62
Vss(l/kg)2.16 ± 0.321.22 ± 0.310.56
 t1/2 (h)0.69 ± 0.070.93 ± 0.091.344.43 ± 1.265.07 ± 1.031.14
 AUC0–last (h⋅µM)0.71 ± 0.111.17 ± 0.201.650.42 ± 0.070.61 ± 0.211.45
 AUCinf (h⋅µM)0.71 ± 0.111.18 ± 0.201.650.45 ± 0.070.76 ± 0.251.67
 Cmax (µM)0.30 ± 0.080.37 ± 0.161.24
 Tmax (h)1.00 ± 0.002.63 ± 1.602.63
2-hydroxy-ATV
 t1/2 (h)0.70 ± 0.051.88 ± 0.24a2.7020.78 ± 10.225.16 ± 1.720.25
 AUC0–last (h⋅µM)0.39 ± 0.031.18 ± 0.26a3.050.24 ± 0.051.80 ± 0.18a7.64
 AUCinf (h⋅µM)0.41 ± 0.031.25 ± 0.273.050.38 ± 0.061.90 ± 0.26a4.97
 Cmax (µM)0.21 ± 0.040.72 ± 0.13a3.410.02 ± 0.000.39 ± 0.07a19.53
 Tmax (h)3.00 ± 0.000.63 ± 0.22a0.214.50 ± 1.502.50 ± 1.500.56
  • a Significantly different from control group (P < 0.05).