TABLE 2

Pharmacokinetics of PF-8380 in rat

ParameterUnitsIntravenous 1 mg/kg (n = 2)Oral 1 mg/kg (n = 5)Oral 3 mg/kg (n = 3)Oral 10 mg/kg (n = 3)Oral 30 mg/kg (n = 3)Oral 100 mg/kg (n = 3)
Dosemg/kg1131030100
AUCμM·h1.120.480 ± 0.1202.25 ± 0.549.22 ± 2.7520.6 ± 6.256.6 ± 11.0
Clearanceml/min/kg31
Vdssl/kg3.2
CmaxμM0.124 ± 0.0250.922 ± 0.1202.55 ± 0.754.23 ± 0.506.19 ± 1.06
Tmaxh0.60 ± 0.220.50 ± 0.00.67 ± 0.290.42 ± 0.143.3 ± 1.2
Effective t1/2h1.2
Terminal t1/2h1.72.1 ± 0.71.5 ± 0.22.2 ± 0.52.8 ± 0.34.3 ± 1.2
Bioavailability%43 ± 968 ± 1683 ± 2562 ± 1952 ± 10