TABLE 1

Pharmacokinetic parameters of PF-04971729 in rats and dogs after a single intravenous or oral dose

Data are mean ± S.D. For studies involving n = 2, pharmacokinetic parameters for the two individual animals are shown in the parentheses.

Species (strain)Gender/No.DoseaRouteCmaxTmaxCLpVdssAUC(0–∞)t1/2F
mg/kgng/mlhml · min1 · kg1l/kgng · h/mlh%
Rat (Sprague-Dawley)M/22.0i.v.N.A.N.A.4.04 (3.39, 4.68)1.13 (1.18, 1.08)8480 (9830, 7040)4.08 (4.85, 3.31)N.A.
M/35.0p.o.1940 ± 1851.0 ± 0.0N.A.N.A.14,700 ± 4320bN.A.69
Dog (beagle)M/22.0i.v.N.A.N.A.1.64 (1.72, 1.56)0.83 (0.81, 0.84)20,400 (19,400, 21,400)7.63 (7.42, 7.84)N.A.
M/32.0p.o.2500 ± 2150.83 ± 0.29N.A.N.A.19,100 ± 365b7.48 ± 0.1394
  • M, male; N.A., not applicable.

  • a The dosing vehicle used in intravenous and oral dosing to rats was DMSO-polyethylene glycol 400–30% sulfobutylether-β-cyclodextrin (10:30:60, v/v/v) and 0.5% (w/v) methyl cellulose with 10% (v/v) polyethylene glycol 400. The dosing vehicle used in intravenous and oral dosing to dogs was 5% polyethylene glycol 400 in 23% hydroxypropyl-β-cyclodextrin and 0.5% methyl cellulose (w/v) with 10% (v/v) polyethylene glycol 400, respectively.

  • b AUC(0–24 h).