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. 2017 May 22;60(12):5072–5085. doi: 10.1021/acs.jmedchem.7b00410

Table 6. Rat and Cynomolgus Monkey Pharmacokinetics of Compounds 27 and 28a.

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  rat IV PKb
rat oral PKb
no. t1/2 (min)c MRT (min)c Clp (mL/min/kg)c VSS (L/kg)c Tmax (min)d Cmax (μM)d AUC (μM·h)d Fd
27 390 93 19.3 1.8 30 4.34 14.6 53
28 281 208 9.2 1.9 90 3.33 38.0 71
  cynomolgus monkey IV PKe
cynomolgus monkey oral PKe
no. t1/2 (min)c MRT (min)c Clp (mL/min/kg)c VSS (L/kg)c Tmax (min)d Cmax (μM)d AUC (μM·h)d Fd
27 302 163 15.5 2.5 180 1.72 7.32 44
28 563 303 13.3 4.0 120 1.36 6.43 35
a

Oral vehicle = 10% polysorbate 80 in 0.5% methyl cellulose; IV vehicle = 10% EtOH, 70% PEG 400, 20% saline.

b

Average n = 2 male Sprague–Dawley rats.

c

t1/2 = Terminal phase plasma half-life; MRT = mean residence time; Clp = plasma clearance; VSS = volume of distribution at steady-state.

d

Tmax = time at which maximum concentration occurs; Cmax = maximum concentration; AUC = area under the curve; F = bioavailability.

e

Average n = 2 male cynomolgus monkeys.