Table 2

Pharmacokinetic variables of tezosentan after i.v. dosing in different species

SpeciesDoseCmaxSystemic Plasma ClearanceVssApparent Elimination Half-life
mg/kg μg/ml ml/min/kg liters/kg h
Rat (n = 4)1094.3  ± 10.34.3  ± 0.10.27  ± 0.022.1  ± 0.2
Rabbit (n = 3)511.4  ± 3.734.3  ± 9.10.44  ± 0.180.4  ± 0.1
Cynomolgus monkey (n = 2)1039.6–69.111.9–19.30.14–0.270.8–0.8
Rhesus monkey (n = 2)1063.4–82.810.0–13.20.10–0.110.5–0.6

Cmax corresponds to the plasma concentration at 5 min postdosing; Vss, volume of distribution at steady state. Values are mean ± S.D. of three to five animals. In monkeys where only two animals were used, individual values are given.