TABLE 7

Pharmacokinetic parameters for ELN441958 in the rat and rhesus monkey

See Materials and Methods for description of the assays. Values are presented as means ± S.E.M. from a single study (rat, n = 3; rhesus, n = 3).


Parameter

Rat

Rhesus
i.v. dose (mg/kg) 2.5 1
i.v. t1/2 (h) 2.0 ± 0.8 3.9 ± 0.3
i.v. AUCo-t (μg · h/ml) 2.6 ± 0.3 2.1 ± 0.3
i.v. Vz (l/kg) 2.7 ± 0.7 2.7 ± 0.4
i.v. clearance (l/h/kg) 0.96 ± 0.12 0.49 ± 0.06
Oral dose (mg/kg) 10 5
Oral Cmax (μg/ml) 1.3 ± 0.5 4.0 ± 0.1
Oral Tmax (h) 1.7 ± 0.6 3.3 ± 0.7
Oral AUCo-t (μg · h/ml) 6.0 ± 1.4 14 ± 0
Oral bioavailability (%) 57 ∼100a
s.c. dose (mg/kg) 10
s.c. Cmax (μg/ml) 5.6 ± 1.8
s.c. Tmax (h) 2.2 ± 1.0
s.c. AUCo-t, (μg · h/ml) 27 ± 6
s.c. bioavailability (%)

∼100a
  • a The oral and s.c. bioavailability of ELN441958 exceeded the maximum possible (100%), and they were calculated to be 138 ± 17 and 137 ± 40%, respectively.