TABLE 3

Pharmacokinetic parameters of MB07811 after i.v. and p.o. administration of 3 and 10 mg/kg, respectively, to rats, dogs, and monkeys

Values are expressed as mean ± S.D.

Analyte
Parameter
Unit
Rat (n = 5)
Dog (n = 6)
Monkey (n = 4)
i.v.
p.o.
i.v.
p.o.
i.v.
p.o.
MB07811 AUClast mg · h/l 0.26 ± 0.04 0.026 ± 0.011 2.53 ± 0.88 0.066 ± 0.033 3.01 ± 0.41 0.085 ± 0.017
C max μg/ml 0.60 ± 0.22 0.012 ± 0.008 2.09 ± 0.98 0.015 ± 0.008 7.32 ± 3.61 0.018 ± 0.009
T max h 0.0 ± 0.0 2.1 ± 1.0 0.0 ± 0.0 4.0 ± 6.0 0.0 ± 0.0 1.5 ± 0.6
t 1/2 h 1.23 ± 0.15 0.95 ± 0.35 4.4 ± 3.8 5.0 ± 2.6 4.07 ± 0.73 4.32 ± 1.99
CL l/h/kg 11.55 ± 1.93 N.A. 1.27 ± 0.39 N.A. 1.00 ± 0.12 N.A.
V ss l/kg 14.82 ± 3.99 N.A. 3.38 ± 1.20 N.A. 2.76 ± 0.81 N.A.
MRT h 1.20 ± 0.20 2.49 ± 0.72 2.3 ± 0.8 6.5 ± 3.7 2.77 ± 0.74 6.89 ± 2.86
F (absolute) % N.A. 5-10 N.A. 2.8 ± 1.7 N.A. 2.8 ± 0.6
MB07344 AUClast mg · h/l 0.34 ± 0.06 0.135 ± 0.035 0.16 ± 0.06 0.42 ± 0.16 4.60 ± 1.64 1.45 ± 0.64
C max μg/ml 0.092 ± 0.017 0.018 ± 0.003 0.014 ± 0.006 0.056 ± 0.031 0.63 ± 0.19 0.18 ± 0.12
T max h 0.60 ± 0.15 3.6 ± 1.1 17.6 ± 9.2 5.7 ± 5.3 0.88 ± 0.25 3.00 ± 1.15
t 1/2 h 8.82 ± 2.38 9.25 ± 6.24 N.D. 10.2 ± 4.2 5.70 ± 1.23 6.52 ± 1.45
F (relative)
%
N.A.
20-39
N.A.
∼50†
N.A.
31.8 ± 11.5

  • N.A., not applicable; N.D., not determined.

  • ↵† Based on AUC to infinity.