TABLE 3

Pharmacokinetics of ILT-threo and ILT-allo in rat, monkey or dog plasma following a single intravenous administration at 1, 5, or 10 mg/kg Values represent mean ± standard deviation when n = 3 and mean when n = 2.



ILT-threo

ILT-allo

1 mg/kg
5 mg/kg
10 mg/kg
1 mg/kg
5 mg/kg
10 mg/kg
Rats (n = 3)
nAUC(0-inf) (ng · h/ml) 612 (57) 826 (184) 988 (139) 614 (152) 743 (6) 682 (86)
Vdss (l/kg) 5.0 (0.6) 3.8 (0.6) 3.0 (1.6) 3.1 (0.7) 3.2 (0.8) 4.1 (0.2)
CLp (ml/min/kg) 27 (2) 21 (4) 17 (2) 28 (6) 23 (0) 25 (3)
t1/2 (h) 1.8 (0.8) 3.1 (0.1) 2.7 (0.2) 1.8 (0.2) 2.0 (0.3) 2.8 (0.5)
Dogs (n = 3)
nAUC(0-inf) (ng · h/ml) 507 (31) 605 (11) 687 (78) 591 (89) 479 (39) 810 (113)
Vdss (l/kg) 2.2 (1.4) 2.3 (0.6) 2.0 (0.2) 2.4 (1.1) 2.6 (0.3) 1.5 (0.2)
CLp (ml/min/kg) 33 (2) 28 (0.5) 25 (3) 29 (5) 35 (3) 21 (3)
t1/2 (h) 1.4 (0.5) 2.1 (0.4) 3.6 (0.6) 1.0 (0.2) 2.2 (0.2) 2.5 (0.7)
Monkeys (n = 2 or 3)
nAUC(0-inf) (ng · h/ml) 2033 1956 (151) 2185 2755 (719) 3018 2929
Vdss (l/kg) 1 1.3 (0.1) 0.9 0.9 (0.2) 0.9 0.8
CLp (ml/min/kg) 8 9 (1) 8 6 (1) 6 6
t1/2 (h)
1.6
2.4 (0.2)
2.5
1.6 (0.3)
2.9
2.7
  • a Clp, plasma clearance; Vdss, volume of distribution at steady state; t1/2, terminal half-life; nAUC(0-inf), dose normalized area under the plasma concentration versus time profile