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