TABLE 5

Mean (S.D.) pharmacokinetic parameters of TG100435 and TG100855 following 5 mg/kg i.v. and i.p. dosing in mice and rats


Species

Route

Compound

C0

AUC(0-∞)

t½

Vd

CL

AUC0-∞a
ng/ml ng · h/ml h l/kg ml/min/kg ng · h/ml
Mouse i.v. TG100435 873 4140 5.4 9.4 20.1
i.v. TG100855 9030 5350 0.9 1.2 15.6 1390
i.p. TG100855 4100 6520 2.8 2.6 11.6 1400
Rat i.v. TG100435 1650 (840) 7030 (2170) 8.9 (1.9) 9.4 (1.7) 12.7 (3.5)
i.v. TG100855 12,200 (3980) 6050 (386) 1.6 (0.2) 1.9 (0.4) 13.8 (0.9) 539 (171)

i.p.
TG100855
1080 (806)
4990 (577)
2.3 (1.4)
3.3 (2.3)
17.0 (2.0)
498 (62)
  • a AUC of TG100435 converted from TG100855 after dosing with TG100855.