TABLE 6

Mean (S.D.) pharmacokinetic parameters of TG100435 and TG100855 following 25 mg/kg p.o. administration in mice and rats


Species

Compound

Cmax

tmax

AUC0-∞

AUC0-last

F
ng/ml h ng · h/ml %
Mouse TG100435 618 8 15,300 15,000 74
TG100855 171 1 939 912 3.5
TG100435a 113 7 1760 1740 6.8b
Rat TG100435 348 (82) 8 8010 (3850) /980 (3810) 23
TG100855 160 (85) 3.5 (1.9) 470 (145) 467 (150) 1.6

TG100435a
73.0 (31.8)
4.0 (2.0)
906 (437)
881 (431)
3.1b
  • a TG100435 converted from TG100855 after dosed with TG100855.

  • b Oral bioavailability from the converted TG100435.