Table 2.
Pharmacokinetic parameters of SB5794 and SB2617 in BALB/c mice (single-dose TK study)a,b
| PK parameters | SB5794 (p.o.) | SB2617 (p.o.) | ||||
|---|---|---|---|---|---|---|
| 100 mg/kg | 300 mg/kg | 1000 mg/kg | 100 mg/kg | 300 mg/kg | ||
| Terminal t1/2 (h) | - | - | - | 29.70 | 31.5 | |
| Tmax (h)c | 11.3 | 17.3 | 26.0 | 7.3 | 14.7 | |
| Cmax (ng/mL) | 12600 | 23733 | 51500 | 1502 | 2659 | |
| AUC0-24 (ng·h/mL) | 261982 | 509222 | 1100298 | 32107 | 57542 | |
| AUC0-last (ng·h/mL) | 325175 | 641778 | 1396410 | - | - | |
| AUC vs SB2617 10 mg/kg | 15.0 | 29.2 | 63.2 | 1.8 | 3.4 | |
ᵃMice (n=3 per group) received SB5794 (100, 300, or 1000 mg/kg) or SB2617 (100 or 300 mg/kg) orally. ᵇSB5794 demonstrated significantly improved Cmax and AUC compared with SB2617. ᶜTmax is given as median.