Species | Rodent: single dose in solution | ||||||||||
Rat | Mouse | Human | |||||||||
Dose | (mg/kg) | 1 | 10 | 1 | 10 | 10 mg | Human: BID | ||||
AUC inf | (uM hr) | 0.6 | 11.4 | 1.2 | 18.2 | More than dose prop exposures | |||||
C max | (uM) | 0.1 | 3.7 | 0.5 | 7.6 | 0.47 | in oral t1/2 suggest change in clearance mechanisms | ||||
C min | (uM) | 0.03 | 0.01 | 0.3 | |||||||
C max/ C min ratio | 123 | 760 | 1.54 | Much lower Cmax/Cmin ratio in human | |||||||
T max | (hr) | 1 | 0.5 - 1 | 0.5 | 0.5 - 1 | 4 - 6 | |||||
1 mg/kg (iv) | 1 mg/kg (iv) | ||||||||||
Vd ss | (L/kg) | 8 - 9 | 8 - 9 | 9 - 11 | |||||||
Cl p | (L/hr/kg) | 4.15 | 3.81 | 0.16 | Much lower (estimated) clearance in human. Renal elimination in all species | ||||||
GFR | (L/hr/kg) | 0.31 | 0.84 | 0.11 | Clp >> GFR suggests active elimination | ||||||
t 1/2 | (hr) | 4 | 3 | 60 - 80 |