Mean pharmacokinetic parameters of brivanib and its enantiomer in rats, monkeys, and humans after oral doses of brivanib alaninate
| Species | Dose | Analytea | Cmax | Tmax | AUC0-t | AUC% of the Enantiomeric Metabolite Relative to Brivanib |
|---|---|---|---|---|---|---|
| μg/ml | h | μg · h/ml | ||||
| Rat | 60 mg/kg | Brivanib | 3.5 | 1 | 7.6 | 94.7 |
| Enantiomeric metabolite | 2.6 | 2 | 7.2 | |||
| Monkey | 10 mg/kg | Brivanib | 1.4 | 1 | 6.8 | 39.7 |
| Enantiomeric metabolite | 0.5 | 4 | 2.7 | |||
| Human | 400 mg | Brivanib | 3.5 | 2 | 21.8 | 1.6 |
| Enantiomeric metabolite | 0.05 | 5 | 0.4 |
↵a The concentration of brivanib and the enantiomeric metabolite were determined with a chiral LC/MS method.