Mean pharmacokinetic parameters of brivanib and plasma TRA in rats, monkeys, and humans after oral administration of [14C]brivanib alaninate
| Species | Dose | Analytea | Cmax | Tmax | AUC0–t | AUC % of Brivanib to TRA |
|---|---|---|---|---|---|---|
| μg/ml | h | μg · h/ml | ||||
| Rat | 100 mg/kg | Brivanib | 6.4 ± 0.2 | 1 | 35.5 ± 3.6 | 14.2 |
| TRA | 35.2 ± 10.4 | 2 | 250 ± 9 | |||
| Monkey | 10 mg/kg | Brivanib | 6.2 ± 0.2 | 2 | 49.0 ± 4.5 | 54.3 |
| TRA | 9.7 ± 0.6 | 2 | 90.3 ± 13.7 | |||
| Humanb | 800 mg | Brivanib | 6.1 ± 0.9 | 1 | 45.9 ± 4.1 | 22.5 |
| TRA | 9.4 ± 1.8 | 1 | 203.8 ± 40.8 |
↵a The concentration of brivanib was determined with an achiral LC-MS/MS method. TRA in rat and monkey plasma was determined by LSC. TRA in human plasma was determined by accelerator mass spectrometry (Mekhail et al., 2010).
↵b The pharmacokinetic parameters of brivanib and plasma TRA in humans were reported in a separate article and are included here for comparison (Mekhail et al., 2010).