In vitro and in vivo protein covalent binding of [14C] BMS-204352
Species | Protein Covalent Binding | ||||
|---|---|---|---|---|---|
| In Liver Microsomal Incubationsa | In Plasma following i.v. Dosesb | In Liver Homogenate following i.v. Dosesb | |||
| pmol/mg protein | |||||
| Human | 1215.8 ± 271.8 | 16.5 ± 7.2 (at24h) | N.D. | ||
| Dog | 302.0 ± 25.2 | 55.3 ± 10.5(at24h) | N.D. | ||
| Rat | 703.6 ± 110.3 | 447.3 ± 33.5(at 4h) | 633.4 ± 45.2 (at4h) | ||
N.D., not determined.
↵ a Incubations were for 30 min at 37°C in 1 mg/ml microsomal proteins at 25 μM [14C] BMS-204352. Protein covalent binding was normalized to pmol/mg · h.
↵ b Dogs and rats were i.v. dosed with 6 and 2 mg/kg, respectively, and human subjects were i.v. dosed with 10 mg of [14C] BMS-204352 (5 μCi/mg).