Species | Dose, Route | Cmax | Tmax a | AUCINFb | Terminal Plasma t1/2 | MRT | CLT | Vdss | F | ||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Brasofensine | BMS-205912 | Brasofensine | BMS-205912 | ||||||||||
ng/ml | ng/ml | h | ng · h/ml | ng · h/ml | h | h | ml/min/kg | l/kg | % | ||||
Ratc | 1.5 mg/kg, i.v. | 125 | 1.04 | 3.5 | 2.1 | 199 | 24 | ||||||
4 mg/kg, p.o. | 10.5 | 0.57 | 1 | 24.9 | 1.16 | 1.7 | 2.5 | 7.4 | |||||
Monkey | 4 mg, i.v. | 507 (367) | 20.4 (19.3) | N.A.d | N.A.e | 32 (17) | 46 (5) | ||||||
12 mg, p.o. | 3.3 (4.1) | N.D | 1 | 9.0 (8.4) | N.D | 3.9 (2.2) | 5.4 (0.7) | 0.8 | |||||
Human | 50 mg, p.o. | 1.2 (0.5) | 0.31 (0.11) | 7 | 39.0 (28.5) | 35.5 (21.4) | 24 (13)g | 39 (23)h |
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↵ a Median
↵ b AUC for monkey is AUC0-T, where T is the last measurable sampling time
↵ c Pharmacokinetic parameters derived from a composite profile
↵ d The terminal slope could not be determined
↵ e AUCINF could not be determined
↵ f No detectable concentrations
↵ g Terminal plasma t1/2 for BMS-205912 was 55 (37) h
↵ h MRT for BMS-205912 was 96 (43) h