Pharmacokinetic parameters of YM796 in rats, dogs and humans
| i.v. administration | Dose | AUCiv | CLtot | t 1/2 | ||
| Species | n | (mg/kg) | (ng · hr/ml) | (ml/min/kg) | (hr) | |
| Rat | 3 | 0.3 | 44.7 | 112 | 0.36 | |
| Dog | 3 | 0.1 | 54.5 (5.6) | 31.2 (3.3) | 0.89 (0.19) | |
| Oral administration | Dose | AUCoral | CLoral | Cmax | F | |
| Species | n | (mg/kg) | (ng · hr/ml) | (ml/min/kg) | (ng/ml) | (%) |
| Rat | 3 | 1.0 | 5.0 | 3330 | 9.3 | 3.4 |
| Dog | 3 | 1.0 | 87.7 (17.0) | 205 (39) | 39.3 (7.1) | 16.1 (2.5) |
| Human1-a | 6 | 5.01-b | 117 (16) | 11.1 (1.3) | 19.8 (2.1) | |
| Other parameters | ||||||
| Species | n | fp 1-c | RB 1-c | |||
| Rat | 3 | 0.694 (0.013) | 1.10 (0.08) | |||
| Dog | 3 | 0.707 (0.006) | 1.07 (0.05) | |||
| Human1-a | 3 | 0.700 (0.013) | 1.11 (0.07) | |||
Numbers in parentheses represent the S.E. of the mean values.
↵1-a The human data were taken from Iwatsubo et al., 1997b.
↵1-b The dose was given as mg/body for humans different from rats and dogs.
↵1-c Both fp and RB were almost constant irrespective of YM796 concentrations ranging from 0.5 to 2500 μM in all species examined.