Parameter | Rat | Rhesus |
---|---|---|
i.v. dose (mg/kg) | 2.5 | 1 |
i.v. t1/2 (h) | 2.0 ± 0.8 | 3.9 ± 0.3 |
i.v. AUCo-t (μg · h/ml) | 2.6 ± 0.3 | 2.1 ± 0.3 |
i.v. Vz (l/kg) | 2.7 ± 0.7 | 2.7 ± 0.4 |
i.v. clearance (l/h/kg) | 0.96 ± 0.12 | 0.49 ± 0.06 |
Oral dose (mg/kg) | 10 | 5 |
Oral Cmax (μg/ml) | 1.3 ± 0.5 | 4.0 ± 0.1 |
Oral Tmax (h) | 1.7 ± 0.6 | 3.3 ± 0.7 |
Oral AUCo-t (μg · h/ml) | 6.0 ± 1.4 | 14 ± 0 |
Oral bioavailability (%) | 57 | ∼100a |
s.c. dose (mg/kg) | 10 | |
s.c. Cmax (μg/ml) | 5.6 ± 1.8 | |
s.c. Tmax (h) | 2.2 ± 1.0 | |
s.c. AUCo-t, (μg · h/ml) | 27 ± 6 | |
s.c. bioavailability (%) |
| ∼100a |
↵ a The oral and s.c. bioavailability of ELN441958 exceeded the maximum possible (100%), and they were calculated to be 138 ± 17 and 137 ± 40%, respectively.