Pharmacokinetic parameters of L-694,458 in orally dosed rats and rhesus monkeys
| Dose (mg/kg) | Form | AUC (μg/hr/ml) | Cmax(μg/ml) | tmax(hr) | t1/2 (hr) |
|---|---|---|---|---|---|
| Rats (N = 4) | |||||
| 10 | Malate | 4.16 ± 1.42 | 0.74 ± 0.22 | 2.3 ± 1.3 | 2.2 ± 0.3 |
| 10 | Free base | 4.22 ± 0.93 | 0.82 ± 0.10 | 1.5 ± 0.6 | 2.7 ± 0.1 |
| 40 | Free base | 38.07 ± 4.87 | 3.39 ± 0.25 | 2.3 ± 1.3 | 4.3 ± 0.1 |
| Rhesus monkeys (N = 1–6) | |||||
| 10 | Malate | 1.60 ± 1.09 | 0.21 ± 0.14 | 3.0 ± 1.5 | 3.9 ± 0.8 |
| 30 | Free base | 8.81 | 0.39 | 24 | 6.3 |
| 40 | Malate | 19.26 ± 6.18 | 0.97 ± 0.25 | 19 ± 9 | n.d. |
| 40 | Free base | 12.88 | 0.60 | 24 | 6.0 |
n.d. = Not determined. Drug concentrations were still increasing at 24 hr, the last sampling time in this study. AUC extrapolations were performed using the terminal half-life obtained when the animals were dosed with the free base.