Pharmacokinetic parameters of CS-1036 after a single oral administration of CS-1036 to rats and monkeys
Values are expressed as mean ± S.D. (n = 3 or 4), and a dash denotes not applicable.
| Species | Dose | AUClast | AUC0-inf | tmax | Cmax | t1/2 | Foral (%) |
|---|---|---|---|---|---|---|---|
| mg/kg | ng·h/ml | ng·h/ml | h | ng/ml | h | ||
| Rat | 0.3 | 42.1 ± 13.1 | 45.6 ± 17.2 | 0.500 ± 0.354 | 16.2 ± 2.4 | 2.69 ± 2.55 | 2.44 |
| 1 | 110 ± 26 | 115 ± 30 | 0.417 ± 0.144 | 45.5 ± 5.5 | 1.81 ± 0.31 | 2.33 | |
| 3 | 324 ± 25 | 325 ± 29 | 0.375 ± 0.144 | 113 ± 15 | 4.16 ± 1.94 | 1.73 | |
| 10 | 1050 ± 140 | 1080 ± 150 | 0.438 ± 0.375 | 285 ± 75 | 18.3 ± 6.7 | 2.03 | |
| Monkey | 0.3 | 15.0 ± 4.2 | — | 1.75 ± 0.50 | 5.23 ± 1.24 | — | — |
| 1 | 52.0 ± 11.4 | 57.9 ± 8.2 | 1.75 ± 0.50 | 15.3 ± 4.2 | 1.29 ± 0.19 | 0.983 | |
| 3 | 186 ± 67 | 191 ± 71 | 1.75 ± 0.50 | 44.8 ± 11.0 | 2.12 ± 0.47 | 1.05 | |
| 10 | 869 ± 300 | 894 ± 305 | 1.75 ± 0.50 | 152 ± 77 | 12.6 ± 5.0 | 1.20 |