Pharmacokinetic parameters for MTIP, CP154526, SSR125543A, and R121919
| Compound/route/dose | ||||||||
|---|---|---|---|---|---|---|---|---|
| MTIP | CP154526 | SSR125543A | R121919 | |||||
| i.v. | p.o. | i.v. | p.o. | i.v. | p.o. | i.v. | p.o. | |
| 1 mg/kg | 10 mg/kg | 3 mg/kg | 10 mg/kg | 3 mg/kg | 10 mg/kg | 3 mg/kg | 10 mg/kg | |
| AUC0– t (ng · h/ml) | 3407 ± 277 | 27,035 ± 3848 | 568 ± 12 | 355 ± 44 | 11,634 ± 2948 | 9116 ± 1892 | 154 ± 1 | 378 ± 25 |
| AUC0–∞ h (ng · h/ml) | 3435 ± 275 | 31,290 (2) | 605 ± 16 | 369 ± 39 | 12,370 ± 3160 | 10,118 (2) | 164 ± 4 | 381 ± 26 |
| t ½ (h) | 3.9 ± 0.3 | 3.3 (2) | 15.1 ± 2.7 | 8.2 ± 1.4 | 10.53 ± 1.84 | 5.88 (2) | 2.8 ± 0.2 | 1.52 ± 0.07 |
| C max (ng/ml) | 2773 ± 148 | 66.5 ± 3.9 | 1603 ± 387 | 77.8 ± 11.1 | ||||
| C 0 (ng/ml) | 4714 ± 1952 | 1274 ± 104 | 25,744 ± 8468 | 261 ± 11 | ||||
| t max (h) | 2.2 ± 1.0 | 4 ± 0 | 4.7 ± 1.8 | 2 ± 0 | ||||
| Clearance (ml · min−1 · kg−1) | 4.9 ± 0.4 | 82.7 ± 2.1 | 4.6 ± 1.1 | 306 ± 7 | ||||
| V d, β (L/kg) | 1.7 ± 0.2 | 114 ± 16 | 4.2 ± 0.8 | 75.7 ± 7.2 | ||||
| % Oral bioavailability | 91.1 | 18.3 | 24.5 | 69.7 | ||||
n = 3, except where indicated otherwise in parentheses.