Pharmacokinetic parameters of MRK-016 in rat, dog, and rhesus monkey
| Parameter | Rat | Dog | Rhesus Monkey | |||
|---|---|---|---|---|---|---|
| i.v. dosing | ||||||
| Dose, mg/kg | 1 | 1 | 1 | |||
| Clearance, ml/min/kg | 27 | 39 | 33 | |||
| Volume of distribution, l/kg | 0.6 | 1.6 | 0.9 | |||
| t1/2, h | 0.5 | 0.5 | 0.3 | |||
| AUC, ng·h/ml | 679 ± 220 | 453 ± 136 | 502 ± 36 | |||
| p.o. dosing | ||||||
| Dose, mg/kg | 1 | 30 | 1 | 3 | 30 | 30 |
| Tmax, h | 0.4 | 3 | 0.5 | 0.6 | 1.7 | 2 |
| Cmax, ng/ml | 306 | 2727 | 29 | 220 | 3487 | 61 |
| AUC, ng·h/ml | 350 ± 120 | 15,300 ± 4100 | 37 ± 6 | 360 ± 42 | 14,800 ± 2500 | 132 ± 106 |
| Oral bioavailability, % | 52 ± 24 | 75 ± 32 | 8 ± 3 | 26 ± 9 | 109 ± 37 | <2 |