TABLE 4.
Prediction of in vivo hepatic clearance of ABI-274 and ABI-286 in rat and human from in vitro metabolic stability
| Rat ABI-274 | Rat ABI-286 | Human ABI-274 | Human ABI-286 | |
|---|---|---|---|---|
| Hepatic blood flow (ml · min−1 · kg−1) | 55 | 55 | 21 | 21 |
| t1/2, in liver microsomes, min | 30 | 46 | 21 | 44 |
| SF | 2400 | 2400 | 1980 | 1980 |
| SF (mg protein/g liver · g liver/kg b.wt.) | (54 · 45) | (54 · 45) | (77 · 25.7) | (77 · 25.7) |
| Cli, in vitro | 0.023 | 0.015 | 0.033 | 0.016 |
| Cli, h | 55.44 | 36.16 | 65.34 | 31.19 |
| Clh, ml · min−1 · kg−1 (predicted) | 28 | 22 | 16 | 13 |
| Clin vivo | 29 | 16 | N.A. | N.A. |
N.A., not available; SF, scaling factor.