TABLE 2.
In vitro metabolism, protein binding, blood/plasma ratio, and plasma stability data for UCT943a
| Parameter | Value for the parameter (SD) in: |
|||
|---|---|---|---|---|
| Human | Dog | Rat | Mouse | |
| Microsomal CLint (μl/min/mg) | <11.6 (0.1) | 28.2 (0.5) | <11.6 (0.2) | <11.6 (0.7) |
| Hepatocyte CLint (μl/min/106 cells)b | <2 | 9 | 4 | <4 |
| Hepatocyte predicted EHb | <0.2 | 0.65 | 0.23 | <0.2 |
| fu microsomes | 0.15 (0.01) | 0.50 (0.04) | 0.45 (0.05) | 0.47 (0.04) |
| fu plasma | 0.17 (0.009) | 0.10 (0.007) | 0.15 (0.009) | 0.10 (0.02) |
| Blood/plasma ratio | 1.5 (0.1) | 2.3 (0.1) | 2.1 (0.2) | 1.9 (0.2) |
| Plasma stability (after 240 min) (%)b | 97 | 95 | 97 | 102 |
Permeability across Caco-2 cells in both directions, Papp B→A and Papp A→B, was determined as (25 ± 5) × 10−6 cm/s and (28 ± 2) × 10−6 cm/s, respectively.
Single determination.