Table 4.
Caco-2 Intestinal Permeability. Expected values are reported in brackets.
| Compound | Direction/±Inhibitor | Papp (nm/s) [Expected Values] |
Recovery % | Efflux Ratio (Reduction %) |
|---|---|---|---|---|
| Atenolol † | A→B | <10 [<10] | 86 ± 1 | |
| Metoprolol † | A→B | >400 [>400] | 105 ± 5 | |
| Digoxin † (P-gp substrate) |
A→B | 2 ± 1 [2] | 67 ± 5 | |
| B→A | 141 ± 26 [139] | 71 ± 6 | >10 | |
| A→B + EL * 2 µM | 35 ± 5 [26] | 72 ± 1 | ||
| B→A + EL * 2 µM | 83 ± 31 [63] | 75 ± 3 | 2.3 (96%) | |
| tolcapone | A→B | 101 ± 12 | 53 ± 1 | 2 |
| B→A | 206 ± 58 | 70 ± 4 | ||
| 3-OMT | A→B | 160 ± 29 | 66 ± 4 | 1.5 |
| B→A | 243 ± 30 | 83 ± 8 | ||
| 1 | A→B | 240 ± 21 | 64 ± 4 | 1 |
| B→A | 231 ± 23 | 77 ± 2 | ||
| 2 | A→B | 250 ± 3 | 69 ± 8 | 1 |
| B→A | 268 ± 25 | 80 ± 9 |
† Reference compounds, * EL: Elacridar.