Table 2.
Potency of ASV and VX-950 against a panel of serine and cysteine proteases
| Protease | IC50 (μM)a |
|
|---|---|---|
| ASV | VX-950 | |
| HCV NS3/4A (1a [H77]) | 0.0007 ± 0.0001 | 0.012 ± 0.002 |
| GBV-B NS3/4A | 21 ± 6 | 7.7 ± 0.0 |
| Human leukocyte elastase | >50 | 3.2 ± 0.1 |
| PPE | >50 | 5.6 ± 0.3 |
| Human chymotrypsin | >50 | 45 ± 8 |
| Human cathepsin A | >5b | 0.33 ± 0.02 |
| Human cathepsin B | >50 | 1.7 ± 0.2 |
| Trypsin | >30 | ND |
| Thrombin | >30 | ND |
| Factor VIIa | >30 | ND |
| Factor Xa | >30 | ND |
| Factor XIa | >30 | ND |
| Kallikrein | >30 | ND |
a
Data are means ± standard deviations from at least three independent experiments. ND, not determined.
b
Assay interference was observed at 20 μM.