TABLE 5.
Activity of grazoprevir in GT4 NS3 RASsa
| Replicon | EC (nM) ± SD and fold shift |
|||
|---|---|---|---|---|
| EC50 | EC50 fold shift | EC90 | EC90 fold shift | |
| Wild type | 0.7 ± 0.4 | 1 | 1.4 ± 0.7 | 1 |
| G162R | 0.7 ± 0.5 | 1 | 1.6 ± 1 | 1.1 |
| G162R_D168A | 96 ± 12 | 137.1 | 216 ± 40 | 154.3 |
| D168G | Unfit | NA | Unfit | NA |
| G162R_D168V | 33 ± 20 | 47.1 | 97 ± 31 | 69.3 |
a
The chimeric replicons bearing the resistance-associated substitutions were generated in a GT2a (JFH1) background, and potencies were determined using a TaqMan-based assay. The fold shift is based on the wild-type value. NA, not applicable.