Table 4.
Potency of grazoprevir and simeprevir against a panel of HCV GT1a NS3 substitutions in replicon assay
| NS3 substitution | Grazoprevir |
Boceprevir |
Simeprevir |
|||
|---|---|---|---|---|---|---|
| EC50 ± S.D. | -Fold shift | EC50 ± S.D. | -Fold shift | EC50 ± S.D. | -Fold shift | |
| nm | nm | nm | ||||
| GT1a_WTa | 0.65 ± 0.32 | 1.0 | 1214 ± 374 | 1.0 | 12.2 ± 6.3 | 1.0 |
| GT1a_R155Ka | 2.9 ± 1.3 | 4.5 | 2582 ± 113 | 2.1 | 484 ± 140 | 40 |
| GT1a_D168Aa | 86 ± 17 | 132 | 962 ± 107 | 0.8 | 4850 ± 76 | 398 |
| GT1a_R155K/D168Aa | 2.7 ± 1.3 | 4.1 | 3266 ± 320 | 2.7 | 5072 | 416 |
| GT1a_WTb | 0.4 ± 0.2 | 1.0 | 275 ± 138 | 1.0 | 3.2 ± 2.6 | 1.0 |
| V36M/R155Kb | 3.5 ± 2.4 | 8.8 | 4785 ± 837 | 17 | 745 ± 233 | 233 |
| Y56H/D168Ab | 655 ± 437 | 1638 | 213 ± 53 | 0.8 | 517 ± 93 | 162 |
a Data are from the transient replicon.
b Data are from the stable replicon.