Table 1.
Agent | EC50 (±SD), nM* | Ctrough, nM* | ||
---|---|---|---|---|
GT 1b (Con1) replicon | GT 1b NS3-D168V, NS5A-L31M-Y93H | Fold change | ||
Asunaprevir | 2.0 ± 0.4 | 401 ± 102 | 201 | 40† |
Daclatasvir | 0.002 ± 0.001 | 49 ± 9 | 24,500 | 250† |
Beclabuvir | 3.4 ± 0.2 | 4.0 ± 0.7 | 1 | 500† |
Ledipasvir | 0.002 ± 0.0004 | 131 ± 40 | 65,500 | 120 [20] |
Sofosbuvir | 147 ± 27 | 102 ± 12 | 1 | 1,100† |
Simeprevir | 1.9 ± 0.1 | 6,296 ± 203 | 3,313 | 2,200† |
Next-gen NS5A (BMS-1) | 0.010 ± 0.002 | 0.354 ± 0.05 | 39 | – |
Next-gen NS3 PI (BMS-2) | 0.7 ± 0.1 | 4.1 ± 0.6 | 6 | 100‡ |
Ribavirin* | 8.1 ± 1.2 | 7.8 ± 5.7 | 1 | 2.5 [21] |
Peginterferon alfa* | 1.2 ± 0.2 | 2.6 ± 0.6 | 2 | 15 [22] |
C trough trough plasma concentrations, EC 50 50% effective concentrations, GT genotype, NS3 non-structural protein 3, NS5A non-structural protein 5A, PI protease inhibitor, SD standard deviation
* All EC50 and Ctrough concentrations are nM, except for ribavirin (µg/mL) and peginterferon alfa (ng/mL)
† BMS data on file
‡ Estimated value