Table 2.
Antiviral activity of FDA-approved compounds in HCV cell culture.
Protein | Compound | In vitro activity (EC50, nM) |
Ref. | |||||||
---|---|---|---|---|---|---|---|---|---|---|
GT-1a | GT-1b | GT-2a | GT-2b | GT-3a | GT-4a | GT-5a | GT-6a | |||
NS3/4A | Boceprevir (SCH503034) | 196 ± 56 | 251 ± 71 | 283 ± 36 | 315 ± 30 | 159 ± 5 | – | – | – | Silva et al., 2013 |
Telaprevir (VX-950) | 395 ± 16 | 285 ± 60 | 252 ± 54 | 402 ± 52 | 953 ± 103 | – | – | – | Silva et al., 2013 | |
Paritaprevir (ABT-450) | 1.0 ± 0.33 | 0.21 ± 0.07 | 5.3 ± 1.2 | – | 19 ± 5.2 | 0.09 ± 0.03 | – | 0.69 ± 0.09 | Pilot-Matias et al., 2015 | |
Grazoprevir (MK-5172) | 0.4 ± 0.2 | 0.5 ± 0.3 | 2.3 ± 1.2 | 3.7 ± 1.1 | 2.1 ± 1 | 0.3 ± 0.2 | 6.6 ± 0.6 | 0.9 ± 0.1 | Lahser et al., 2016 | |
Simeprevir (TMC435) | 28.4 (19–39.7) | 8.1 (4.5–11.9) | – | – | – | – | – | – | Lin et al., 2009 | |
NS5A | Daclatasvir (BMS-790052) | 0.05 ± 0.013 | 0.009 ± 0.004 | 0.071 ± 0.017 | – | 0.146 ± 0.034 | 0.012 ± 0.004 | 0.033 ± 0.01 | Gao et al., 2010 | |
Ledipasvir (GS-5885) | 0.031 | 0.004 | 21 | 16 | 168 | 0.39 | 0.15 | 1.1 | Cheng et al., 2016 | |
Ombitasvir (ABT-267) | 0.0141 ± 0.0068 | 0.005 ± 0.0019 | 0.0124 ± 0.0027 | 0.0043 ± 0.0012 | 0.0193 ± 0.0058 | 0.00171 ± 0.00088 | 0.0043 ± 0.0009 | 0.415 ± 0.097 | DeGoey et al., 2014 | |
Elbasvir (MK-8742) | 0.004 ± 0.002 | 0.003 ± 0.001 | 0.003 ± 0.001 | 3.4 ± 2.6 | 0.14 ± 0.09 | 0.0003 ± 0.0001 | 0.001 ± 0.001 | 0.009 ± 0.006 | Lahser et al., 2016 | |
Velpatasvir (GS-5816) | 0.013 | 0.015 | 0.009 | 0.01 | 0.013 | 0.009 | 0.059 | 0.007 | Cheng et al., 2013 | |
NS5B | Sofosbuvir (GS-7977) | 44 ± 4.7 | 48 ± 13 | 37 ± 3.6 | 20 ± 4.4 | 16 ± 3.4 | – | – | – | Lam et al., 2012 |
Dasabuvir (ABT-333) | 7.7 ± 3.8 | 1.8 ± 0.98 | – | – | – | – | – | – | Kati et al., 2015 |
-: Unavailable data. Information of HCV strains and experimental settings is available in the literature.