TABLE 3.
Antiviral activity of NVR 3-778, LMV, ETV, and TDF in HepG2 cells transiently transfected with nucleoside-resistant HBV variants
| Compound | WT EC50 (µM) | EC50 fold changec |
||||
|---|---|---|---|---|---|---|
| rtL180M/M204V | rtL180M/M204V/N236T | rtA181V | rtN236T | rtA181V/N236T | ||
| LMV | 0.53 ± 0.12 | >190 | >190 | 1.7 ± 0.9d | 1.0 ± 0.5d | 4.8 ± 2.3a |
| ETV | 0.0014 ± 0.0004 | 31 ± 16a | 14 ± 4a | 2.2 ± 0.5a | 0.67 ± 0.22d | 1.8 ± 0.6d |
| TDF | 0.032 ± 0.015 | 1.1 ± 0.3d | 2.9 ± 1.5b | 1.4 ± 0.05d | 2.2 ± 1.0b | 2.8 ± 1.4b |
| NVR 3-778 | 0.31 ± 0.10 | 1.3 ± 0.6d | 1.4 ± 0.5d | 0.82 ± 0.19d | 0.85 ± 0.40d | 0.85 ± 0.26d |
a
The t-test P value was <0.01.
b
The t-test P value was <0.05.
c
Ratio of the mean EC50 value for the HBV inhibitors determined against reverse transcriptase variants over those against wild-type (WT) HBV. EC50 fold change values compared to the value for the WT are shown as the mean value ± standard deviation from at least three independent studies.
d
The t-test P value was not significant (P > 0.05).