TABLE 3

Antiviral activity of NVR 3-778, LMV, ETV, and TDF in HepG2 cells transiently transfected with nucleoside-resistant HBV variants

CompoundWT EC50 (µM)EC50 fold changec
rtL180M/M204VrtL180M/M204V/N236TrtA181VrtN236TrtA181V/N236T
LMV0.53 ± 0.12>190>1901.7 ± 0.9d1.0 ± 0.5d4.8 ± 2.3a
ETV0.0014 ± 0.000431 ± 16a14 ± 4a2.2 ± 0.5a0.67 ± 0.22d1.8 ± 0.6d
TDF0.032 ± 0.0151.1 ± 0.3d2.9 ± 1.5b1.4 ± 0.05d2.2 ± 1.0b2.8 ± 1.4b
NVR 3-7780.31 ± 0.101.3 ± 0.6d1.4 ± 0.5d0.82 ± 0.19d0.85 ± 0.40d0.85 ± 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).