TABLE 3

Antiviral activity in HBV-infected primary human hepatocytesa

Day and compoundnMean (SD) EC50 (nM)
HBV DNAIntracellular total HBV RNAHBe/cAgHBsAg
Day 0
    JNJ-6323415 (129)2,664 (158)1,826 (1)2,818 (127)
    BAY41-41093263 (42)1,539 (287)1,529 (110)2,708 (87)
    ETV1<0.16 (NA)>100 (NA)>100 (NA)>100 (NA)
Day 5
    JNJ-6323418 (96)>25,000 (NA)>25,000 (NA)>25,000 (NA)
    BAY41-41093532 (81)>25,000 (NA)>25,000 (NA)>25,000 (NA)
    ETV1<0.16 (NA)>100 (NA)>100 (NA)>100 (NA)
  • a Cryopreserved PHH were infected with HBV derived from HepG2.2.15 cell culture supernatants in vitro. The anti-HBV activity of JNJ-632, BAY41-4109, and ETV was tested in a dose-response assay. HBV DNA was extracted from the cell culture supernatant, and DNA levels and intracellular HBV RNA levels were assessed using qPCR. HBe/cAg and HBsAg in the cell culture supernatant was detected by AlphaLISA. EC50, 50% effective concentration; n, number of experimental repeats; NA, not applicable.