(-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (524W91) inhibits hepatitis B virus replication in primary human hepatocytes.
The anti-hepatitis B virus (HBV) activity of (-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (524W91) in cultures of primary human hepatocytes was examined. 524W91 was anabolized to the active 5'-triphosphate in these cells. HBV replication was equally inhibited in cultures incubated with 524W91 when the drug was added 24 h preinfection, at infection, or 24 h postinfection. 524W91 inhibited HBV replication by 50% at less than 20 nM in human hepatocytes.
Condreay
L D
LD
Division of Experimental Therapy, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709, USA. USBWCVRC@IBMMAIL.COM
Condreay
J P
JP
Jansen
R W
RW
Paff
M T
MT
Averett
D R
DR
D000998:Antiviral Agents / Q000494:pharmacology*; D015139:Blotting, Southern; D002478:Cells, Cultured; D000068679:Emtricitabine / Q000031:analogs & derivatives; D006515:Hepatitis B virus / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000821:virology; D013997:Time Factors; D014779:Virus Replication / Q000187:drug effects*; D016047:Zalcitabine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000998:Antiviral Agents; D016047:Zalcitabine; D000068679:Emtricitabine; C075889:Racivir