Evaluation of the potent anti-hepatitis B virus agent (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in a novel in vivo model.
A murine model was developed to investigate the in vivo activity of anti-hepatitis B virus (HBV) agents. Mice with subcutaneous tumors of HBV-producing 2.2.15 cells showed reductions in levels of HBV in serum and in intracellular levels of HBV when the mice were orally dosed with (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (FTC). No effects on tumor size or alpha-fetoprotein levels were observed. FTC can selectively inhibit HBV replication at nontoxic doses.
Condreay
L D
LD
Division of Experimental Therapy, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.
Jansen
R W
RW
Powdrill
T F
TF
Johnson
L C
LC
Selleseth
D W
DW
Paff
M T
MT
Daluge
S M
SM
Painter
G R
GR
Furman
P A
PA
Ellis
M N
MN
D000818:Animals; D000998:Antiviral Agents / Q000627:therapeutic use*; D001682:Biological Availability; D002460:Cell Line; D004279:DNA, Viral / Q000096:biosynthesis; D000068679:Emtricitabine / Q000031:analogs & derivatives; D006509:Hepatitis B / Q000188:drug therapy* / Q000382:microbiology; D006515:Hepatitis B virus / Q000187:drug effects; D006801:Humans; D051379:Mice; D016133:Polymerase Chain Reaction; D014779:Virus Replication / Q000187:drug effects; D016047:Zalcitabine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D000509:alpha-Fetoproteins / Q000378:metabolism
D000998:Antiviral Agents; D004279:DNA, Viral; D000509:alpha-Fetoproteins; D016047:Zalcitabine; D000068679:Emtricitabine; C075889:Racivir