title: 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.
abstract: 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.
authors.affiliation: Division of Experimental Therapy, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.
authors.forename: L D
authors.initials: LD
authors.lastname: Condreay
authors.forename: R W
authors.initials: RW
authors.lastname: Jansen
authors.forename: T F
authors.initials: TF
authors.lastname: Powdrill
authors.forename: L C
authors.initials: LC
authors.lastname: Johnson
authors.forename: D W
authors.initials: DW
authors.lastname: Selleseth
authors.forename: M T
authors.initials: MT
authors.lastname: Paff
authors.forename: S M
authors.initials: SM
authors.lastname: Daluge
authors.forename: G R
authors.initials: GR
authors.lastname: Painter
authors.forename: P A
authors.initials: PA
authors.lastname: Furman
authors.forename: M N
authors.initials: MN
authors.lastname: Ellis
mesh_terms: 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
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D000509:alpha-Fetoproteins; D016047:Zalcitabine; D000068679:Emtricitabine; C075889:Racivir