Telbivudine: an upcoming agent for chronic hepatitis B.
Telbivudine, the prototype member of beta-L-2 -deoxynucleosides, has proven to be safe in in vitro animal and human studies. Telbivudine given for 4 weeks resulted in an 8-log reduction of woodchuck hepatitis virus DNA, and a 3.8-log reduction of hepatitis B virus DNA in human. After 52 weeks of telbivudine treatment there was an approximate 6-log reduction of hepatitis B virus DNA levels, hepatitis B virus DNA became undetectable by PCR assay in 61% of patients. Its antiviral efficacy is significantly better than lamivudine. The probability of tyrosine-methionine-aspartate-aspartate mutations at 52 weeks of telbivudine therapy is low, although still occurring in 4.5% of patients. After 96 weeks of therapy, the proportion of patients with undetectable hepatitis B virus DNA by PCR assay increased to 71%, but genotypic resistance also increased to 18.2%, with only 4.5% showing alanine aminotransferase flares. Telbivudine is probably one of the most potent antiviral agents for hepatitis B virus that will become available in the near future.
Yuen
Man-Fung
MF
Department of Medicine, The University of Hong Kong, Queen Mary Hospital, Pokfulam Road, Hong Kong, China. mfyuen@hkucc.hku.hk
Lai
Ching-Lung
CL
D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D004279:DNA, Viral / Q000097:blood; D006515:Hepatitis B virus / Q000378:metabolism; D019694:Hepatitis B, Chronic / Q000188:drug therapy*; D006801:Humans; D015394:Molecular Structure; D009705:Nucleosides / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011744:Pyrimidinones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000077712:Telbivudine; D013936:Thymidine / Q000031:analogs & derivatives
D000998:Antiviral Agents; D004279:DNA, Viral; D009705:Nucleosides; D011744:Pyrimidinones; D000077712:Telbivudine; D013936:Thymidine