LB80380: a promising new drug for the treatment of chronic hepatitis B.
Hepatitis B virus is a significant cause of liver cirrhosis and hepatocellular carcinoma in patients with chronic infection. Higher levels of viral load are associated with increased risk of developing liver-related complications. The current available oral therapies suppress viral replication through their action on the hepatitis B virus polymerase. As treatment with oral nucleoside/nucleotide analogues is associated with the development of drug-resistant mutations, there is continuing research for newer and more potent antiviral agents to reduce the chance of drug resistance. LB80380, a prodrug, is an oral nucleotide analogue that inhibits viral replication by incorporation into the viral DNA. Antiviral activity against wild-type virus and virus with drug-resistant mutations was demonstrated in Phase II trials, with significant reduction of viral load in patients treated with LB80380. LB80380 was also shown to be safe and well tolerated.
Fung
James
J
The University of Hong Kong, Queen Mary Hospital, Department of Medicine, Pokfulam Road, Hong Kong.
Lai
Ching-Lung
CL
Yuen
Man-Fung
MF
D000225:Adenine / Q000031:analogs & derivatives / Q000627:therapeutic use; D000410:Alanine Transaminase / Q000097:blood; D000998:Antiviral Agents / Q000627:therapeutic use*; D004279:DNA, Viral / Q000097:blood; D006147:Guanine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D006513:Hepatitis B e Antigens / Q000097:blood; D019694:Hepatitis B, Chronic / Q000188:drug therapy*; D006801:Humans; D007155:Immunologic Factors / Q000627:therapeutic use; D063065:Organophosphonates / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D017410:Practice Guidelines as Topic
C487369:((1-((2-amino-9H-purin-9-yl)methyl)cyclopropyl)oxy)methylphosphonic acid dipivoxyl; D000998:Antiviral Agents; D004279:DNA, Viral; D006513:Hepatitis B e Antigens; D007155:Immunologic Factors; D063065:Organophosphonates; C413685:entecavir; D006147:Guanine; C053001:adefovir; D000410:Alanine Transaminase; D000225:Adenine