Hepatitis C: Development of a Ribavirin Liver-Targeting Prodrug
Background:The current recommended treatment for chronic hepatitis C virus infection is a combination of interferon and oral ribavirin. Ribavirin treatment is associated with hemolytic anemia, a dose-limiting side-effect.
Result: Viramidine, a liver-targeting prodrug of ribavirin by design, was tested for its pharmacokinetic parameters and safety in animals and humans. Viramidine yielded higher liver drug levels and had superior liver-targeting properties than ribavirin in animal studies. Viramidine gave lowered plasma and red blood cell drug levels of both parent and its ribavirin metabolites when administered at the sane oral dose. In a phase I study, a dose of up to 1,600 mg daily orally for 4 weeks was administered and clinically tolerated in patients with chronic hepatitis C. A phase II study is currently ongoing.
KeywordsChronic Hepatitis Hemolytic Anemia Adenosine Deaminase Current Recommended Treatment Serum Alanine Aminotransferase Level
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