R-1626, a specific oral NS5B polymerase inhibitor of hepatitis C virus.

Roche Holding AG is developing R-1626, an oral nucleoside inhibitor of HCV RNA polymerase. R-1626 has been demonstrated to be well absorbed and rapidly converted to the active component R-1479. The compound has demonstrated a strong capacity to inhibit HCV replication in vitro and in vivo, without the rapid development of viral resistance. After 4 weeks of treatment with R-1626 in combination with PEG-IFN plus ribavirin in treatment-naïve patients with genotype 1 HCV infection, HCV RNA could no longer be detected in approximately 74% of patients, compared with 5% of patients treated with PEG-IFN plus ribavirin alone, indicating the high potency of R-1626 to induce HCV RNA viral load reductions. R-1626 was generally well tolerated, although severe side effects of neutropenia were observed at high doses. A phase IIb clinical trial was ongoing at the time of publication to test the efficacy of R-1626 in combination with a standard or lower dose of PEG-IFN and ribavirin in HCV genotype 1-infected patients. Given its potent antiviral effect with an apparent high genetic barrier, R-1626 represents an important advancement in improving the outcome of patients with chronic HCV infection.
AuthorsPierluigi Toniutto, Carlo Fabris, Davide Bitetto, Elisa Fumolo, Ezio Fornasiere, Mario Pirisi
JournalIDrugs : the investigational drugs journal (IDrugs) Vol. 11 Issue 10 Pg. 738-49 (Oct 2008) ISSN: 1369-7056 [Print] England
PMID18828074 (Publication Type: Journal Article, Review)
Chemical References
  • Antiviral Agents
  • Enzyme Inhibitors
  • NS-5 protein, hepatitis C virus
  • Nucleosides
  • Prodrugs
  • RNA, Viral
  • Viral Nonstructural Proteins
  • balapiravir
  • Administration, Oral
  • Animals
  • Antiviral Agents (administration & dosage, therapeutic use)
  • Drug Evaluation, Preclinical
  • Drug Resistance, Viral
  • Drug Therapy, Combination
  • Enzyme Inhibitors (administration & dosage, therapeutic use)
  • Hepacivirus (drug effects, enzymology, genetics)
  • Hepatitis C, Chronic (drug therapy)
  • Humans
  • Molecular Structure
  • Nucleosides (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
  • Patents as Topic
  • Prodrugs (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
  • RNA, Viral (blood)
  • Structure-Activity Relationship
  • Treatment Outcome
  • Viral Load
  • Viral Nonstructural Proteins (adverse effects, antagonists & inhibitors, metabolism, pharmacokinetics)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!

Choose Username:
Verify Password: