Chemistry:PSI-6130

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Short description: Chemical compound
PSI-6130
PSI-6130.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC10H14FN3O4
Molar mass259.237 g·mol−1
3D model (JSmol)
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PSI-6130 is an experimental treatment for hepatitis C. PSI-6130 is a member of a class of antiviral drugs known as nucleoside polymerase inhibitors that was created by chemist Jeremy L. Clark.[1] Specifically, PSI-6130 inhibits the hepatitis C virus RNA dependant RNA polymerase called NS5B.[2]

PSI-6130 is currently being developed by Hoffmann–La Roche as a 3',5'-diisobutyrl ester prodrug, R7128.[3] R7128 is part of the combination of all-oral agents clinical trial known as INFORM-1.[4]

References

  1. "Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication". Journal of Medicinal Chemistry 48 (17): 5504–8. August 2005. doi:10.1021/jm0502788. PMID 16107149. 
  2. "Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication". Antiviral Chemistry & Chemotherapy 17 (2): 79–87. 2006. doi:10.1177/095632020601700203. PMID 17042329. 
  3. "R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection". Drugs of the Future 34 (4): 282–290. 2009. doi:10.1358/dof.2009.034.04.1367744. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1367744&p_IsPs=N. 
  4. "Oral combination therapy with a nucleoside polymerase inhibitor (RG7128) and danoprevir for chronic hepatitis C genotype 1 infection (INFORM-1): a randomised, double-blind, placebo-controlled, dose-escalation trial". Lancet 376 (9751): 1467–75. October 2010. doi:10.1016/S0140-6736(10)61384-0. PMID 20951424.