PSI-6130 explained

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]

Notes and References

  1. Clark JL, Hollecker L, Mason JC, Stuyver LJ, Tharnish PM, Lostia S, McBrayer TR, Schinazi RF, Watanabe KA, Otto MJ, Furman PA, Stec WJ, Patterson SE, Pankiewicz KW . 6 . 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 . 16107149 . 10.1021/jm0502788 .
  2. Stuyver LJ, McBrayer TR, Tharnish PM, Clark J, Hollecker L, Lostia S, Nachman T, Grier J, Bennett MA, Xie MY, Schinazi RF, Morrey JD, Julander JL, Furman PA, Otto MJ . 6 . 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 . 17042329 . 10.1177/095632020601700203 . 22710780 .
  3. Cole P, Castaner R, Bolos J . R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection . Drugs of the Future . 34 . 4 . 282–290 . 2009 . 10.1358/dof.2009.034.04.1367744 .
  4. 6 . Gane EJ, Roberts SK, Stedman CA, Angus PW, Ritchie B, Elston R, Ipe D, Morcos PN, Baher L, Najera I, Chu T, Lopatin U, Berrey MM, Bradford W, Laughlin M, Shulman NS, Smith PF . October 2010 . 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 . 10.1016/S0140-6736(10)61384-0 . 20951424 . 28977802.

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