Chemistry:Filibuvir
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Short description: Chemical compound
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| Other names | PF-00868554 |
| Routes of administration | Oral |
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| Formula | C29H37N5O3 |
| Molar mass | 503.647 g·mol−1 |
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Filibuvir (also known as PF-00868554, PF-868554) was a non-nucleoside orally available[1] NS5B inhibitor developed by Pfizer for the treatment of hepatitis C. It binds to the non-catalytic Thumb II allosteric pocket of NS5B viral polymerase and causes a decrease in viral RNA synthesis. It is a potent and selective inhibitor, with a mean IC50 of 0.019 μM against genotype 1 polymerases.[2] Several filibuvir-resistant mutations have been identified, M423 being the most common that occurred after filibuvir monotherapy.[3] It was intended to be taken twice-daily.[4]
Its investigation was discontinued in February 2013 due to strategic reasons.[5][6]
References
- ↑ "Pfizer Halts Development of Hepatitis C Drug Filibuvir: Report". Doctor's Guide Publishing Limited. http://www.firstwordpharma.com/node/1063595#axzz3tTW1Jy65.
- ↑ "Preclinical characterization of PF-00868554, a potent nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase". Antimicrobial Agents and Chemotherapy 53 (6): 2544–52. June 2009. doi:10.1128/AAC.01599-08. PMID 19307358.
- ↑ "Understanding the drug resistance mechanism of hepatitis C virus NS5B to PF-00868554 due to mutations of the 423 site: a computational study". Molecular BioSystems 10 (4): 767–77. April 2014. doi:10.1039/c3mb70498j. PMID 24452008.
- ↑ "Filibuvir, a non-nucleoside NS5B polymerase inhibitor for the potential oral treatment of chronic HCV infection". IDrugs 13 (12): 938–48. December 2010. PMID 21154154.
- ↑ Loftus, Peter (8 March 2013). "Pfizer Stops Developing Hepatitis C Drug". The Wall Street Journal (Dow Jones & Company, Inc.). https://www.wsj.com/articles/SB10001424127887324128504578348370181890456.
- ↑ "Discontinued drugs in 2012 - 2013: hepatitis C virus infection". Expert Opinion on Investigational Drugs 24 (2): 239–51. February 2015. doi:10.1517/13543784.2015.982274. PMID 25384989.
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