NS5A inhibitors: a new breakthrough for the treatment of chronic hepatitis C.
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TLDR
These results provide the first clinical validation of an inhibitor of HCV NS5A, a protein with no known enzymatic function, as an approach to the suppression of virus replication that offers potential as part of a therapeutic regimen based on combinations ofHCV inhibitors.About:
This article is published in Journal of Hepatology.The article was published on 2011-05-01 and is currently open access. It has received 30 citations till now. The article focuses on the topics: Boceprevir & NS5B.read more
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HCV direct‐acting antiviral agents: the best interferon‐free combinations
TL;DR: The aim of this review was to summarize the results obtained from recent DAA combination studies without IFN, making HCV, the first chronic viral infection to be eradicated worldwide with a finite duration of combination DAA therapy withoutIFN or ribavirin.
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Discovery and Development of Simeprevir (TMC435), a HCV NS3/4A Protease Inhibitor
Åsa Rosenquist,Bertil Samuelsson,Per-Ola Johansson,Maxwell D. Cummings,Oliver Lenz,Pierre Jean-Marie Bernard Raboisson,Kenny Simmen,Sandrine Vendeville,Herman de Kock,Magnus Nilsson,Andras Horvath,R. Kalmeijer,Guy De La Rosa,M. Beumont-Mauviel +13 more
TL;DR: The extensive medicinal chemistry effort to develop novel P2 cyclopentane macrocyclic inhibitors guided by HCV NS3 protease assays, the cellular replicon system, structure-based design, and a panel of DMPK assays are summarized.
Journal ArticleDOI
Direct acting antivirals for the treatment of chronic hepatitis C: one pill a day for tomorrow.
Tarik Asselah,Patrick Marcellin +1 more
TL;DR: Combinations of antivirals with additive potency that lack cross resistance and with a good safety profile may provide new regimens in the future to make HCV the first chronic viral infection eradicated worldwide with a finite duration of combination DAA therapy without IFN.
Journal ArticleDOI
Interferon free therapy with direct acting antivirals for HCV.
Tarik Asselah,Patrick Marcellin +1 more
TL;DR: Combinations of antivirals with additive potency that lack cross‐resistance and with a good safety profile may provide new regimens in the future to make HCV the first chronic viral infection to be eradicated worldwide with a finite duration of combination DAA therapy without IFN.
Journal ArticleDOI
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication
Andrew V. Stachulski,Andrew V. Stachulski,Chandrakala Pidathala,Eleanor C. Row,Raman Sharma,Neil G. Berry,Mazhar Iqbal,Joanne Bentley,Sarah Allman,Geoffrey Edwards,Alison Helm,Jennifer Hellier,Brent E. Korba,J. Edward Semple,Jean-Francois Rossignol +14 more
TL;DR: The syntheses and activities of a wide range of thiazolides against hepatitis B virus replication are reported, with QSAR analysis of results showing a good correlation of observed EC(90) for intracellular virions withThiazolide structural parameters.
References
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Journal ArticleDOI
Isolation of a cDNA clone derived from a blood-borne non-A, non-B viral hepatitis genome
TL;DR: A random-primed complementary DNA library was constructed from plasma containing the uncharacterized non-A, non-B hepatitis agent and screened with serum from a patient diagnosed with NANBH, showing consistent with the agent being similar to the togaviridae or flaviviridae.
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Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect
Min Gao,Richard E. Nettles,Makonen Belema,Lawrence B. Snyder,Van N. Nguyen,Robert A. Fridell,Michael H. Serrano-Wu,David R. Langley,Jin-Hua Sun,Donald R. O'Boyle,Julie A. Lemm,Chunfu Wang,Jay O. Knipe,Caly Chien,Richard J. Colonno,Dennis M. Grasela,Nicholas A. Meanwell,Lawrence G. Hamann +17 more
TL;DR: These results provide the first clinical validation of an inhibitor of HCV NS5A, a protein with no known enzymatic function, as an approach to the suppression of virus replication that offers potential as part of a therapeutic regimen based on combinations ofHCV inhibitors.
Journal ArticleDOI
Telaprevir for previously treated chronic HCV infection.
John G. McHutchison,Michael P. Manns,Andrew J. Muir,Norah A. Terrault,Ira M. Jacobson,Nezam H. Afdhal,E. Jenny Heathcote,Stefan Zeuzem,Hendrik W. Reesink,Jyotsna Garg,Mohammad Bsharat,Shelley George,Robert S. Kauffman,Nathalie Adda,Adrian M. Di Bisceglie +14 more
TL;DR: In HCV-infected patients in whom initial peginterferon alfa-2a and ribavirin treatment failed, retreatment with telaprevir in combination with pegin terferonAlfa-1a and 2a and Ribavirin was more effective than retreatment without combination.
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Efficacy of boceprevir, an NS3 protease inhibitor, in combination with peginterferon alfa-2b and ribavirin in treatment-naive patients with genotype 1 hepatitis C infection (SPRINT-1): an open-label, randomised, multicentre phase 2 trial
Paul Y. Kwo,Eric Lawitz,Jonathan McCone,Eugene R. Schiff,John M. Vierling,David Pound,M. Davis,Joseph S. Galati,Stuart C. Gordon,Natarajan Ravendhran,Lorenzo Rossaro,Frank H. Anderson,Ira M. Jacobson,Raymond A. Rubin,Kenneth Koury,Lisa D. Pedicone,Clifford A. Brass,Eirum Chaudhri,Janice K. Albrecht +18 more
TL;DR: In patients with untreated genotype 1 chronic hepatitis C infection, the addition of the direct-acting antiviral agent boceprevir to standard treatment with peginterferon and ribavirin after a 4-week lead-in seems to have the potential to double the sustained response rate compared with that recorded with standard treatment alone.
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Exploring biology with small organic molecules
TL;DR: The mapping of biological-activity space using small molecules is akin to mapping the stars — uncharted territory is explored using a system of coordinates that describes where each new feature lies.