R7128, a prodrug of PSI-6130
Presentations
Phase 1 Combination Cohorts 1 and 2
Potent Antiviral Activity of the HCV Nucleoside Polymerase Inhibitor, R7128, in Combination with PEG-IFN alfa-2a and Ribavirin.
McHutchison, et al.
43rd Annual Meeting of the European Association for the Study of the Liver (EASL)
Milan, Italy
April 23-27, 2008
Phase 1 Overview
Potent Antiviral Activity of the Nucleoside HCV Inhibitor, R7128, in Prior IFN Non-Responders.
JG McHutchison, et al.
Frontiers in Drug Development in Viral Hepatitis (HEP-DART)
Lahaina, Hawaii
December 9 - 13, 2007
Phase 1 Multiple Ascending Dose Study
Antiviral Activity, Pharmacokinetics, Safety, and Tolerability of R7128, a Novel Nucleoside HCV RNA Polymerase Inhibitor, Following Multiple, Ascending, Oral Doses in Patients with HCV Genotype 1 Infection Who have Failed Prior Interferon Therapy. R. Reddy, et al.
58th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD)
Boston USA
November 2-6, 2007
Phase 1 Single Ascending Dose Study
Pharmacokinetics, Safety, and Tolerability of R7128, a Novel Nucleoside Polymerase Inhibitor for HCV Following Single, Ascending Oral Doses in Healthy Volunteers.
Otto MJ, et al.
14th International Symposium on Hepatitis C Virus and Related Viruses
Glasgow, Scotland
September 9-13, 2007
R7128, A Potent and Selective Nucleoside Inhibitor of HCV NS5B Polymerase: An Overview of Clinical Efficacy and Progress Toward Second Generation Inhibitors
M. Sofia
HCV Drug Discovery 2008
Chicago, IL
April 28, 2008
Preclinical
High Genetic Barrier to HCV Resistance Presented by PSI-6130.
A Uzgiris, et al.
Frontiers in Drug Development in Viral Hepatitis (HEP-DART)
Lahaina, Hawaii
December 9-13, 2007
Preclinical
The Mechanism of Action of Beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine Involves a Second Metabolic Pathway Leading to Beta-D-2'-Deoxy-2'-fluoro-2'-C-methyluridine 5'-Triphosphate, a Potent Inhibitor of the HCV RNA-Dependent RNA Polymerase.
Murakami E, et al (Pharmasset).
14th International Symposium on Hepatitis C Virus and Related Viruses
Glasgow, Scotland
September 9-13, 2007
Preclinical
The Nucleoside Inhibitors R1479, PSI-6130, and NM107 have a Higher Genetic Barrier to Resistance than the Non-nucleoside Inhibitor HCV-796 and the Protease Inhibitor VX-950.
McCown M, et al (Roche Palo Alto).
14th International Symposium on Hepatitis C Virus and Related Viruses
Glasgow, Scotland
September 9-13, 2007
Preclinical
In Vitro Selection and Characterization of HCV Replicons Resistant to PSI-6130.
Ali S, et al (Roche Palo Alto).
14th International Symposium on Hepatitis C Virus and Related Viruses
Glasgow, Scotland
September 9-13, 2007
Preclinical
Inhibition of HCV Replication by PSI-6130: Characterization of Activity in the HCV Replicon System
42nd Annual Meeting of the European Association for the Study of the Liver (EASL)
Barcelona, Spain
April 11-15, 2007
Preclinical
Inhibition of HCV Replication by PSI-6130: Mechanism of Biochemical Activation and Inhibition
42nd Annual Meeting of the European Association for the Study of the Liver (EASL)
Barcelona, Spain
April 11-15, 2007
Preclinical
Inhibition of HCV Replication by PSI-6130: Mechanism of Biochemical Activation and Inhibition
1st International Workshop on Hepatitis C Resistance & New Compounds
Boston, MA
October 25-26, 2006
Preclinical
Inhibition of HCV Replication by PSI-6130: Characterization of Activity in the HCV Replicon System
1st International Workshop on Hepatitis C Resistance & New Compounds
Boston, MA
October 25-26, 2006
Publications
Murakami E, Bao H, Ramesh M, McBrayer TR, Whitaker T, Micolochick Steuer HM, Schinazi RF, Stuyver LJ, Obikhod A, Otto MJ, Furman PA. Mechanism of activation of {Beta}-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. Antimicrobial Agents and Chemotherapy. February 2007, 51(2):503-509.
Stuyver LJ, McBrayer TR, Thranish PM, Clark J, Hollecker L, Lostia S, Nachman T, Grier J, Bennett MA, Xie M-Y, Schinazi RF, Morrey JD, Julander JL, Furman PA, and Otto MJ. Inhibition of hepatitis C replicon RNA synthesis by β-D-2’-deoxy-2’-fluoro-2’-methylcytidine: A specific inhibitor of hepatitis C virus replication. Antiviral Chemistry and Chemotherapy. 2006, 17: 79-87.
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, Pankiewicx KW. 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. 2005, 48(17): 5504-5508.
Stuyver LJ, McBrayer TR, Whitaker T, Tharnish PM, Ramesh M, Lostia S, Cartee L, Shi, Hobbs A, Schinazi RF, Watanabe KA, Otto MJ. Inhibition of the Subgenomic Heptatitis C Virus Replicon in Huh-7 cells by 2'-Deoxy-2'-Fluorocytidine. Antimicrobial Agents Chemotherapy. February 2004, 77 (19):651-654.
Stuyver LJ, McBrayer TR, Tharnish PM, Hassan AEA, Chu CK, Pankiewicz K, Watanabe KA, Schinazi RF, Otto MJ. Dynamics of subgenomic heptatitis C virus replicon RNA levels in huh-7 cells after exposure to Nucleoside Antimetabolites. Journal of Virology. October 2003, 77(19):10689-10694.
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