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HCV Drug Discovery 2009

Day 1 - Day 2 - Download Brochure 


Monday, April 6

7:00am Registration and Morning Coffee

8:00 Chairperson’s Opening Remarks

Robert Ralston, Ph.D., Senior Director of Virology, Schering-Plough Research Institute

HCV: New Drugs, New Trials, New Thinking

John McHutchisonJohn G. McHutchison, M.D., Associate Director, Duke Clinical Research Institute, Director, GI/Hepatology Research Program; Professor of Medicine, Division of Gastroenterology, Duke University

The advent of newer therapies for the treatment of patients with viral hepatitis raises many challenges. Some that will be discussed are:

  • Determining the most appropriate combination of new agents to maximize efficacy, while at the same time minimizing adverse events
  • Developing and implementing strategies and strict guidelines for evaluating resistance that will allow the safest regimens to emerge
  • Creating systems to evaluate whether certain classes of drugs interact more positively with others in terms of patient outcomes

Protease Inhibitors and Taribavirin

8:50 Discovery of Telaprevir, a Potent HCV Protease Inhibitor

Anne-Laure Grillot, Ph.D., Director of Medicinal Chemistry, Vertex Pharmaceuticals 

9:20 Rational Design of Hepatitis C Virus NS3 Protease Inhibitors

Atul Agarwal, Ph.D., Senior Director, Computational Chemistry and Informatics, Achillion

9:50 Networking Coffee Break

10:15 Update on Boceprevir and other HCV protease inhbitors

Robert Ralston, Ph.D., Senior Director of Virology, Schering-Plough Research Institute

10:45 Pharmacokinetics and Pharmacodynamics of Taribavirin

Gordon Loewen, Ph.D., Senior Director of Clinical Pharmacology and Preclinical Development, Valeant Pharmaceuticals

This presentation will review recent data on the pharmacokinetics and pharmacodynamics of weight-based taribavirin dosing and will discuss the potentialy beneficial risk-benefit profile of taribavirin relative to ribavirin.

11:15 Sponsored Presentation

11:30 Panel Session on Combining Therapies

Moderator: John McHutchison, M.D., Duke Research Institute
James (Jim) Appleman, Ph.D., Vice President, Preclinical Biology and Translational Research Anadys Pharmaceuticals, Inc.
Robert Ralston, Ph.D., Senior Director, Virology, Schering-Plough Research Institute
Scott Seiwert, Ph.D., Vice President, Research & Preclinical Development, InterMune, Inc. 
Flossie Wong-Staal, Ph.D., Chief Scientific Officer; Executive Vice President Research, ItherX

  • Factors to consider when choosing combinations
  • Which drug combinations are likely to work?
  • Lead-in strategies and duration considerations

12:00pm Luncheon Presentation or Lunch on your own



Polymerase Inhibitors

1:25 Chairperson’s Remarks

Dave Smith, Ph.D., Principal Research Scientist, Medicinal Chemisty, Roche Palo Alto

1:30 Polymerase Inhibitors for the Treatment of Hepatitis C

Dave Smith, Ph.D., Principal Research Scientist, Medicinal Chemisty, Roche Palo Alto

The HCV genome encodes an RNA-dependent RNA polymerase (NS5B), which is responsible for the synthesis of new viral RNA strands. In this talk, an overview and update on our efforts to develop novel inhibitors of the HCV polymerase NS5B will be presented.

2:00 Nucleoside Approach to Inhibitors for HCV Polymerase
Michael Sofia, Ph.D., Vice President, Chemistry, Pharmasset, Inc.
The presentation will discuss the current status of our clinical candidate R7128 and will present current data on our novel liver targeting inhibitor PSI-7851. A overview of the PSI-7851 design rationale and data supporting liver targeting will be highlighted. In addition, data supporting the development of PSI-7851 will be reviewed.

2:30 Identification of Potent, Orally Bioavailable Non-Nucleoside HCV RNA Polymerase Inhibitors

Frank Ruebsam, Ph.D., Director, Medicinal Chemistry, Anadys Pharmaceuticals, Inc.

We previously disclosed the identification of several novel series of potent, non-nucleoside NS5B inhibitors containing a 1,1-dioxo-1,4-dihydro-1lambda6-benzo[1,2,4]thiadiazine moiety which bind to the “palm” site of the NS5B protein. Many of these molecules exhibited poor pharmacokinetic properties following oral administration to animals. We now describe new modifications that led to significantly improved oral bioavailability properties of the resulting compounds without sacrificing other desirable biological attributes.

3:00 Sponsored Presentation

3:15 Networking Refreshment Break in the Exhibit Hall


Inhibitors of New Viral Targets

4:00 Small Molecule Approaches to NS4B and Other Novel Non-Structural Protein Targets

Jeffrey S. Glenn, M.D., Ph.D., Associate Professor of Medicine, Department of Gastroenterology and Hepatology; Director of Center for Hepatitis and Liver Tissue Engineering, Stanford University School of Medicine

NS4B plays an important role in establishing the HCV replication complex. Several key domains have been genetically validated as essential for NS4B’s function in HCV replication. This in turn has led to the development of small molecule approaches to targeting NS4B, including a new role for an old antihistamine.

4:30 Current Progress in Developing HCV Entry Inhibitors

Flossie Wong-Staal, Ph.D., Chief Scientific Officer; Executive Vice President Research, ItherX

Our small molecule entry inhibitors for HCV exhibit EC50 of <1 nM and >10000 fold therapeutic window in the infectious virus assays. The compounds act additively with the current standard of care (IFN and Ribavirin) as well a HCV protease inhibitor. A clinical development candidate has been selected based on in vivo PK and bioavailability parameters for further development. This class of compounds can add significantly to a drug cocktail targeting multiple steps of the viral life cycle, with the goal of completely eliminating virus infection.

5:00 HCV NS3 Helicase Inhibitors

Anna Boguszewska-Chachulska, Ph.D., Associate Professor of Biology, Warsaw Institute of Biochemistry and Biophysics and Scientific Director, Genomed Ltd.

We discuss helicase inhibitors as potential components of a multidrug therapy against HCV. Viral helicase, a part of NS3 protein, is necessary for the replication of the viral RNA. Helicase inhibitors were identified by fluoromeric assay of helicase activity in a subgenomic HCV replicon system in Huh-7 hepatoma cells. We demonstrated higher antiviral activities in the HCV replication system, together with low cytotoxicity, for compounds belonging to three different groups: acridone-4-carboxylic derivatives (EC50 in the range of 9-10 uM), amidinoanthracyclines (EC50 in the range of 0.01 – 0.14 uM) and tropolone derivatives (EC50 corresponding to 30-46 uM).

5:30 Reception in the Exhibit Hall

6:30 End of Day


For questions or suggestions about the meeting, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute

For sponsorship or exhibiting information, please contact:
Suzanne Carroll
Manager, Business Development
Cambridge Healthtech Institute
Phone: 781-972-5452