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WEDNESDAY, APRIL 28
12:30 pm Registration
1:30 Chairperson's Opening Remarks
1:40 Structure-Based Design of Non-Nucleoside NS5B Inhibitors for the Treatment of HCV
Francisco Talamas, Ph.D., Associate Director, Virology, Roche Palo Alto
This presentation will describe the approach used to design potent non- nucleoside NS5B inhibitors using crystallographic information. I will also highlight the different strategies that were utilized in the optimization of potency, physical properties and safety issues.
2:10 PSI-7851: Development of a Nucleotide Prodrug for the Treatment of HCV
Michael J. Sofia, Ph.D., Vice President, Chemistry, Pharmasset, Inc.
Nucleosides have been shown to have a number of advantages for the treatment of HCV. These advantages include a high barrier to resistance, broad genotype coverage and the ability to be combined with other direct acting antiviral agents to produce a robust antiviral response. PSI-7851 is a novel nucleotide prodrug designed to produce a high liver to plasma ratio with the goals of increased potency and once a day dosing. The discovery of PSI-7851 and recent clinical results will be described.
2:40 Novel Phosphoramidate HCV NS5b Inhibitors
Joseph Patti, Ph.D., Co-founder, CSO, Inhibitex, Inc.
Prodrugs of nucleosides are emerging as the second generation of HCV polymerase inhibitors. The prodrugs are highly potent and are preferentially localized to the liver. It is anticipated that this class of nucleosides will emerge as the preferred drug for combination therapy.
3:10 Sponsored Presentations (Opportunity Available)
3:40 Networking Refreshment Break, Poster and Exhibit Viewing
4:20 The Identification and Optimization of HCV Replicon Inhibitors Characterised by NS5A Specific Mutations
Stuart Cockerill, Ph.D., Head of Discovery, Virology, Arrow Therapeutics/Astra Zeneca
The approach to the identification of HCV Replicon Inhibitors and their characterization by reference to their resistant mutant profile is described. Optimization to orally available potent drug candidates will also be discussed.
4:50 Discovery and Characterization of PPI-461, a Potent and Selective HCV NS5A Inhibitor with Broad-Spectrum Coverage of all HCV Genotypes
Richard Colonno, Ph.D., Chief Scientific Officer, Presidio Pharmaceuticals
HCV NS5A protein plays a critical role in the HCV viral replicative cycle and is an attractive target for antiviral intervention. PPI-461 is a newly discovered inhibitor of HCV NS5A protein that exhibits a preclinical virologic, pharmacokinetic and toxicology profile supportive of advancement into clinical trials.
5:20 pm Break-Out Discussions
6:30 End of Day
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