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Genelabs Technologies Announces Presentation of Data on,Non-Nucleoside HCV Polymerase Inhibitor at 20th International,Conference on Antiviral Research Meeting

REDWOOD CITY, Calif., May 02, 2007 /PRNewswire-FirstCall/ -- Genelabs Technologies, Inc. announced today that a presentation was made today at the 20th International Conference on Antiviral Research being held in Palm Springs, California, on a non-nucleoside hepatitis C virus (HCV) polymerase inhibitor discovered by Genelabs.

The oral presentation was given by Christopher D. Roberts, Ph.D., Director of Medicinal Chemistry at Genelabs, entitled "GL59728: A Potent Allosteric Inhibitor of the HCV NS5b RNA Dependent RNA Polymerase with Excellent Pharmacokinetic Properties."

GL59728 is one of a number of non-nucleoside HCV polymerase inhibitors discovered by Genelabs. In the presentation, Dr. Roberts outlined the lead optimization of certain non-nucleoside HCV polymerase inhibitors through an iterative process involving testing for potency in directly inhibiting HCV NS5b polymerase, inhibiting the replication of an HCV sub-genomic replicon, and pharmacokinetic properties.

The optimized lead that emerged from this chemistry approach, one of several taken by Genelabs, is known as GL59728. The IC50 of GL59728 for inhibition of the HCV NS5b polymerase is 16 nanomolar and the EC50 for inhibition of HCV replicon is 170 nanomolar. Further, GL59728 shows excellent oral bioavailability, exceeding 50% in all four species tested, including higher-order species, low clearance and a half-life consistent with once- or twice-daily dosing. The tissue distribution of GL59728 also appears favorable; since its concentration is enhanced several fold in liver, the site of HCV infection, relative to that obtained in plasma. Importantly, GL59728 was also tested in combination with other classes of HCV antiviral compounds, including a nucleoside chain terminator, a protease inhibitor and interferon alpha, and shown to be additive in activity with each.

In June 2006 Genelabs entered into a license and research co
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