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GNLB Presents Preclinical Data on Non-
Nucleoside HCV Polymerase Inhibitor

[It would be easy to dismiss GNLB as an also-ran in the HCV arena were it not for one thing: they have a partnership with NVS, inked in 2006, to develop a non-nuke polymerase inhibitor for HCV. This is the same class of drug as HCV-796 from VPHM and WYE. The purpose of working on this drug class is to combine it with a nuke and/or a protease inhibitor, similar to what has been done in the treatment cocktails for HIV.]

http://biz.yahoo.com/prnews/070502/sfw098.html?.v=82

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

Wednesday May 2, 7:00 pm ET

REDWOOD CITY, Calif., May 2 /PRNewswire-FirstCall/ -- Genelabs Technologies, Inc. (Nasdaq: GNLB ) 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 collaboration with Novartis covering Genelabs' non-nucleoside HCV polymerase inhibitors.

"The data presented today clearly support the further investigation of non-nucleoside polymerase inhibitors for the future treatment of HCV infection," said Ronald C. Griffith, Ph.D., Genelabs' Chief Scientific Officer. "Furthermore, we believe future treatment of HCV is likely to involve combinations of antiviral drugs and these data suggest that combinations of this type of non-nucleoside agent with interferon or other likely therapeutic drugs, such as nucleoside chain terminators or protease inhibitors, may be feasible."

About Genelabs Technologies

Genelabs Technologies, Inc. is a biopharmaceutical company focused on the discovery and development of pharmaceutical products to improve human health. We have built drug discovery capabilities that can support various research and development projects. Genelabs is currently concentrating these capabilities on discovering novel compounds that selectively inhibit replication of the hepatitis C virus and advancing preclinical development of compounds from this hepatitis C virus drug discovery program, while also developing a late-stage product for lupus. We believe that these high-risk, potentially high reward programs focus our research and development expertise in areas where we have the opportunity to generate either first-in-class or best-in-class products that will address diseases for which current therapies are inadequate. For more information, please visit www.genelabs.com.
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