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Two New HCV Polymerase Inhibitors: early study data show potency & perhaps once daily dosing
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Press Release Source: Genelabs Technologies, Inc.
Genelabs Presents Data on Two Preclinical Candidates at the 12th International Symposium on Hepatitis C and Related Viruses
Monday October 3, 8:00 am ET
REDWOOD CITY, Calif., Oct. 3 /PRNewswire-FirstCall/ -- Genelabs Technologies, Inc. (Nasdaq: GNLB - News) announced the presentation of data on two internally-developed hepatitis C virus (HCV) preclinical development candidates at the 12th International Symposium on Hepatitis C and Related Viruses in Montreal. Genelabs preclinical development candidates GL59728 (728) and GL60667 (667) are highly potent inhibitors of the hepatitis C replicon, demonstrating inhibitory concentrations of 170 and 37 nanomolar, respectively, and 16 and 28 nanomolar for inhibition of the HCV polymerase. Compounds 728 and 667 are both non-nucleoside HCV polymerase inhibitors, although the discovery of each resulted from optimization of distinctly different chemotypes. Because of this structural distinction, as well as certain advantages inherent to each, Genelabs believes that both merit further development. Compound 667, in particular, is a member of a large class of closely related compounds discovered by Genelabs, a number of which appear to be among the most potent inhibitors of the HCV polymerase yet described.
In addition to the potency data presented at the symposium in Montreal, Genelabs presentation also noted that the compounds have demonstrated good DMPK (drug metabolism and pharmacokinetic) properties in multiple species -- mice, rats, monkeys and dogs. For example, the canine data showed that the compounds had half-lives of 5.1 and 3.2 hours, with oral bioavailability of 56% and 47% for compounds 728 and 667, respectively. Based on this data, Genelabs believes that these compounds may be suitable for once-a-day dosing, which would provide a competitive advantage over other published compounds currently in development as inhibitors of the hepatitis C virus polymerase.
Recently, Genelabs completed 1-day and 7-day sub-acute toxicity studies in two different species. Based on the safety profile for both compounds from interim data from these studies, and their favorable potency and DMPK attributes, both compounds have thus far met Genelabs' criteria for advancement into IND-enabling preclinical studies. Genelabs retains all rights to both of the preclinical development candidates presented.
About Hepatitis C
The Hepatitis C virus is an infectious and potentially fatal virus that can be contracted through blood and bodily fluid contact. The virus attacks the liver and can cause liver inflammation, liver scarring, liver failure and liver cancer. In most cases, the body is not able to fight off the infection and the infected individual becomes a chronic carrier of HCV. According to the World Health Organization, as many as 170 million people worldwide have chronic HCV infection. The United States Centers for Disease Control and Prevention estimates that approximately 2.7 million people in the United States are chronically infected with HCV and that each year there are approximately 25,000 new cases of HCV infection and approximately 8,000 to 10,000 deaths from hepatitis C complications. Liver failure resulting from chronic HCV infection is now recognized as the leading cause of liver transplantation in the United States. The current standard of care for treatment of HCV is a combination of pegylated interferon alpha and the nucleoside analogue ribavirin, typically given over a number of months, with interferon injected once weekly and ribavirin given orally once daily. This treatment regimen is effective only in approximately 50% of patients infected with HCV genotype 1, the genotype most prevalent in the United States. The interferon/ribavirin treatment has significant toxicities, most importantly severe anemia and psychiatric effects. There are no other drugs or biologics approved by the FDA for treatment of HCV. As a consequence, the pool of patients continues to grow.
About Genelabs
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 and clinical development capabilities that can support various research and development projects. Genelabs is currently concentrating its capabilities on developing a late-stage product for lupus, 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. 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.
NOTE: Genelabs® and the Genelabs logo are registered trademarks of Genelabs Technologies, Inc.
NOTE ON FORWARD LOOKING STATEMENTS AND RISKS:
Genelabs cautions that compounds in preclinical studies are at an early stage of development and there is no assurance that any of these compounds will successfully pass all the requirements necessary for studies in humans. This press release contains forward-looking statements including statements regarding the progress of Genelabs' hepatitis C virus research programs, the potency of compounds being developed by Genelabs and elsewhere, and the potential future properties of the compounds. These forward-looking statements are based on Genelabs' current expectations and are subject to uncertainties and risks that could cause actual results to differ materially from the statements made. Uncertainties and risks include, without limitation, failures or setbacks in our HCV research programs or in our collaboration with Gilead Sciences, Inc.; progress and announcements by competitors regarding their HCV programs; de-listing from the Nasdaq National Market; fluctuations in Genelabs' stock price; events which reduce Genelabs' future prospects; unexpected expenses and Genelabs' capital requirements and history of operating losses. Please see the information appearing in the Genelabs' filings with the Securities and Exchange Commission, including our most recent Annual Report on Form 10-K, under the captions "Risk Factors" and "Forward- Looking Statements," for more discussion regarding these uncertainties and risks and others associated with the company's research programs, early stage of development and other risks which may affect the company or cause actual results to differ from those included in the forward-looking statements. Genelabs does not undertake any obligation to update these forward-looking statements or risks to reflect events or circumstances after the date of this release.
Source: Genelabs Technologies, Inc.
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