First U.S. Patent Issued On Class Of SIRT1 Activators, Which Lower Glucose And Improve Insulin Sensitivity In Preclinical Models Of Type 2 Diabetes

Main Category: Diabetes
Article Date: 21 Mar 2008 - 10:00 PDT

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Sirtris Pharmaceuticals, Inc. (NASDAQ: SIRT), a biopharmaceutical company focused on discovering and developing small molecule drugs to treat diseases of aging such as Type 2 Diabetes, announced today that the United States Patent Office issued to Sirtris the first patent covering a broad class of compounds that activate the enzyme SIRT1. Several Sirtris compounds - or new chemical entities (NCEs) - from this class lower glucose and improve insulin sensitivity in preclinical models of Type 2 Diabetes. The patent covers the first NCE that Sirtris plans to take into a human clinical safety trial in the first half of 2008.

"Just five months ago in the publication Nature, we reported the identification of new chemical entities that lower glucose and improve insulin sensitivity in preclinical models that the FDA - in recent draft guidance - recommended for the development of Type 2 Diabetes drugs," says Christoph Westphal, M.D., Ph.D., Chief Executive Officer and Vice Chair of Sirtris Pharmaceuticals. "We are very pleased to have the first patent covering a class of compounds that have the potential to be a frontline therapy for Type 2 Diabetes."

"Sirtris has a strong intellectual property program with over 180 patent applications for broad coverage of sirtuin activators, including composition of matter, formulations, and methods of treatment claims," says Karl Normington, Ph.D., Senior Director of Intellectual Property at Sirtris Pharmaceuticals. "This is the first patent issued by the U.S. Patent Office covering a class of compounds known to activate SIRT1."

In 2006, consecutive papers in the journals Cell and Nature by Sirtris scientists and Sirtris co-founder David Sinclair, Ph.D. of Harvard Medical School, showed that resveratrol, a SIRT1 activator found in red wine, could reduce the impact of a high fat diet, increase stamina two fold and significantly extend lifespan of mice. However, it is estimated that a person would need to drink roughly 1000 bottles of red wine per day to obtain the equivalent dose of resveratrol used in these studies. Sirtris has developed SIRT1 activating molecules that are chemically distinct from, and up to 1000 times more potent in in-vitro studies than resveratrol.

The sirtuins are a family of seven enzymes that help regulate the body's natural defense against disease. In preclinical research, members of the sirtuin family have been shown to have protective effects against various diseases such as Type 2 Diabetes, metabolic diseases, cardiovascular disease, neurodegeneration, inflammation and cancer. Future sirtuin therapeutics may have the potential to treat diseases of aging in a new way.

About Sirtris Pharmaceuticals

Sirtris Pharmaceuticals is a biopharmaceutical company focused on discovering and developing proprietary, orally available, small molecule drugs with the potential to treat diseases associated with aging, including metabolic diseases such as Type 2 Diabetes. Our drug candidates are designed to mimic certain beneficial health effects of calorie restriction, without requiring a change in eating habits, by activation of sirtuins, a recently discovered class of enzymes that the Company believes control the aging process. The Company's headquarters are in Cambridge, Massachusetts.

This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Such statements include, but are not limited to, the potential therapeutic effects of sirtuins and SIRT1 activators, including novel chemical entities and SRT501, for diseases of aging, such as Type 2 Diabetes; the progress and potential results of preclinical and clinical studies of SIRT1 activators; the success of SIRT1 activators as therapies for diseases, such as Type 2 Diabetes; and the potential of sirtuin modulators to receive regulatory approval. These forward-looking statements about future expectations, plans and prospects of Sirtris Pharmaceuticals involve significant risks, uncertainties and assumptions, including risks related to the lack of results that would provide a basis for predicting whether any of the Company's product candidates will be safe or effective, or receive regulatory approval, the possibility that results of pre-clinical studies are not necessarily predictive of clinical trial results, the Company's potential inability to initiate and complete pre-clinical studies and clinical trials for its product candidates, the fact that none of the Company's product candidates has received regulatory approvals, the potential inability of the Company to gain market acceptance of the Company's product candidates, and those other risks factors that can be found in the Company's filings with the Securities and Exchange Commission. Actual results may differ materially from those Sirtris Pharmaceuticals contemplated by these forward-looking statements. Sirtris Pharmaceuticals does not undertake to update any of these forward-looking statements to reflect a change in its views or events or circumstances that occur after the date of this release.

http://www.sirtrispharma.com