Research published in Nature by Sirtris scientists is first demonstration in
mammals that resveratrol, a sirtuin activator, can treat diseases of aging, such as diabetes

CAMBRIDGE, Mass.--(BUSINESS WIRE)--Sirtris Pharmaceuticals, the leading sirtuin therapeutics company, announced today that SRT501, its initial clinical candidate which is a proprietary formulation of resveratrol with improved bioavailability, has been administered to patients with Type 2 diabetes in a human Phase 1b clinical study. Sirtris is studying SRT501 as a drug candidate for Type 2 diabetes, based in part on the scientific evidence that sirtuin activation, by means of compounds like resveratrol, has been shown to have a positive effect on key clinical measures for diabetes. In an article published today in Nature, “Resveratrol improves health and survival of mice on a high-calorie diet,” resveratrol was shown in mice to promote normal cellular function and extend healthy lifespan, including an increase in insulin sensitivity, a decrease in insulin growth factor-1 levels, and an increase in the number of cellular mitochondria. The authors of the Nature article include principal investigator David Sinclair, Ph.D., Associate Professor of Pathology and Co-Director of the Paul F. Glenn Laboratories for the Biological Mechanisms of Aging at Harvard Medical School and co-founder and Board member of Sirtris, and Olivier Boss, Ph.D., Associate Director of Pharmacology at Sirtris.

“This study indicates that SIRT1 is associated with extension of healthy lifespan in obese mice and if this is translated into humans, it could have an enormous impact on medicine.” said David Sinclair. “I believe that the measures of health improvement in this study, such as increased insulin sensitivity and decreased IGF-1 levels, show the potential for sirtuin activation to treat metabolic diseases, such as diabetes.”

SRT501 is the first small molecule to enter human clinical trials that is designed to target SIRT1, the best characterized of the recently-discovered family of sirtuin enzymes. Activation of SIRT1 is believed to be a key pathway by which resveratrol regulates such processes as glucose and insulin production, fat metabolism, and cell survival. Sirtris has applied this scientific discovery to the development of SRT501, which activates SIRT1, for the treatment of diseases of aging such as metabolic and mitochondrial disorders. In addition, Sirtris has a robust pipeline of small molecule drug candidates that are potent SIRT1 activators and are chemically distinct from resveratrol.

“Based on the continuing scientific evidence, as shown in this most recent Nature article, we are continuing to advance drug candidates, such as SRT501, to translate the science of sirtuins into new treatments for diseases of aging, such as diabetes,” said Christoph Westphal, M.D., Ph.D., Chief Executive Officer of Sirtris Pharmaceuticals. “We are excited about the ability of SRT501 to activate SIRT1 as a potential treatment for diabetes. In addition, we are developing a strong pipeline of sirtuin activators that are more potent and are targeted for a broad range of diseases of aging.”

Sirtris has exclusively in-licensed from Harvard University a broad portfolio of intellectual property relating to the therapeutic potential of activating sirtuins, largely based on the work of Dr. David Sinclair. In the current human clinical study of SRT501, Sirtris has designed this Phase 1b trial to evaluate the safety and pharmacokinetics of SRT501 in 90 patients with Type 2 diabetes using daily oral administration of SRT501 for 28 days.

Online copies of the article can be obtained at http://www.nature.com/.

About Sirtuins

Sirtuins are a recently discovered family of enzymes that promote normal cellular function. In particular, sirtuins improve the function of mitochondria which generate energy in cells. When organisms face adversity, sirtuins are activated as part of a natural process that maintains healthy function.

Therefore, sirtuins are attractive drug targets which may be therapeutically beneficial for diseases in which mitochondria are dysfunctional, often observed in diseases of aging. These diseases include metabolic diseases such as Type 2 Diabetes and other mitochondrial disorders. Sirtuin therapeutics offer the potential for a novel class of drugs that can treat significant diseases of aging in a new way.

About Sirtris Pharmaceuticals

Sirtris Pharmaceuticals is a biopharmaceutical company developing novel therapeutics that modulate sirtuins. Sirtris has the dominant sirtuin intellectual property estate and know-how with a comprehensive suite of reagents, proprietary assays, transgenic animal models, and biomarkers. Sirtris is building a robust pipeline of therapeutics for diseases of aging in the areas of metabolic and mitochondrial diseases.

Sirtris Pharmaceuticals was founded in 2004 by Rich Aldrich, Richard Pops, Paul Schimmel, David Sinclair and Christoph Westphal and has raised a total of $82 million since inception from investors including: Bessemer Venture Partners, Cardinal Partners, Cargill Ventures, Genzyme Ventures, Novartis Bioventures Fund, Polaris Venture Partners, QVT Fund LP, Skyline Ventures, The Wellcome Trust, Three Arch Partners, and TVM Capital. The company's headquarters are in Cambridge, Massachusetts. For additional information, please visit http://www.sirtrispharma.com.