Drugs Fut 2009, 34(4): 291
- DOI:
http://dx.doi.org/10.1358/dof.2009.034.04.1360696
Resveratrol/SRT-501
Elliott, P.J., Walpole, S., Morelli, L., Lambert, P.D., Lunsmann, W., Westphal, C.H., Lavu, S.
The consumption of resveratrol, a naturally occurring polyphenol found in foods, has been associated with possible health benefits. These benefits are derived, in part, from activation of NAD-dependent deacetylase sirtuin-1 (SIRT1), an enzyme thought to control the aging process in multiple species. To date, the activation of SIRT1 by resveratrol has been suboptimal due to its poor bioavailability, limiting the full treatment potential of SIRT1 activation. We have developed a novel formulation of resveratrol, SRT501, with improved bioavailability. The present report describes the safety and pharmacokinetic profile in animals and humans, as well as the glucose-lowering activity of once- and twice-daily dosing schedules of SRT501 in type 2 diabetic patients. Our results demonstrate that SRT501 was safe and well tolerated in multiple preclinical toxicity studies and in clinical trials involving healthy normal volunteers and type 2 diabetes patients. The efficacy seen in animal models of diabetes appears to be replicated in type 2 diabetic patients, and as such it shows promise as a novel treatment for diabetes.
