Sirtris Pharmaceuticals has completed dosing 85 subjects in a Phase I safety and pharmacokinetic trial of SRT501. SRT501 is the first small molecule designed to target SIRT1, a member of the human sirtuin family of enzymes. Specifically, SRT501 acts by increasing mitochondrial activity, and is thus therapeutically targeted to address metabolic diseases like diabetes and obesity.
There are seven human sirtuins, each having a different sub-cellular localization. Critical to the survival of organisms in adverse conditions, sirtuins are fundamental in the biological processes of most life forms. Sirtuins are attractive drug targets since some have a specialized function in mitochondrial activity, which may be therapeutically beneficial for metabolic and neurological diseases. By harnessing a natural process, sirtuin therapeutics offer the potential for a novel class of drugs that can treat significant diseases of aging.