SRT3025

SRT3025 is an experimental, orally available small molecule developed as a selective activator of the NAD-dependent deacetylase enzyme sirtuin 1 (SIRT1). It was originally studied by Sirtris Pharmaceuticals for potential therapeutic use in metabolic diseases such as insulin resistance and metabolic syndrome. Mechanistically, SRT3025 activates wild-type SIRT1 protein, leading to increased deacetylation of downstream targets such as hepatic p65 and skeletal muscle Foxo1. Preclinical studies have shown that it can decrease plasma LDL-cholesterol and total cholesterol levels, reduce atherosclerosis in animal models, inhibit RANKL-induced osteoclast differentiation (suggesting possible utility in osteoporosis), and expand hematopoietic stem cell populations with potential benefit for bone marrow failure syndromes like Fanconi anemia. The drug has undergone Phase 1 clinical trials to assess safety and pharmacokinetics in healthy volunteers but has not advanced further or received regulatory approval.