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BIOIO-1001 is a first-in-class small molecule insulin sensitizer developed by BIOIO. It was discovered using the company's proprietary Mechanism of Action Technology (MOAT) platform. The drug targets a unique NAD+-dependent pathway, specifically modulating Sirtuin 3 (SIRT3), and activates the NMNAT-Sirt3 axis to improve mitochondrial health. Unlike existing metabolic drugs such as fibrates, glitazars, and thiazolidinediones, BIOIO-1001 induces fatty acid oxidation without relying on PPARs. This mechanism restores cellular energy balance and enhances metabolic flexibility, resulting in significant insulin sensitization. Preclinical studies have shown that BIOIO-1001 improves markers of steatosis and heart failure in models of diabetes and reduces inflammation and fibrosis characteristic of non-alcoholic steatohepatitis (NASH). Additionally, it has demonstrated protective effects in amyotrophic lateral sclerosis (ALS) models by increasing lifespan and delaying paralysis onset. The compound acts at the intersection of mTOR/insulin signaling and NAD+ pathways—two core aging pathways—making it a promising gerotherapeutic for multiple age-related diseases including type 2 diabetes mellitus (T2DM), NASH, and ALS[1][2][3][4].
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