TRANSFORMATIONAL SCIENCE

Until now, no medication for obesity and related diseases has utilized the master metabolic regulatory switch to address the core issue of calorie excess. Sterol Regulatory Element-Binding Proteins (SREBPs) are a family of transcription factors that influence many genes in the pathways of fat synthesis and fat oxidation. SREBP inhibition or activation controls the master regulatory switch leading to fat oxidation or fat synthesis. Our technology promotes utilization of calories, subsequent weight loss and significant improvements in markers of altered metabolism toward a healthy metabolic state.

INNOVATION

FGH BioTech identified small molecules that regulate SREBP transcription factors. In rodents fed a high fat, high carbohydrate diet, these small molecules significantly lower body weight compared to untreated animals and preserve lean body mass. Treated animals demonstrate improved plasma levels of glucose, total cholesterol, LDL-cholesterol, triglycerides and enhance insulin sensitivity. Gene analysis shows suppression of fat synthesis and activation of fat oxidation pathways. Liver histology demonstrates dramatic improvement or resolution of fatty liver in treated animals.

These molecules block fatty acid, triglyceride and cholesterol synthesis, while popular statin drugs only block cholesterol production. Proposed therapies that signal through FXR agonists, PPAR alpha/gamma agonists, and fibroblast growth factor 19 all require SREBP inhibition as a necessary step for clinical effect.

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