BioEnergenix, through a team of experienced drug hunters, medicinal chemists, pharmacologists, and regulatory consultants, is developing first-in-class orally-active PAS kinase inhibitors for the treatment of dyslipidemia and other facets of the metabolic syndrome.  5 million in the United States have severe hypertriglyceridemia (circulating triglycerides > 500 mg/dL) with serious risk of acute pancreatitis (in addition to atherosclerosis), and standard-of-care medications (i.e. Omega 3 fatty acids) are ineffective.  BioEnergenix has discovered numerous highly potent and selective small molecule inhibitors of PAS kinase, a cellular nutrient sensor which drives dyslipidemia, hepatic steatosis, and insulin resistance when mis-regulated.  Our lead development candidate is BioE1115, an orally-active nanomolar-potent and highly-selective inhibitor of PAS kinase.  In rodent models of metabolic disease, BioE1115 lowers triglycerides (far superior to Omega 3 fatty acids), and restores insulin sensitivity (comparable to glitazones in oral glucose tolerance tests).  Favorable pharmacology and beneficial effects in animal disease models suggest that BioE1115 could be an attractive treatment option for patients with various aspects of the metabolic syndrome, particularly hypertriglyceridemia.  BioE1115 has a clean in vitro pharmacology profile, and GLP toxicology/safety studies are currently in progress.


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