ENT-03: A Novel Drug for Obesity and Type 2 Diabetes

ENT-03 is a centrally-acting endogenous steroidal molecule (spermine-bile acid) that regulates whole-body responsiveness to insulin, energy homeostasis and body weight.

  • Potent inhibitor of PTP1b, an established Obesity and Type 2 Diabetes target

  • Rapidly induces weight loss, normalizes glucose and restores insulin senstitivity

  • May be used as monotherapy or in combination with GLP-1’s

  • Administered subcutaneously weekly

  • Preserves lean muscle mass in comparison to GLP-1s

  • Sustained effect weight loss and glucose control after therapy cessation

Obesity is prevalent in almost 38% of US adults and type 2 diabetes (T2D) affects approximately 9% of US adults. Obesity reduces lifespan and increases the risk of cardiovascular disease, T2D, Metabolic Dysfunction-Associated Steatohepatitis (MASH), and hypertension. The cost of healthcare, caregiving, and hospice care exceeds $290 billion annually in the US, expected to increase to $1.1 trillion by 2050.

In animal studies with ENT-03, we have observed a rapid increase in insulin sensitivity and normalization of blood glucose levels prior to any weight loss. The treated animals had reduced food intake and lost significant amounts of weight, which was maintained for several months after treatment. Consequently, ENT-03 could be used as a stand-alone drug, or in combination with GLP-1 agonists which increase pancreatic insulin secretion and suppress eating behavior including interest in calorie rich foods.