Grant: Proof of Principle Program - Phase I

Type-2 diabetes affects nearly 300 million people worldwide with a staggering $3 trillion in associated health costs in North America alone. Unfortunately, currently available drugs lack long-term effectiveness and need to be used in combination of 2 or more drugs, and often lead to the damage of insulin making beta cells. Thus, most patients end up taking insulin, which it self has several associated problems, including hypoglycemia, frequent blood glucose monitoring and weight gain. An ideal drug for type-2 diabetes would enhance insulin secretion by the beta cells in response to glucose, increase the sensitivity of body tissues to insulin and also block the excess glucose production by liver. We have discovered that inhibition of a specific enzymatic step in a metabolic pathway called glycerolipid/ free fatty acid cycling, is able to achieve at least two of these goals without causing any toxicity to pancreatic beta cells and also to animals. This is an entirely novel concept and our results are protected by a recently filed PCT application and we do not anticipate any immediate competition in this area. Thus, we believe that our discovery offers unique opportunity to widen the scope of our preliminary findings for identifying New Chemical Entities that specifically inhibit this enzymatic step and developing them as effective type-2 diabetes therapeutics.