February 4, 2008
Potential new diabetes drugs enhance insulin secretion. Type 2 (adult onset) diabetes mellitus is a chronic disease that affects an estimated 5% of the population of the Western world. The disease is also becoming more common in developing countries such as China and India as people adopt the high-calorie diets and more sedentary lifestyles of many people in the industrialized West.
Type 2 diabetes is characterized by elevated levels of circulating blood sugar (hyperglycemia) and abnormalities in lipid and protein metabolism. Patients with Type 2 diabetes may have relatively low effective levels of circulating insulin, a protein hormone secreted by the pancreas that enables muscle cells to take up sugar from the blood stream. Left untreated, the disease can be fatal. Even if it is treated, it can result in life-threatening complications, including blindness, foot or leg amputations, and an increased risk for cardiovascular disease.
Current treatments for type 2 diabetes include diet and exercise, which help reduce blood sugar levels. People with advanced stages of the disease must take daily injections of insulin or its analogues. Therapeutic interventions used to treat patients in early stages of the disease include drugs that increase the sensitivity of muscle cells to the uptake of blood glucose, slow the adsorption of foods with high sugar contents, and increase the rate at which the pancreas secretes insulin.
Insulin secretagogues, drugs that increase the rate at which insulin is secreted from pancreatic islet cells, include sulfonylurea compounds such as 1. However, sulfonylureas have several drawbacks, including the risk of hypoglycemia, the difficulty of achieving normal glycemia in some patients, a 5–10%/year secondary failure rate of adequate glycemic control, and possible negative effects on the cardiovascular system.
Inventors B. Fischer, V. Kleiman-Nahum, and P. Petit describe new compounds that act as secretagogues, including 2-methylthioadenosine 5’-O-1-boranotriphosphate (2). In vitro testing of these compounds demonstrates that they can increase the rate of insulin secretion from rat pancreatic cells.
Future work in this area will likely include testing these compounds in animal models to determine their toxicity and efficacy as treatments for controlling type 2 diabetes. (Bar-Ilan University [Ramat-Gan, Israel]; University of Montpellier [France]. U.S. Patent 7,319,093, Jan 15, 2008; John Emanuele)
[See also Noteworthy Chemistry for January 28 for another promising new type 2 diabetes drug.—Ed.]
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