Small molecule could hold the key to diabetes' pill

January 4, 2007 - 0:0
CHICAGO (AFP) -- Chinese researchers have identified a compound that controls diabetes in mice and may point the way to more user-friendly treatments for the most common type of human diabetes, a study said.

The compound has only been tested in mice so far, but if it were shown to be effective in humans, it could be turned into a drug, replacing less user-friendly medicines that need to be injected twice a day, the authors of the study said.

"We are seeking pharmaceutical partners so we can develop this lead," said Ming-Wei Wang, director of China's National Center for Drug Screening in Shanghai, and lead author of the study.

Researchers at the center identified the molecule -- Boc5 -- after screening thousands of substances to find ones with properties similar to one of the body's own glucose-regulating gut hormones, called GLP-1, in an "orally available" form.

GLP-1 has been shown to normalize glucose levels in diabetic patients, but because its efficacy diminishes quickly with time, the drug industry has focused its attention on a class of agents that mimic the effects of the hormone but are longer-acting.

In 2005, Amylin Pharmaceuticals and Eli Lilly and Company began marketing the first of these so-called "incretin mimetic" medications for type II, or adult-onset diabetes.

The medicine, called Byetta, helps diabetes patients manage their blood sugar levels by stimulating the pancreas to produce insulin after a meal and slowing the rate at which food and glucose leave the stomach, preventing glucose spikes after a meal. Byetta has also been shown to curb appetite and help with weight loss in some patients, but it is only available as an injection, which may be a deterrent for some patients, so researchers have continued to hunt for compounds that act like GLP-1, but are "orally available."

In lab tests and tests on diabetic mice, Boc5 increased insulin sensitivity (the ability to metabolize glucose), reduced cholesterol levels, and curbed appetite, according to the study in the Proceedings of the National Academy of Sciences (PNAS).

After a month on Boc5, the diabetic mice performed the same as the control mice on a test to measure long-term serum glucose regulation, and after a month on high-dose Boc5, the diabetic mice had lost at least 20 percent of their body weight.

A compound that controls diabetes in mice, and that could be produced in pill form, might one day take some of the pain out of managing the most common form of human diabetes.