Metabolex Initiates Phase 1 Trial o...( - Potential First-in-Class T...),Health

- Potential First-in-Class Treatment for Type 2 Diabetes -

HAYWARD, Calif., March 26 /PRNewswire/ -- Metabolex, Inc., a biopharmaceutical company focused on the discovery and development of proprietary new medicines for the treatment of metabolic diseases, announced today that it has dosed the first cohort of healthy subjects in a Phase 1 clinical trial of MBX-2982, a potential first-in-class treatment for type 2 diabetes.

The Phase 1 clinical trial will evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic profile of MBX-2982. Investigators expect to enroll a total of 60 healthy volunteers in the 6-cohort ascending-dose study.

MBX-2982 is an agonist of GPR119, a G-protein coupled receptor (GPCR) that is expressed in pancreatic islets and the gastrointestinal tract. Pre-clinical studies conducted by Metabolex and others show that GPR119 agonists can stimulate glucose-dependent insulin secretion and may preserve beta cell health -- properties that mimic incretins such as GLP-1, and exenatide (a GLP-1 analogue marketed as Byetta(R)). Unlike exenatide, however, MBX-2982 can be delivered orally. In addition, MBX-2982 may provide additional benefit when used in combination with a DPP-4 inhibitor such as sitagliptin (Januvia(R)), or other oral therapies.

"We have identified a number of potent GPR119 agonists that improve glucose control in normal and diabetic animal models," said David B. Karpf, MD, chief medical officer of Metabolex. "Advancing MBX-2982 into Phase 1 represents a significant achievement in the expansion of our clinical pipeline and further validates our research and development capabilities."

About Diabetes

Diabetes is a worldwide health problem and a rapidly growing source of illness, death and health care costs. According to the International Diabetes Federation, approximately 230 million people, or almost 6 percent of the world's population, had diabetes in 2006. The American Diabet
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