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^®). 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^®), 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."

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 Diabetes Association estimates that there were approximately 20.8 million people in the United States with diabetes in 2005, making up 9.6 percent of the adult population. From 1995 through 2005, newly-diagnosed cases of diabetes among American adults increased by 81 percent. According to estimates from the ADA, approximately 11 percent of U.S. healthcare dollars are spent on treating diabetes. Type 2 diabetes accounts for roughly 90 to 95 percent of diabetic cases.

Metabolex is a privately-held biopharmaceutical company focused on the discovery and development of proprietary new medicines for the treatment of metabolic diseases, with an emphasis on type 2 diabetes. Metabolex has drawn on its deep understanding of diabetes to create a large database of genes involved in diabetes and to build a rich pipeline of product candidates and drug discovery targets. The company has four clinical-stage compounds: MBX- 102/JNJ 39659100, which has recently completed a Phase 2/3 trial; MBX-2044, which has completed a Phase 2a trial; MBX-8025, currently being studied in a Phase 2 trial in patients with dyslipidemia; and MBX-2982, which has just commenced a Phase 1 trial. Ortho-McNeil, Inc. has the exclusive right to develop and commercialize MBX-102/JNJ 39659100.