Metabolex and Sanofi-Aventis announced today that they have entered into a global license and development agreement for the research, development, manufacture and commercialization of small molecules that modulate the G-protein coupled receptor 119 (GPR119), a receptor in the gut and pancreas that interacts with bioactive lipids to stimulate glucose-dependent incretin and insulin secretion. Agonists of GPR119 represent a first-in-class oral treatment for type 2 diabetes that function through a unique dual mechanism of action. First, they act directly on the pancreatic beta cell to increase insulin secretion. In addition, they stimulate release of the incretin GLP-1 from the intestines. This unique dual action may offer improved glucose homeostasis over existing diabetes therapies, with the potential for weight loss and improved islet health.

The agreement includes MBX-2982, a potent selective orally active GPR119 agonist discovered by Metabolex. MBX-2982 has completed three Phase 1 clinical studies and has consistently shown clinically meaningful glucose reductions in healthy volunteers and subjects with impaired glucose tolerance. In all of these studies, MBX-2982 was found to be safe and well tolerated. MBX-2982 is currently in a multi-national 28-day Phase 2 clinical study in patients with type 2 diabetes.

Under this agreement, Metabolex will receive an upfront payment and will be eligible to receive development, regulatory, and specified commercial milestones that total as much as $375 Million. Metabolex is also eligible to receive royalties on worldwide sales of marketed products.

“We are excited about working with Sanofi-Aventis on this exciting new therapy for type 2 diabetes,” said Harold Van Wart, president and CEO of Metabolex. “Sanofi’s clear strategic commitment to the field of diabetes makes them the ideal partner to maximize the significant potential of this compound and provide an exciting new therapeutic option for diabetes patients.”