Intercept Pharmaceuticals, Inc. (Intercept) and Les Laboratoires Servier (Servier) announced that they have entered into a worldwide ex-US and Japan agreement for the discovery and development of novel TGR5 agonists for the treatment of type 2 diabetes and other metabolic indications. The collaboration will leverage Intercept's drug discovery platform based on its proprietary bile acid analogue chemistry and expertise targeting TGR5 and other bile receptors.

Under the terms of the agreement, Intercept will receive up to $ 163 million in total upfront, research support and milestone payments, as well as royalties on sales, based on the successful outcome of the collaboration. Intercept and Servier will jointly support the discovery effort, while Servier alone will be responsible for all costs associated with the global development, regulatory approval and commercialization of any compound selected as a lead candidate by the parties. Intercept retains all rights in the US and Japan.

“This agreement provides important validation of our approach to targeting TGR5,” said Mark Pruzanski, MD, Intercept's president and chief executive officer. “Type 2 diabetes and associated metabolic disorders have reached epidemic proportions globally and there is a critical need for novel effective and safe drugs. Intercept is uniquely positioned to exploit the therapeutic potential of rationally modified bile acids, which play a central role in the maintenance of metabolic homoeostasis. I am thrilled to enter this agreement with Servier given the company's commitment to research and expertise in this therapeutic area.”

“We are very happy to enter into this collaboration with Intercept which will allow us to further expand our diabetes and metabolic disease franchise,” stated Emmanuel Canet, MD, PhD, Head of Servier R&D. “TGR5 is a target of great interest with its effects on GLP-1 that complement those of other classes of marketed diabetes drugs.”

TGR5 (GPR131) is a cell-surface G protein coupled receptor that is regulated by bile acids. Bile acids are known to be key regulators of lipid, glucose and overall energy metabolism. This receptor has been shown to be a key regulator of energy homoeostasis through induction of the incretin GLP-1 in the intestine with resulting insulin sensitizing effects, as well as through activation of metabolic pathways in brown adipose tissue and skeletal muscle that drive energy expenditure and resulting resistance to weight gain. TGR5 is also involved in the modulation of cytokine production by immune cells, potentially playing a role in the control of inflammation.

Intercept is a biotechnology company focused on discovering and developing small molecule drugs for the treatment of chronic liver and metabolic diseases.

Servier is the leading independent pharmaceutical company with its main therapeutic products treating type II diabetes, cardiovascular diseases, CNS disorders, oncology and rheumatological diseases.