New Oral, Small Molecule Investigational Drug Is Designed to Inhibit SGLT1 in the GI Tract with Minimal Systemic Absorption

THE WOODLANDS, TX, USA I January 9, 2016 I Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX) announced today the commencement of dosing in a Phase 1 clinical trial of LX2761, an orally-delivered small molecule compound for the potential treatment of diabetes.  LX2761 is an internally generated compound and is designed to inhibit SGLT1 locally in the gastrointestinal tract without any significant inhibition of SGLT2 in the kidney.  

“Building on science relating to the importance of the gastrointestinal tract in diabetes and Lexicon’s work around the SGLT1 target, LX2761 provides an approach to glycemic control that is focused on local action in the GI tract with minimal systemic absorption,” said Praveen Tyle, Ph.D., Lexicon’s executive vice president of research and development.  “LX2761 is a potent, locally-acting SGLT1 inhibitor that may help patients achieve greater glycemic control without the significantly-elevated urinary glucose excretion that characterizes inhibitors of SGLT2.”

In preclinical studies, LX2761 delayed and reduced intestinal glucose absorption and reduced postprandial glucose, the level of blood glucose after a meal, while increasing plasma levels of GLP-1, consistent with inhibition of intestinal SGLT1.  In addition, LX2761 was minimally absorbed into the systemic circulation, resulting in little effect on urinary glucose excretion, indicating that LX2761 was restricted to the gastrointestinal tract.  The initial Phase 1 clinical trial of LX2761 is planned as a double-blind, randomized, placebo-controlled, ascending single dose study in both healthy volunteers and people with type 2 diabetes.  The study is designed to evaluate the safety and tolerability of LX2761.  Lexicon has granted Sanofi certain rights of first negotiation with respect to the future development and commercialization of LX2761.

About Lexicon

Lexicon is a fully integrated biopharmaceutical company that is applying a unique approach to gene science based on Nobel Prize-winning technology to discover and develop precise medicines for patients with serious, chronic conditions. Through its Genome5000™ program, Lexicon scientists have studied the role and function of nearly 5,000 genes over the last 20 years and have identified more than 100 protein targets with significant therapeutic potential in a range of diseases. Through the precise targeting of these proteins, Lexicon is pioneering the discovery and development of innovative medicines to safely and effectively treat disease. Lexicon has a pipeline of promising drug candidates in clinical and pre-clinical development in oncology, diabetes and metabolism, and neuropathic pain. For additional information please visit www.lexpharma.com.

SOURCE: Lexicon Pharmaceuticals