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

The Woodlands, Texas, January 9, 2017 – 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

Safe Harbor Statement

This press release contains “forward-looking statements,” including statements relating to Lexicon’s and its licensees’ clinical development of and regulatory filings for LX2761 and the results and projected timing of clinical trials and the potential therapeutic and commercial potential of LX2761. In addition, this press release also contains forward-looking statements relating to Lexicon’s growth and future operating results, discovery and development of products, strategic alliances and intellectual property, as well as other matters that are not historical facts or information. All forward-looking statements are based on management’s current assumptions and expectations and involve risks, uncertainties and other important factors, specifically including the risk that clinical studies of LX2761 may be halted, delayed or otherwise not demonstrate safety or efficacy, the risk that the FDA and other regulatory authorities may not grant regulatory approval of LX2761 in accordance with Lexicon’s currently anticipated timelines or at all, and the risk that such regulatory approvals, if granted, may have significant limitations on the approved use of LX2761. As a result, LX2761 may never be successfully commercialized. Other risks include Lexicon’s ability to meet its capital requirements, successfully conduct preclinical and clinical development and obtain necessary regulatory approvals of its other potential drug candidates, achieve its operational objectives, obtain patent protection for its discoveries and establish strategic alliances, as well as additional factors relating to manufacturing, intellectual property rights, and the therapeutic or commercial value of its drug candidates. Any of these risks, uncertainties and other factors may cause Lexicon’s actual results to be materially different from any future results expressed or implied by such forward-looking statements. Information identifying such important factors is contained under “Risk Factors” in Lexicon’s annual report on Form 10-K for the year ended December 31, 2015, as filed with the Securities and Exchange Commission. Lexicon undertakes no obligation to update or revise any such forward-looking statements, whether as a result of new information, future events or otherwise.