Lexicon Presents Preclinical Data On LX2761, a New Clinical Candidate for Diabetes Designed to Reduce Glucose Absorption From Gastrointestinal Tract LX2761 Acts Locally in GI Tract to Inhibit Sodium Glucose Transporter 1

Data Published in Oral Presentation at the American Diabetes Association Meeting

THE WOODLANDS, Texas, June 24, 2013 /PRNewswire/ -- Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), a biopharmaceutical company focused on discovering breakthrough treatments for human disease, presented the first publication of data on LX2761 at the 73rd Scientific Sessions of the American Diabetes Association (ADA) in Chicago, on June 23, 2013.

David Powell, M.D., Lexicon's senior vice president of metabolism research, delivered an oral presentation titled "LX2761, an SGLT1 Inhibitor Restricted to the Intestine, Improves Glycemic Control in Mice."  Dr. Powell's presentation described the effects of LX2761 treatment on blood sugar control in mice with diabetes.

"LX2761 was designed to act locally in the gastrointestinal tract to reduce glucose absorption by inhibiting SGLT1 without any significant inhibition of SGLT2 in the kidney," said Alan Main, Ph.D., Lexicon's executive vice president of pharmaceutical research.  "This was accomplished through a dedicated medicinal chemistry effort to identify molecules with limited systemic exposure that showed efficacy in animal models of diabetes."

Consistent with design goals for an SGLT1 inhibitor without systemic exposure, LX2761 resulted in no urinary glucose excretion in mice while showing delayed intestinal glucose absorption and increased postprandial GLP-1 levels in mice, both alone and synergistically with the DPP-4 inhibitor sitagliptin. Notably, blood glucose excursions after an oral glucose challenge were still decreased 15 hours after oral LX2761 administration. Finally, LX2761 improved glycemic control in STZ-diabetic mice and in the KKAy mouse model of type 2 diabetes, as measured by reductions in hemoglobin A1c and oral glucose tolerance test results.

"We hope LX2761 may one day treat a large population of patients with diabetes, and potentially prediabetes, that may wish to avoid the urinary glucose excretion associated with SGLT2 inhibition in the kidney," said Brian Zambrowicz, Ph.D., executive vice president and chief scientific officer. "In addition, the synergy demonstrated with a DPP-4 inhibitor provides the mechanistic rationale to consider future combination therapies."

All presentations will be available for download from Lexicon's corporate website www.lexpharma.com.

About Lexicon

Lexicon is a biopharmaceutical company focused on discovering breakthrough treatments for human disease.  Lexicon currently has multiple programs in clinical development for diabetes, irritable bowel syndrome, carcinoid syndrome and other indications, all of which were discovered by Lexicon's research team.  Lexicon has used its proprietary gene knockout technology to identify more than 100 promising drug targets.  Lexicon has focused drug discovery efforts on these biologically-validated targets to create its extensive pipeline of clinical and preclinical programs.  For additional information about Lexicon and its programs, please visit www.lexpharma.com.

Safe Harbor Statement

This press release contains "forward-looking statements," including statements relating to Lexicon's preclinical development of LX2761 and the potential therapeutic and commercial potential of LX2761.  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 those relating to Lexicon's ability to successfully conduct preclinical and clinical development of LX2761 and its other potential drug candidates, advance additional candidates into preclinical and clinical development, obtain necessary regulatory approvals, 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, that may cause Lexicon's actual results to be materially different from any future results expressed or implied by such forward-looking statements.  Unless specifically indicated otherwise, results reported as trends were not statistically significant. 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, 2012, 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.

SOURCE Lexicon Pharmaceuticals, Inc.



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