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Lexicon Presents LX4211 Mechanism of Action Data at American Diabetes Association Meeting and Announces Commencement of Phase 2b Clinical Trial in Type 2 Diabetes

THE WOODLANDS, Texas, June 27, 2011 /PRNewswire/ -- Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), a biopharmaceutical company focused on discovering breakthrough treatments for human disease, announced today that the company presented clinical data from a mechanistic study of LX4211, a dual inhibitor of sodium glucose transporters 1 and 2 (SGLT1 and SGLT2), in patients with type 2 diabetes at the 71st Scientific Sessions of the American Diabetes Association (ADA) in San Diego, California.  In addition, the company announced that it has commenced enrollment of patients with type 2 diabetes in its Phase 2b clinical trial of LX4211.

Data from the mechanistic study demonstrated that a single dose of LX4211 significantly increased circulating levels of GLP-1 (active and total) and PYY, important regulators of glycemic and appetite control.  For more information on this program or to download a copy of the poster from the ADA meeting, please visit

The Phase 2b trial is a randomized, double-blind, placebo controlled study of LX4211 in approximately 285 adult patients (18-75 years) with type 2 diabetes who are not adequately controlled on metformin monotherapy.  Patients will be administered LX4211 in combination with standard metformin therapy over 12 weeks.  Doses will include 75 mg once daily, 200 mg once daily, 200 mg twice daily, 400 mg once daily or placebo.  The primary endpoint of the study is the change from baseline in HbA1c at Week 12.  Secondary endpoints will include percentage of patients achieving HbA1c < 7%, and changes in fasting plasma glucose, 3-hour glucose tolerance test, weight, blood pressure, and triglycerides.  The study will be conducted at approximately 50 sites in the United States.  For additional information on this study, please see (ID NCT01376557).

About LX4211

LX4211 is an orally-delivered small molecule under development as a potential treatment for diabetes.  LX4211 inhibits both sodium-glucose co-transporter type 1 (SGLT1) and sodium-glucose co-transporter type 2 (SGLT2).  SGLT2 is a transporter responsible for most of the glucose reabsorption performed by the kidney.  SGLT1 is a transporter responsible for glucose and galactose absorption in the gastrointestinal tract, and to a lesser extent than SGLT2, glucose reabsorption in the kidney.  For more information on LX4211, please visit

About Lexicon

Lexicon is a biopharmaceutical company focused on discovering breakthrough treatments for human disease.  Lexicon currently has four drug candidates in mid-stage development for diabetes, irritable bowel syndrome, carcinoid syndrome and rheumatoid arthritis, 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

Safe Harbor Statement

This press release contains "forward-looking" statements, including statements relating to Lexicon's clinical development of LX4211, including characterizations of the results of clinical trials of LX4211, the mechanism of action of LX4211 and the potential therapeutic and commercial potential of LX4211.  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 clinical development of LX4211 and preclinical and clinical development of 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.  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, 2010, 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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