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The Woodlands, Texas, June 29, 2012 – Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX) announced today the publication of results from two initial trials of LX4211 in patients with type 2 diabetes in the online edition of the journal Clinical Pharmacology & Therapeutics. The paper, containing results from both trials, is entitled, “LX4211, a Dual SGLT1/SGLT2 Inhibitor, Improved Glycemic Control in Patients with Type 2 Diabetes in a Randomized, Placebo-controlled Trial,” and will also appear in an upcoming print edition of the journal. A link to the online article can be accessed at http://www.nature.com/clpt/journal/vaop/ncurrent/full/clpt201258a.html
“This publication represents the first peer-reviewed description of SGLT1 inhibition stimulating GLP-1 and PYY release in man,” said Dr. Brian Zambrowicz, Lexicon’s executive vice president and chief scientific officer. “Since LX4211 also inhibits SGLT2, the rapid and significant glycemic control and metabolic benefits observed may be attributed to effective dual inhibition of these two targets.”
In the 4-week Phase 2a study described in the paper, 36 patients received once-daily oral administration of placebo or 150 mg or 300 mg of LX4211 (randomized 1:1:1) in an in-patient setting. Patients receiving LX4211 exhibited rapid and significant improvements relative to placebo in multiple measures of glycemic control, including hemoglobin A1c (HbA1c), fasting plasma glucose, and oral glucose tolerance. In addition, serum triglycerides were significantly lower at the end of the four-week treatment period, and trends of meaningful reductions in body weight and blood pressure were observed. Importantly, LX4211 treatment demonstrated a favorable safety profile and was well tolerated in the study. Also described in the paper was a subsequent clinical study conducted in a similar population of poorly-controlled patients with type 2 diabetes that showed LX4211 treatment elevated GLP-1 and PYY, two gastrointestinal peptides known to be associated with enhanced metabolic control. These elevations in GLP-1 levels after LX4211 treatment were previously suggested by data from the Phase 2a study and, hence, the repeated observation confirmed that LX4211 can act as an oral, GLP-1 secretagogue.
Lexicon recently reported top-line results from a Phase 2b double-blind study of LX4211 that extend favorable observations of the early trials to an out-patient setting in a larger population with a longer duration of therapy. The 12-week study was conducted at more than 50 centers in the United States in 299 patients with poorly-controlled diabetes despite treatment with metformin, an established diabetes therapy. Primary and secondary measures of efficacy from this study demonstrated substantial, dose-dependent, statistically-significant reductions in HbA1c, body weight and blood pressure. LX4211’s dual inhibition of SGLT1 and 2 was associated with an overall favorable safety profile in the study and, notably, LX4211’s inhibition of SGLT1 was associated with a gastrointestinal safety profile similar to placebo.
Lexicon is a biopharmaceutical company focused on discovering breakthrough treatments for human disease. Lexicon currently has five drug programs in mid-stage development for diabetes, carcinoid syndrome, irritable bowel syndrome, rheumatoid arthritis and glaucoma, 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 clinical development of LX4211, characterizations of the results of and projected timing of clinical trials 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. 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, 2011, 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.