The Woodlands, TX – December 20, 2018 - Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), today announced topline results from Phase 1 clinical studies of LX2761, an oral sodium-glucose cotransporter type 1 (SGLT1) inhibitor in development for the treatment of diabetes.

“Results from our Phase 1 studies build on previously reported promising preclinical data for LX2761 and confirm the drug candidate’s unique preclinical profile as a potent, gastrointestinal tract-selective SGLT1 inhibitor,” said Praveen Tyle, Ph.D., executive vice president of Research and Development. “We are evaluating next steps for this compound and look forward to providing updates in the future.”

The Phase 1 clinical studies of LX2761 included a Phase 1a single ascending-dose study in healthy volunteers and patients with type 2 diabetes, and a Phase 1b multiple ascending-dose study in patients with type 2 diabetes.

The Phase 1a study involved 5 cohorts of healthy volunteers and 2 cohorts of patients with type 2 diabetes. Patients with type 2 diabetes were washed off metformin for 3 days prior to dosing. LX2761 demonstrated minimal absorption and no systemic effect, with no increase in urine glucose excretion from baseline. In addition, LX2761 reduced postprandial glucose in diabetic patients while increasing plasma levels of GLP-1. The most common adverse and dose-limiting event was diarrhea, consistent with the SGLT1 mechanism of action due to reduced glucose absorption in the gut.

The randomized, double-blind, placebo-controlled Phase 1b study was performed to assess the safety, tolerability, pharmacodynamics and pharmacokinetics of multiple doses of orally administered LX2761 in patients with type 2 diabetes. Patients were randomly assigned to receive LX2761 or placebo over an 8-day treatment period as either a single dose or twice a day dose at breakfast and dinner. Patients were treated with metformin at the time of screening and for the duration of the study. LX2761 showed reduced postprandial glucose, demonstrating delayed and reduced intestinal glucose absorption while increasing plasma levels of GLP-1 with minimal effect on urinary glucose excretion, consistent with inhibition of intestinal SGLT1. The most common adverse event was diarrhea.

About LX2761

LX2761 is an orally-delivered small molecule compound that is designed to inhibit SGLT1 locally in the gastrointestinal tract without any significant inhibition of SGLT2 in the kidney. In preclinical studies, LX2761 delayed and reduced intestinal glucose absorption and reduced postprandial glucose while increasing plasma levels of GLP-1 with minimal effect on urinary glucose excretion. Lexicon has granted Sanofi certain rights of first negotiation with respect to the future development and commercialization of LX2761.

About Lexicon Pharmaceuticals

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. In addition to its first commercial product, XERMELO® (telotristat ethyl), Lexicon has a pipeline of promising drug candidates in clinical and pre-clinical development in diabetes and metabolism and neuropathic pain. For additional information please visit www.lexpharma.com.

Safe Harbor Statement

This press release contains “forward-looking statements,” including statements relating to Lexicon’s clinical development of and regulatory filings for LX2761 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, development and commercialization 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 commercialize XERMELO (telotristat ethyl), successfully conduct preclinical and clinical development and obtain necessary regulatory approvals of sotagliflozin, LX9211 its other potential drug candidates on its anticipated timelines, 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, 2017, 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.

For Investor Inquiries:

Kimberly Lee, D.O.
Head of Investor Relations and Corporate Strategy
Lexicon Pharmaceuticals
(281) 863-3383
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For Media Inquiries:

Chas Schultz
Executive Director, Corporate Communications and Patient Advocacy
Lexicon Pharmaceuticals
(281) 863-3421
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