The Woodlands, Texas, September 27, 2017 – Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX) today announced the company has initiated dosing in a Phase 1 study of LX9211, an orally-administered small molecule for the treatment of neuropathic pain. LX9211 is a selective inhibitor of AAK1 (adapter-associated kinase), which in preclinical studies demonstrated significant reduction in pain response in a series of pain models and was well-tolerated at and above efficacious doses in animals.

“The successful filing of the IND followed by initiation of the first-in-human clinical study for LX9211 are significant milestones for the company as these events validate our robust preclinical results and bring us closer to demonstrating clinical proof-of-concept for LX9211 in patients with neuropathic pain,” said Praveen Tyle, Ph.D., Lexicon’s executive vice president, research and development. “Based on animal data, LX9211 has the potential to significantly reduce pain response while offering a novel therapeutic approach to neuropathic pain through inhibition of AAK1. We look forward to producing important early data to guide our future development plans.” 

The Phase 1 double-blind, placebo-controlled, single ascending dose study for LX9211 is designed to assess the safety, tolerability and pharmacokinetics of LX9211 across nine oral escalating dose levels (5 mg to 300 mg) in healthy volunteers.


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

Safe Harbor Statement

This press release contains “forward-looking statements,” including statements relating to Lexicon’s clinical development of and regulatory filings for LX9211 and the results and projected timing of clinical trials and the potential therapeutic and commercial potential of LX9211. 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 LX9211 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 LX9211 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 LX9211. As a result, LX9211 may never be successfully commercialized. Other risks include Lexicon’s ability to meet its capital requirements, successfully commercialize its approved product, 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, 2016, 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
Senior Director, Corporate Communications and Advocacy
Lexicon Pharmaceuticals
(281) 863-3421
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