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Lexicon Files Investigational New Drug Application for LX1032 as a Potential Treatment for Carcinoid Syndrome

Saturday, December 22, 2007 General News
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THE WOODLANDS, Texas, Dec. 21 LexiconPharmaceuticals, Inc. (Nasdaq: LXRX) announced today that it has submitted aninvestigational new drug (IND) application to the U.S. Food and DrugAdministration (FDA) for LX1032, an oral drug candidate for managinggastrointestinal symptoms associated with carcinoid syndrome. The initialPhase 1 clinical trial of LX1032 is planned as a double-blind, randomized,placebo-controlled, ascending single-dose study in healthy volunteers. Thisstudy is designed to evaluate the safety, tolerability, and pharmacokineticsof LX1032. Lexicon expects to initiate clinical trials with LX1032 followingFDA review.
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"We believe LX1032 has the potential to be an important new therapy in anarea of high unmet medical need," said Philip M. Brown, M.D., J.D., vicepresident of clinical development at Lexicon. "LX1032 may offer importantbenefits to patients with carcinoid syndrome, who have very limited treatmentoptions."
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Carcinoid syndrome is the result of metastatic carcinoid tumors thatusually originate from enterochromaffin cells in the lining of thegastrointestinal tract. These tumors secrete large amounts of serotonin,which causes a variety of symptoms that often includes severe diarrhea andabdominal discomfort. Carcinoid tumors are a type of neuroendocrine tumorand, according to the American Cancer Society, about 11,000 to 12,000neuroendocrine tumors and neuroendocrine cancers are diagnosed each year inthe United States. About 10% of people with carcinoid tumors will developcarcinoid syndrome.

The target for LX1032 was identified through the Genome5000(TM) project,Lexicon's program to identify the function of 5,000 druggable genes in thehuman genome. LX1032 was developed at Lexicon as a potent inhibitor oftryptophan hydroxylase (TPH), a rate-limiting enzyme in the synthesis ofserotonin. In preclinical studies, LX1032 was able to reduce peripheralserotonin in several different species without affecting serotonin levels inthe brain. LX1032 is Lexicon's second compound to target TPH and, unlikeLX1031, which acts locally within the gastrointestinal tract, was designed toact systemically.

LX1032 is being developed in a product development collaboration withSymphony Capital Partners, L.P. and its co-investors.

About Lexicon

Lexicon is a biopharmaceutical company focused on the discovery anddevelopment of breakthrough treatments for human disease. Lexicon currentlyhas development programs underway for such areas of major unmet medical needas irritable bowel syndrome, cognitive disorders, and autoimmune diseases.The company has used its proprietary gene knockout technology to discover morethan 100 promising drug targets and create an extensive pipeline of clinicaland preclinical programs in the therapeutic areas of diabetes and obesity,cardiovascular disease, psychiatric and neurological disorders, cancer, immunesystem disorders and ophthalmic disease. To advance the development andcommercialization of its programs, Lexicon is working both independently andthrough collaborators including Bristol-Myers Squibb Company, Genentech, Inc.and N.V. Organon. For additional information about Lexicon and its programs,please visit http://www.lexpharma.com.

Safe Harbor Statement

This press release contains "forward-looking statements," includingstatements relating to Lexicon's clinical development of LX1032 and thepotential therapeutic and commercial potential of LX1032. This press releasealso contains forward-looking statements relating to Lexicon's growth andfuture operating results, discovery and development of products, strategicalliances and intellectual property, as well as other matters that are nothistorical facts or information. All forward-looking statements are based onmanagement's current assumptions and expectations and involve risks,uncertainties and other important factors, spe
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