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Lexicon Presents Class of Compounds Modulating TPH1, the Target for its LX1031 Investigational Drug for Irritable Bowel Syndrome
Date:8/21/2007

BOSTON and THE WOODLANDS, Texas, Aug. 21 /PRNewswire-FirstCall/ -- Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX) presented data today describing the structure-activity relationship (SAR) of a class of internally-developed compounds that includes LX1031 and other compounds under evaluation by the company as potential treatments for irritable bowel syndrome (IBS) and other gastrointestinal disorders. LX1031 is currently under evaluation in a Phase 1b clinical trial in healthy volunteers.

Employing high-throughput screening of its proprietary chemical libraries, x-ray crystallography and medicinal chemistry, Lexicon scientists discovered and optimized a series of orally-administered, peripherally-acting small molecule inhibitors of the key enzyme responsible for producing serotonin in the gastrointestinal tract, tryptophan hydroxylase 1 (TPH1). In preclinical studies with these molecules, including LX1031, Lexicon scientists confirmed that serotonin levels could be predictably reduced in the intestine without affecting levels of the neurotransmitter in the brain, where it mediates mood and other behaviors. The data were presented here today at the American Chemical Society National Meeting and Exposition in Boston.

"Our genetic insights and chemistry expertise enabled us to discover a class of potent molecules that can inhibit TPH activity in the gastrointestinal tract while preserving normal levels of serotonin in the brain, an accomplishment we believe represents a significant advance for the field," commented Arthur T. Sands, M.D., Ph.D., president and chief executive officer of Lexicon Pharmaceuticals. "Given serotonin's established role as a neurotransmitter modulating gastrointestinal function, these fin
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SOURCE Lexicon Pharmaceuticals, Inc.
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