Lexicon Presents Class of Compounds Modulating TPH1, the Target for its LX1031 Investigational Drug for Irritable Bowel Syndrome
August 21 2007 - 4:00PM
PR Newswire (US)
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
findings have allowed us to pursue a potential new mechanism for
treating conditions, such as IBS, that are not well-served by
current therapies." Using Lexicon's proprietary knock-out mouse
technology, company scientists established that serotonin in the
brain and neurons is synthesized by TPH2, an enzyme related to but
distinct from TPH1, which is responsible for the synthesis of
almost all peripheral serotonin. Knock-out studies showed that mice
lacking a functional TPH1 gene exhibited normal brain levels of
serotonin with no detectable levels in the periphery. Importantly,
the TPH1 knockout mice were healthy and exhibited no significant
adverse effects. Top-line Phase 1 clinical results for LX1031 are
expected to be presented at the American College of
Gastroenterology's Annual Scientific Meeting in Philadelphia in
October. About Lexicon Lexicon is a biopharmaceutical company
focused on the discovery and development of breakthrough treatments
for human disease. Lexicon currently has development programs
underway for such areas of major unmet medical need as irritable
bowel syndrome and cognitive disorders. The company has used its
proprietary gene knockout technology to discover more than 100
promising drug targets and create an extensive pipeline of clinical
and preclinical programs in the therapeutic areas of diabetes and
obesity, cardiovascular disease, psychiatric and neurological
disorders, cancer, immune system disorders and ophthalmic disease.
To advance the development and commercialization of its programs,
Lexicon is working both independently and through 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," including
statements relating to Lexicon's clinical development of LX1031 and
the potential therapeutic and commercial potential of LX1031. 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 LX1031 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. Information identifying such important factors is
contained under "Factors Affecting Forward-Looking Statements" and
"Risk Factors" in Lexicon's annual report on Form 10-K for the year
ended December 31, 2006, 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. DATASOURCE: Lexicon
Pharmaceuticals, Inc. CONTACT: Bobbie Faulkner, Manager, Investor
Relations of Lexicon Pharmaceuticals, Inc., +1-281-863-3503, Web
site: http://www.lexpharma.com/
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