Lexicon Identifies Transporter in Brain as the Target for LX6171
The Woodlands, Texas, April 15, 2008 – Lexicon
Pharmaceuticals, Inc. (Nasdaq: LXRX), a leader in genomics-based drug
discovery, presented data today describing the target of LX6171 and
initial Phase 1 clinical results at the American Academy of Neurology
in Chicago. LX6171 is an internally-developed compound under
evaluation by the company as a potential treatment for cognitive
disorders. LX6171, currently in Phase 2 clinical testing, is one of
four programs in human clinical trials as part of Lexicon’s 10TO10
program.
LX6171 is an orally-delivered, small molecule inhibitor of SLC6A7, a
high-affinity L-proline transporter found in the brain. SLC6A7 is a
member of the gamma-aminobutyric acid (GABA) neurotransmitter
transporter family, and is expressed in regions of the brain that are
known to be involved in learning and memory. In preclinical studies,
mice treated with LX6171 displayed improved performance in tests of
learning and memory, corroborating observations in knockout mice
lacking SLC6A7.
“Until we identified and analyzed SLC6A7 in our Genome5000™ program,
relatively little was known about this transporter and its role in
behavior,” said Dr. Brian Zambrowicz, Lexicon’s chief scientific
officer. “Our results indicate that inhibiting this target may
delineate a novel approach to the treatment of cognitive disorders.”
“Initial human studies with both young and elderly volunteers have
shown that the compound achieves good systemic exposure and is well
tolerated at the doses studied,” said Philip M. Brown, M.D., J.D.,
senior vice president of clinical development at Lexicon. “LX6171 may
have potential in a broad range of applications involving cognitive
disorders, including Alzheimer’s disease, attention disorders, and
developmental disorders.”
Clinical Results
In Phase 1 clinical trials, LX6171 was generally well
tolerated at all dose levels and showed good systemic exposure with no
significant adverse events or cognitive impairment observed.
Preliminary data on attention parameters were encouraging and suggest
the appropriateness of proceeding with further studies to determine if
LX6171 could have a potential effect on cognitive or attention
disorders.
LX6171 is currently under evaluation in a Phase 2 clinical trial to
evaluate the safety, tolerability and cognitive effects of LX6171 in
approximately 100 elderly subjects with age-associated memory
impairment (AAMI). The placebo-controlled trial will include a low
dose group receiving 120 mg of the drug candidate once per day, and a
higher dose group receiving 240 mg once per day. Both groups will
receive the drug candidate for 28 days and will be evaluated regularly
for effects on several dimensions of learning and memory. LX6171 is
being developed in a product development collaboration with Symphony
Capital Partners, L.P. and its co-investors.
About Lexicon
Lexicon is a leader in genomics-based drug discovery. Through
its proprietary gene knockout technology, the company is dedicated to
discovering and developing breakthrough treatments for human disease.
Lexicon currently has development programs underway for such areas of
major unmet medical need as irritable bowel syndrome, cognitive
disorders, autoimmune diseases, and carcinoid syndrome. 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 cardiology,
gastroenterology, immunology and oncology, metabolism, neurology and
ophthalmology. To focus its commitment, Lexicon initiated its 10TO10
program to advance 10 new drug candidates into human clinical trials by
the end of 2010. To advance the development and commercialization of
its programs, Lexicon is working both independently and through
collaborators including Bristol-Myers Squibb Co., Genentech, Inc. and
N.V. Organon. For additional information about Lexicon and its
programs, please visit www.lexpharma.com.
Safe Harbor Statement
This press release contains “forward-looking statements,”
including statements relating to Lexicon’s clinical development of
LX6171 and the potential therapeutic and commercial potential of
LX6171. 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
LX6171 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, 2007, 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.
