Monday October 1, 7:01 am Eastern Time
Press Release
SOURCE: Lexicon Genetics Incorporated
Lexicon Genetics Announces Discovery of Gene
Target For the Development of Drugs to Treat Heart
Disease
Gene Knockout Lowers Cholesterol, Triglycerides and Body Fat
THE WOODLANDS, Texas, Oct. 1 /PRNewswire/ -- Lexicon Genetics Incorporated
(Nasdaq: LEXG - news) today announced that the Company has discovered and validated
in vivo a new target for the development of potential treatments for heart disease, obesity and
related diseases, such as diabetes. The gene was uncovered through the Company's
industrialized gene knockout program in which mice lacking specific genes are associated
with desirable medical profiles. These knockout mice registered significantly lower
triglyceride and cholesterol levels, as well as reduced body fat, with no change in diet.
Blocking this target, an enzyme designated LG-314, could provide a powerful new avenue to
develop therapies for cardiovascular disease and obesity. Lexicon expects to discover
compounds that can inhibit the enzyme target within one year.
``We are very excited about discovering compounds targeting this enzyme. We are currently
moving this target into screening for lead drug candidates,'' said Arthur T. Sands, M.D.,
Ph.D., President and Chief Executive Officer of Lexicon. ``We believe LG-314 is a
significant example of how our knockout technology will deliver substantially greater
productivity in the discovery of new drugs from the human genome. This discovery is also
demonstrative of Lexicon's strategy to focus on targets with blockbuster potential.''
The worldwide annual market for cholesterol and lipid-lowering agents is approximately $16
billion and represents approximately 13 million patients. Current treatment approaches
typically involve statins, to lower cholesterol, or fibrates, to lower trigylcerides. However,
there is no drug that can work on both, and the two categories of drugs are typically not
prescribed together because of heightened side effects. Obesity is typically treated by
appetite suppressants that encourage patients to eat less, but can often have substantial side
effects. Lexicon's knockout mice showed a 49 percent reduction in triglycerides and a 26
percent decrease in cholesterol. Importantly, body fat was also reduced by 32 percent in
females and 26 percent in males, although the knockout mice ate the same amount as the normal animals.
``We find LG-314 particularly compelling because currently there are no drugs available that decrease cholesterol, triglycerides
and body fat while maintaining a consistent diet. Due to the profile of Lexicon's target, a drug created to act on it could have
dramatic benefits for heart disease and obesity patients,'' said Hector BeltrandelRio, M.D., Ph.D., Lexicon's Director of
Cardiology. ``With in vivo validation up front in our drug discovery process, we select those targets that demonstrate the best
mechanism of action of a potential new therapeutic.''
Lexicon used a battery of tests conducted in vivo to validate LG-314's activity in an actual mammalian system. Scientists at
Lexicon are now working to screen small molecule drugs that could act on the target and eventually be brought into clinical
testing. The target is the first from Lexicon's drug discovery efforts to be unveiled; the Company currently has several additional
targets that are rapidly being moved into drug screening in the fields of cardiology, neurology, oncology and immunology.
Lexicon Genetics Incorporated is a drug discovery company of the post-genome era, using gene knockout technology to define
the functions of genes for the discovery of pharmaceutical products. Lexicon is using this technology to fuel drug discovery
programs in cancer, cardiovascular disease, immune disorders, neurological disease, diabetes and obesity. Lexicon has
established drug discovery alliances and functional genomics collaborations with leading pharmaceutical and biotechnology
companies, research institutes and academic institutions throughout the world to commercialize its technology and further
develop its discoveries. Additional information about the Company is available through Lexicon's corporate website,
www.lexicon-genetics.com .
This press release contains ``forward-looking statements,'' including statements about 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. These 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 develop drug candidates from its discoveries, achieve its operational objectives, obtain patent protection for its discoveries
and establish strategic alliances, 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 ``Business -- Risk Factors'' in Lexicon's annual report on Form 10-K
for the year ended December 31, 2000, 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.
SOURCE: Lexicon Genetics Incorporated |
