THE WOODLANDS, Texas, Jan. 7 /PRNewswire-FirstCall/ -- Lexicon Genetics Incorporated (Nasdaq: LEXG - News) announced today the publication of a retrospective evaluation of the targets of the 100 best-selling drugs of 2001 as modeled by mouse knockout phenotypes.
In an article published in the January 2003 issue of Nature Reviews Drug Discovery, Brian P. Zambrowicz, Ph.D., Lexicon's executive vice president of research, and Arthur T. Sands, M.D., Ph.D., Lexicon's president and chief executive officer, concluded that in most cases there is a direct correlation between the knockout and the therapeutic effect of the drug. The 100 best- selling drugs of 2001 modulate a total of 43 host targets. Of these 43 targets, 34 have been knocked out in the mouse. 85% of those knockouts were informative with respect to the physiological function and pharmaceutical utility of the target.
Since most drugs act as antagonists or blockers of specific targets, mouse gene knockouts can be used to successfully model the physiological action of drugs. With the high degree of gene function and physiological similarity between the human and the mouse, Lexicon believes this approach provides unprecedented opportunities to discover the next generation of breakthrough therapeutics based on novel targets from the human genome.
"The degree to which mouse knockouts model the top drugs is truly remarkable," said Dr. Zambrowicz. "We have already used knockouts to discover new targets in obesity, diabetes, cardiology, inflammation, oncology, and neuropsychiatry for Lexicon's drug discovery programs."
Lexicon scientists are focused on discovering drugs by first knocking out and analyzing the genes that encode future potential drug targets. With knowledge of the physiological function of these targets, therapeutic compounds are then developed to interact specifically with the targets that demonstrate the greatest potential for therapeutic intervention.
"We anticipate discovering lead molecules in some of our most exciting therapeutic programs this year," said Dr. Sands. "Within four years, we plan to complete the 'druggable' genome under our Genome5000 program."
A complete copy of the Nature Review article is available for download at Lexicon's corporate website, www.lexicon-genetics.com . |
