Genetics-driven Drug Discovery
The Genome5000^TM program is Lexicon's initiative to determine the physiological and behavioral functions for 5,000 human genes by studying the corresponding mouse genes in knockout animals.  This effort is focused on gene families that we believe are pharmaceutically important, such as transporters, G-protein coupled receptors (GPCRs), ion channels, kinases and other key enzymes, membrane proteins (e.g., receptors), and secreted proteins.  Since most drugs act as antagonists of their targets, we interpret mouse knockout phenotypes as genetic models of future drug action in an idealized state of complete inhibition of target function, that is, 100% potent and 100% specific. 

Over 100 Validated Targets Identified
We have already analyzed more than 80% of these 5,000 genes, and have identified over 100 validated targets.  All of Lexicon's clinical development programs were discovered in the Genome5000 program, in which our unique approach to drug discovery has identified small molecule and biologic drug targets in six therapeutic areas:  cardiology, gastroenterology, immunology and oncology, metabolism, neurology, and ophthalmology.