4000 Research Forest Drive
The Woodlands, TX 77381-4287
Phone: 281-863-3000
www.lexicongenetics.com

Arthur Sands, president and CEO
NASDAQ:LEXG

Overview

Lexicon Genetics Inc. calls itself “a drug discovery company of the post-genome era.” It uses gene knockout technology to define the functions of genes for the discovery of pharmaceutical products. Its LexVision database is a relational database that catalogues the functions of candidate drug targets it has knocked out using its gene targeting and gene trapping technologies; it is expanding LexVision to fuel its drug discovery programs in cancer, cardiovascular disease, immune disorders, neurological disease, diabetes and obesity.

Lexicon identifies the best targets from the genome using in vivo mammalian target validation and develops drugs to modulate those targets. It believes it has the world’s largest gene knockout capabilities and plans to discover the in vivo mammalian function and pharmaceutical value of a total of 5,000 potential drug targets and therapeutic proteins over five years in its Genome 5000 program. The Genome 5000 program consists of the 1,250 candidate drug targets that have been designated for inclusion in the LexVision database, as well as the additional potential drug targets and therapeutic proteins Lexicon is pursuing in its drug discovery alliances and internal programs.

Also, Lexicon has applied its high-throughput gene trapping technology to create OmniBank, a library of more than 200,000 genetically modified mouse embryonic stem cell clones.

Lexicon is building a drug discovery pipeline of its own. In October 2001, Lexicon said it discovered and validated in vivo a new target for the development of potential treatments for heart disease, obesity and related diseases. Lexicon discovered the gene through its industrialized gene knockout program.

In December 2001, Lexicon, using the same gene knockout program, said it discovered a new role in the immune system for a known enzyme. The company said it is planning to develop drugs that could be used to block inflammation and potentially even prevent organ transplant rejection.

In early January 2002, Lexicon said it discovered and validated in vivo a new drug target, LG527, to develop potential treatments for depression. The human gene encoding the new target was discovered using Lexicon’s gene trap technology.

The company acquired Coelacanth Corp., of Princeton, N.J., in 2001, announcing the closing of the merger on July 12. The acquisition was valued at $32 million. Coelacanth uses chemistry technologies to discover new chemical entities for drug development and will form the core of a new division called Lexicon Pharmaceuticals, based in Princeton.

In September 2001, Lexicon and Deltagen Inc., of Redwood City, Calif., settled their patent infringement litigation. Through the settlement, Deltagen obtained a commercial license under the patents covering Lexicon’s gene targeting technologies, and Lexicon obtained a subscription to Deltagen’s DeltaBase database of mammalian genes and their in vivo functions.

Partners

Drug discovery partners include Abgenix Inc., Arena Pharmaceuticals Inc. and Incyte Genomics Inc.; LexVision partners include Bristol-Myers Squibb Co. and Incyte Genomics Inc.; and functional genomics partners include Abgenix Inc., American Home Products Corp., Boehringer Ingelheim GmbH, DuPont Pharmaceuticals Co., Immunex Corp., Johnson & Johnson, NV Organon, Millennium Pharmaceuticals Inc., Pharmacia Corp. and Tularik Inc.