Lexicon Pharmaceuticals, Inc. is a

biopharmaceutical A biopharmaceutical, also known as a biological medical product, or biologic, is any pharmaceutical drug product manufactured in, extracted from, or semisynthesized from biological sources. Different from totally synthesized pharmaceuticals, t ...

company developing treatments for human disease. The company was founded in 1995 in

The Woodlands, Texas The Woodlands is a Special district (United States), special-purpose district and census-designated place (CDP) in the U.S. state of Texas in the Greater Houston, Houston–The Woodlands–Sugar Land metropolitan statistical area. The Woodlands ...

under the name Lexicon Genetics, Incorporated by co-founders Professor Allan Bradley, FRS and Professor Bradley's postdoctoral fellow Arthur T Sands. The company has used its patented mouse

gene knockout Gene knockouts (also known as gene deletion or gene inactivation) are a widely used genetic engineering technique that involves the gene targeting, targeted removal or inactivation of a specific gene within an organism's genome. This can be done t ...

technology and extensive in vivo screening capabilities to study nearly 5,000 genes in its Genome5000 program and has identified over 100 potential therapeutic targets. Lexicon has advanced multiple drug candidates into human

clinical trials Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

and has a broad and diverse pipeline of drug targets behind its clinical programs. Lexicon is pursuing drug targets in five therapeutic areas including

oncology Oncology is a branch of medicine that deals with the study, treatment, diagnosis, and prevention of cancer. A medical professional who practices oncology is an ''oncologist''. The name's Etymology, etymological origin is the Greek word ὄγ ...

gastroenterology Gastroenterology (from the Greek gastḗr- "belly", -énteron "intestine", and -logía "study of") is the branch of medicine focused on the digestive system and its disorders. The digestive system consists of the gastrointestinal tract, sometime ...

immunology Immunology is a branch of biology and medicine that covers the study of Immune system, immune systems in all Organism, organisms. Immunology charts, measures, and contextualizes the Physiology, physiological functioning of the immune system in ...

metabolism Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the co ...

, and

ophthalmology Ophthalmology (, ) is the branch of medicine that deals with the diagnosis, treatment, and surgery of eye diseases and disorders. An ophthalmologist is a physician who undergoes subspecialty training in medical and surgical eye care. Following a ...

. The company's clinical drug candidates include sotagliflozin (LX4211) for the treatment of

type 2 diabetes Type 2 diabetes (T2D), formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent ...

; LX1033 for the treatment of

irritable bowel syndrome Irritable bowel syndrome (IBS) is a functional gastrointestinal disorder characterized by a group of symptoms that commonly include abdominal pain, abdominal bloating, and changes in the consistency of bowel movements. These symptoms may ...

and other gastrointestinal disorders;

telotristat ethyl Telotristat ethyl (United States Adopted Name, USAN, brand name Xermelo) is a prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase. It is formulated as telotristat etiprate — a Hippuric acid, hippurate salt of telotristat eth ...

(LX1032) for the treatment of the symptoms associated with

carcinoid syndrome Carcinoid syndrome is a paraneoplastic syndrome comprising the signs and symptoms that occur secondary to neuroendocrine tumors (formerly known as carcinoid tumors). The syndrome is caused by neuroendocrine tumors most often found in the gut ...

; and LX2931 for the treatment of autoimmune diseases, such as

rheumatoid arthritis Rheumatoid arthritis (RA) is a long-term autoimmune disorder that primarily affects synovial joint, joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and h ...

Company history

Lexicon Pharmaceuticals was founded in September 1995 as a biotech venture of

Baylor College of Medicine The Baylor College of Medicine (BCM) is a private medical school in Houston, Texas, United States. Originally as the Baylor University College of Medicine from 1903 to 1969, the college became independent with the current name and has been se ...

. The company went public in April 2000 with one of the largest initial public offerings in biotech history ($220 million). In June, 2001 Lexicon purchased a privately owned small chemical library synthesis company, Coelacanth Corporation in

Princeton, New Jersey The Municipality of Princeton is a Borough (New Jersey), borough in Mercer County, New Jersey, United States. It was established on January 1, 2013, through the consolidation of the Borough of Princeton, New Jersey, Borough of Princeton and Pri ...

, which became the site for the company's small molecule and medicinal chemistry efforts. The company's original name was Lexicon Genetics Incorporated, but in 2007, the name changed to Lexicon Pharmaceuticals, Inc. to reflect a renewed focus on drug development. The company initially focused on using

technology to define the function of genes. This effort complemented and benefited from the international effort to sequence the human and mouse genomes (see

Human Genome Project The Human Genome Project (HGP) was an international scientific research project with the goal of determining the base pairs that make up human DNA, and of identifying, mapping and sequencing all of the genes of the human genome from both a ...

). Using its proprietary gene trapping and

gene targeting Gene targeting is a biotechnological tool used to change the DNA sequence of an organism (hence it is a form of Genome Editing). It is based on the natural DNA-repair mechanism of Homology Directed Repair (HDR), including Homologous Recombinat ...

technologies, the company created the world’s largest repository of genetically modified mouse

embryonic stem cells Embryonic stem cells (ESCs) are Cell potency#Pluripotency, pluripotent stem cells derived from the inner cell mass of a blastocyst, an early-stage pre-Implantation (human embryo), implantation embryo. Human embryos reach the blastocyst stage 4� ...

, known as OmniBank, and established a large-scale mammalian knockout program to discover the physiological and behavioral functions of the most druggable mammalian genes. The information collected from this program is stored in the company’s LexVision database, which contains almost 5,000 gene knockouts studied. Over the years, Lexicon evolved from a genomics company into a drug discovery and development company focused on discovering and developing breakthrough treatments for human disease. The company currently has multiple drug candidates in various stages of

. In 2016, the company was ranked #8 on the Deloitte Fast 500 North America list.

Technology

Lexicon uses patented gene trapping and

technologies to generate and study

knockout mice A knockout mouse, or knock-out mouse, is a genetically modified mouse (''Mus musculus'') in which researchers have inactivated, or " knocked out", an existing gene by replacing it or disrupting it with an artificial piece of DNA. They are importan ...

to discover the physiological and behavioral effects that result from the disruption of a single

. Because there is a close similarity in gene function and physiology between mice and humans, with a large majority of human genes having a counterpart in the mouse genome, knockout mouse technology has become a powerful tool in the discovery of new medicines. The value of Lexicon’s technology in drug discovery has been described in a retrospective analysis by the scientific journal

Nature Nature is an inherent character or constitution, particularly of the Ecosphere (planetary), ecosphere or the universe as a whole. In this general sense nature refers to the Scientific law, laws, elements and phenomenon, phenomena of the physic ...

. The conclusion of this analysis was that, in most cases, there was a direct correlation when comparing the physiological characteristics, or phenotypes, of knockout mice to the therapeutic effect of the 100 best-selling drugs of 2001. The tremendous utility of knockout mouse technology was recognized in 2007 with the Nobel Prize in Physiology or Medicine to Drs.

Mario Capecchi Mario Ramberg Capecchi (born 6 October 1937) is an Italian-born molecular geneticist and a co-awardee of the 2007 Nobel Prize in Physiology or Medicine for discovering a method to create mice in which a specific gene is turned off, known as knoc ...

Martin Evans Sir Martin John Evans FLSW (born 1 January 1941) is an English biologist who, with Matthew Kaufman, was the first to culture mice embryonic stem cells and cultivate them in a laboratory in 1981. He is also known, along with Mario Capecchi ...

, and

Oliver Smithies Oliver Smithies (23 June 1925 – 10 January 2017) was a British-American geneticist and physical biochemist. He is known for introducing starch as a medium for gel electrophoresis in 1955, and for the discovery, simultaneously with Mario Cap ...

. In developing small molecule drugs for its validated targets, Lexicon uses medicinal chemistry known as "

click chemistry Click chemistry is an approach to chemical synthesis that emphasizes efficiency, simplicity, selectivity, and modularity in chemical processes used to join molecular building blocks. It includes both the development and use of "click reactions", a ...

." Dr. K. Barry Sharpless, who was awarded the 2001 Nobel Prize in Chemistry, pioneered this set of powerful and reliable tools for the rapid synthesis of novel compounds. Lexicon uses solution-phase chemistry to generate diverse libraries of optically pure compounds that are built using highly robust and scalable organic reactions that allow the company to generate compound collections of great diversity and to specially tailor the compound collections to address various therapeutic target families. Lexicon’s medicinal chemists design these libraries by analyzing the chemical structures of drugs that have been proven safe and effective against human disease and using that knowledge in the design of scaffolds and chemical building blocks for the generation of large numbers of new drug-like compounds.

Locations

Lexicon operates from two locations found in

Texas Texas ( , ; or ) is the most populous U.S. state, state in the South Central United States, South Central region of the United States. It borders Louisiana to the east, Arkansas to the northeast, Oklahoma to the north, New Mexico to the we ...

and

New Jersey New Jersey is a U.S. state, state located in both the Mid-Atlantic States, Mid-Atlantic and Northeastern United States, Northeastern regions of the United States. Located at the geographic hub of the urban area, heavily urbanized Northeas ...

. The corporate headquarters are in

just north of

Houston Houston ( ) is the List of cities in Texas by population, most populous city in the U.S. state of Texas and in the Southern United States. Located in Southeast Texas near Galveston Bay and the Gulf of Mexico, it is the county seat, seat of ...

. This location serves as Lexicon’s primary research facility to discover and validate the company's drug targets and test drug candidates in preclinical research. The company’s clinical development and regulatory team is also based at the corporate headquarters. Lexicon's campus in

is the home of Lexicon's small molecule medicinal chemistry and preclinical development efforts. This site serves as Lexicon's primary medicinal chemistry site to create new chemical entities for therapeutic development.

References

{{Pharmaceutical companies of the United States Pharmaceutical companies established in 1995 Pharmaceutical companies of the United States Companies based in The Woodlands, Texas Companies listed on the Nasdaq Health care companies based in Texas 2000 initial public offerings Pharmaceutical companies