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Lexicon initiates preclinical development of new drug candidate for glaucoma
Woodlands, Texas | Monday, August 18, 2008, 08:00 Hrs  [IST]

Lexicon Pharmaceuticals, Inc, a biopharmaceutical company, announced that it has initiated formal preclinical development of LX7101, a new drug candidate for glaucoma.

LX7101 is a small molecule compound that may have application in treating glaucoma by lowering fluid pressure in the eye through a new mechanism of action. Glaucoma is a disease of the eye which gradually impairs vision and is a leading cause of blindness in the United States.

Upon successful completion of preclinical development, Lexicon plans to file an Investigational New Drug (IND) application with the US Food and Drug Administration (FDA) for LX7101.

Drugs currently on the market for glaucoma lower intraocular pressure by either reducing aqueous humour production or by increasing the passive outflow of fluid from the anterior chamber of the eye. Lexicon's drug candidate, LX7101, reduces intraocular pressure by enhancing the outflow facility of the eye. Increased resistance to fluid outflow facility is thought to be a major contributing factor to the higher incidence of glaucoma that is observed as people age.

"Our drug discovery strategy is continuing to produce a pipeline of novel programs with significant potential to advance medicine," said Arthur T Sands, MD, Ph D, president and chief executive officer. "LX7101 is now the sixth drug discovery program to enter formal preclinical development as part of Lexicon's 10TO10 Program."

The target of LX7101 was discovered by Lexicon scientists through the company's Genome5000 program, which was designed to determine the function of 5,000 druggable genes using knockout mice. Lexicon's ophthalmology team launched a drug discovery program based on the observation that knockout mice lacking the gene encoding the target of LX7101 had lower intraocular pressure compared to normal mice. Lexicon's medicinal chemists then developed a series of small molecules that could be administered in an eye drop. A single topical dose significantly reduced intraocular pressure in a model of ocular hypertension. After extensive testing, LX7101 was identified as a drug candidate with the right profile to enter formal preclinical development.

"Our LX7101 compound addresses an important mechanism that regulates intraocular pressure in humans," said Brian Zambrowicz, Ph D, Lexicon's executive vice president and chief scientific officer. "LX7101 has the potential to be an effective pressure lowering agent in patients with glaucoma."

Glaucoma is a group of eye diseases that gradually impair vision and are usually associated with abnormally high fluid pressure within chambers of the eye (intraocular pressure). All forms of glaucoma damage the optic nerve, and may lead to blindness. While diagnosis and treatment options have improved, many patients still suffer from partial or total vision loss. Risk factors for glaucoma include age, genetic history, diabetes, and nearsightedness. According to the Glaucoma Research Foundation, glaucoma is estimated to affect 65 million people worldwide, including more than 4 million Americans.

Lexicon is a biopharmaceutical company focused on discovering and developing breakthrough treatments for human disease. Lexicon currently has six drug candidates in development for autoimmune disease, carcinoid syndrome, cognitive disorders, diabetes, glaucoma and irritable bowel syndrome, all of which were discovered by the company's research team.

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