* New Oral Small Molecule Drug Candidate for Type 2 Diabetes
* SGLT2 Inhibition Shown to Reduce Blood Glucose Levels and Body
Weight
* Phase 1 Clinical Trials to Begin Following FDA Review
THE WOODLANDS, Texas, Dec. 1, 2008 (GLOBE NEWSWIRE) -- Lexicon Pharmaceuticals, Inc. (Nasdaq:LXRX), a biopharmaceutical company focused on discovering and developing breakthrough treatments for human disease, announced today that it has submitted an investigational new drug (IND) application to the U.S. Food and Drug Administration (FDA) for LX4211, an oral small molecule drug candidate for type 2 diabetes. The initial Phase 1 clinical trial of LX4211 is planned as a double-blind, randomized, placebo-controlled, ascending single- and multiple-dose study in healthy volunteers. This study is designed to evaluate the safety, tolerability, and pharmacokinetics of LX4211. Upon initiation of testing following FDA review, LX4211 would constitute Lexicon's fifth drug candidate to enter human clinical trials as part of its 10TO10 program.
"We observed the remarkable potential and biological specificity of the target of LX4211 in our Genome5000 program, a finding corroborated by human genetic studies," said Brian Zambrowicz, Ph.D., executive vice president and chief scientific officer at Lexicon. "The mechanism of action of LX4211 specifically blocks reabsorption of glucose by the kidney, which may help to improve glucose control in patients with type 2 diabetes. We believe that LX4211 will be favorably distinguished within an emerging new class of agents being developed for the treatment of diabetes."
About the Target
LX4211 was developed at Lexicon as a potent inhibitor of the sodium glucose transporter 2 (SGLT2), a transporter that is responsible for most of the glucose reabsorption performed by the kidneys. Compounds that inhibit SGLT2 can potentially treat diabetes by increasing urinary glucose excretion, thereby lowering blood glucose levels as well as caloric load. This mechanism contrasts with that of certain drugs for type 2 diabetes which cause glucose calories to be stored rather than released, further stressing the insulin producing pancreatic beta cells. In preclinical studies using a diabetic mouse model, LX4211 increased urinary glucose excretion and decreased levels of both blood glucose and hemoglobin A1c (HbA1c), the latter of which is an indicator of long-term blood glucose levels. Loss of calories through increased glucose excretion could also have beneficial metabolic effects. Support for this possibility was recently provided by results from an SGLT2 inhibitor already in clinical trials which, in addition to reducing levels of HbA1c, has shown weight loss in studies of diabetic patients. Currently, there are no marketed products targeting the SGLT2 mechanism of action to treat diabetes.
About Diabetes
Diabetes mellitus is a common metabolic disorder associated with abnormally high blood sugar levels. Diabetes is classified as either type 1, which is characterized by severely diminished insulin production, or type 2, which is characterized by moderately diminished insulin production in conjunction with insulin resistance (insensitivity of the tissues of the body to insulin). Insulin, a hormone that regulates blood glucose levels, is required to convert sugar, starches, and other food into energy needed for daily life. Diabetes can seriously impair overall quality of life and may lead to multiple complications including heart disease, stroke, and kidney failure. According to the International Diabetes Foundation, more than 245 million people have diabetes, with type 2 diabetes being the most prevalent.
About Lexicon
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. Lexicon's goal is to advance 10 drug candidates into human clinical trials by the end of 2010, the strategic objective of its 10TO10 program. The company has used its proprietary gene knockout technology to identify more than 100 promising drug targets. Lexicon has applied small molecule chemistry and antibody technology to these biologically-validated targets to create its extensive pipeline of clinical and preclinical programs. For additional information about Lexicon and its programs, please visit www.lexpharma.com.
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Safe Harbor Statement
This press release contains "forward-looking statements," including statements relating to Lexicon's clinical development of LX4211 and the potential therapeutic and commercial potential of LX4211. This press release also contains forward-looking statements relating to Lexicon's growth and future operating results, discovery and development of products, strategic alliances and intellectual property, as well as other matters that are not historical facts or information. All forward-looking statements are based on management's current assumptions and expectations and involve risks, uncertainties and other important factors, specifically including those relating to Lexicon's ability to successfully conduct clinical development of LX4211 and preclinical and clinical development of its other potential drug candidates, advance additional candidates into preclinical and clinical development, obtain necessary regulatory approvals, achieve its operational objectives, obtain patent protection for its discoveries and establish strategic alliances, as well as additional factors relating to manufacturing, intellectual property rights, and the therapeutic or commercial value of its drug candidates, that may cause Lexicon's actual results to be materially different from any future results expressed or implied by such forward-looking statements. Information identifying such important factors is contained under "Factors Affecting Forward-Looking Statements" and "Risk Factors" in Lexicon's annual report on Form 10-K for the year ended December 31, 2007, as filed with the Securities and Exchange Commission. Lexicon undertakes no obligation to update or revise any such forward-looking statements, whether as a result of new information, future events or otherwise.