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Cengent Therapeutics Announces Successful Test of a Drug-Like Anthrax Lethal Factor Inhibitor in Two Animal Species.

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Cengent Therapeutics today announced the successful demonstration in animals of protection against anthrax toxin-induced disease processes that lead to death from anthrax infection. Unlike other protein and peptide-based anthrax therapeutics and prophylactics currently under development, Cengent is developing small-molecule compounds for prevention and treatment of anthrax infection. The novel agents, which show in vivo efficacy, are inhibitors of the zinc metalloprotease anthrax lethal factor, the most toxic component of the anthrax bacillus. The significance of Cengent's small-molecule inhibitors is that they are cell-permeable, a requirement of mechanism-base efficacy, and may be expected to demonstrate oral bioavailability. In October 2002, Cengent announced the issuance of the first United States Patent describing small-molecule inhibitors of anthrax lethal factor.

During Bacillus anthracis infection, the microorganism produces a number of proteins including lethal factor, a protease that can destroy other proteins inside the host's cells, resulting in immune suppression and death. A small-molecule that can inhibit anthrax lethal factor and is cell-permeable can potentially provide significant protection against anthrax as prophylactic and acute therapy. The recent results show that Cengent's inhibitor partially restores anthrax lethal toxin-suppressed immunological function in mice. In addition, treating lethal toxin-exposed rats with a Cengent inhibitor increases the life span of the rats significantly.

"Cengent Therapeutics' ability to rapidly discover and develop inhibitors of anthrax lethal factor is yet one more demonstration of the power of the company's structure-based drug design technology platform called Genes to Leads(R). The technology is broadly applicable to the rapid discovery of new leads with activity against important therapeutic targets in metabolic, infectious, and inflammatory diseases, as well as cancer," stated Edward T. Maggio, Ph.D., Chief Executive Officer.

"These recent results represent the first case of intervening in anthrax toxin-induced immune suppression and death with a small-molecule lethal factor inhibitor. The results validate lethal factor as a potentially useful therapeutic target for anthrax infection," stated Dr. Ruth F. Nutt, Vice President of Drug Discovery at Cengent Therapeutics.

Our Drug Pipeline

Cengent currently has pre-clinical programs in the obesity/diabetes and anti-infective areas. Cengent's most advanced program is in the diabetes area where we have succeeded in developing a number of selective and orally active PTP-1B (protein tyrosine phosphatase-1B) inhibitors, which promise to afford an entirely new mode of intervention for this increasingly prevalent disease. In preclinical studies, once a day dosing results in statistically significant lowering of blood glucose levels and sustained glycemic control.

About Cengent Therapeutics

Cengent Therapeutics is a structure-guided drug discovery company utilizing integrated, proprietary computational and experimental lab technologies to accelerate and optimize the drug discovery process.

Cengent provides pharmaceutical and biotech companies with a comprehensive suite of structural services and capabilities for accelerating and optimizing the drug discovery process. The Company's technologies include Genes To Leads(R) -- yielding novel drug leads in 60 - 120 days; Structure Determination Services including X-ray crystallography and Cengent's ProMax(R) 1.5A to 2A RMS augmented homology modeling service; and StructureBank(R), a database for the large-scale comparative analysis of protein targets and anti-targets. The company has applied its technologies to advance the drug discovery programs of a growing number of external research collaborators.

Our shareholders include Perseus-Soros, New York Life, BioAsia, Burrill Capital, Inglewood Ventures, Dansk Kapital, Deutsche Asset Management, Merrill Lynch, Invesco, and Veritas; corporate investors include Takara Shuzo, IBM, Quest Diagnostics, Encysive Pharmaceuticals, and Johnson & Johnson Development Corp. For more information on Cengent Therapeutics, its drug pipeline, products, and services, please visit the company's web site at
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Publication:Business Wire
Geographic Code:1USA
Date:Nov 19, 2003
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