Entelos Announces U.S. Patent for Gene Expression Test for Liver Toxicity Screening

    


Entelos Inc.



ENTELOS, Inc.

("Entelos" or "the Company")

Entelos, Inc. (LSE:ENTL), a leading life sciences company applying predictive
technologies and "virtual humans" to find better drugs and more tailored
health-related products, announced today that the U.S. Patent and Trademark
Office has granted U.S. Patent No. 7,396,645 entitled "Cholestasis Signature" to
the Company. This enabling technology helps researchers to screen novel
compounds more rapidly and efficiently during preclinical studies for
cholestasis, a specific type of drug-induced liver damage.

This patent relates to a method of testing a drug or novel compound to determine
its propensity for inducing cholestasis, a common toxic side effect of certain
drugs, by looking at its impact on a set of indicator genes, or biomarkers. This
biomarker set is one of dozens from the Company's proprietary library of Drug
Signatures(R), which have been derived from DrugMatrix(R), the world's largest
reference database linking gene expression profiles of over 630 drugs to results
from traditional preclinical pharmacology, safety, and toxicity tests.

In traditional drug development, safety assessment of drug candidates is
performed in laboratory animals only after lead compounds have been selected and
initial efficacy studies have been completed. As a consequence, adverse events
and potential toxic side effects of a chemical compound or compound series are
often discovered relatively late in the development process. Problems with
toxicity or safety are the leading cause of drug failures and some
pharmaceutical companies have reported compound attrition rates reaching almost
50%. Entelos' DrugMatrix system is used to predict safety and toxicity
liabilities of novel molecules using much shorter, faster, and more
cost-effective gene expression studies.

"We are pleased to add this new patent to our growing portfolio of patents that
strengthen our leadership position in both disease simulation and predictive
technologies focused on safety and toxicity testing," stated James Karis,
President and CEO of Entelos. "Drug failures are often due to unwanted side
effects in the liver and DrugMatrix is used by our pharmaceutical customers to
rapidly prioritize compound portfolios and minimize or eliminate these
liabilities much earlier in their R&D process. In addition, this patent
complements Entelos' ongoing effort with the FDA to build a model of
drug-induced liver injury to identify patients at risk for developing rare side
effects."

For further information please contact:

Entelos, Inc.
Jill Fujisaki, VP Investor Relations                        Tel: +1 650 572 5400
Buchanan Communications
Lisa Baderoon / Mary-Jane Johnson                       Tel +44 (0) 20 7466 5000

Notes for Editors

About Entelos' DrugMatrix(R) Database

The DrugMatrix Database is a unique reference set of gene expression profiles
for benchmark drugs and compounds that are linked to classic pharmacology,
toxicology and clinical pathology measurements.

DrugMatrix is populated with the comprehensive results of thousands of highly
controlled and standardized toxicological experiments in which rats or cultured
rat hepatocytes are treated with compounds at both non-toxic and toxic doses.
Multiple time points and target organs are evaluated and extensive observations
of relevant pharmacology, clinical chemistry, hematology, histology, body and
organ endpoints are recorded. A curation team extracts information on the
compounds from the literature and other relevant sources.

These data are linked to large-scale gene expression data sets generated by
extracting RNA from the toxicologically relevant organs and tissues and
measuring changes in the level of gene expression. DrugMatrix contains the
profiles derived from administering over 630 different compounds to rats.
Compounds include FDA approved drugs, drugs approved in Europe and Japan,
withdrawn drugs, drugs in preclinical and clinical studies, biochemical
standards and industrial and environmental toxicants.

Unique collections of biomarkers, Drug Signatures, have been identifed from the
gene expression, molecular pharmacology and histopathology data in DrugMatrix.
Drug Signatures are composed of statistically validated lists of genes and
coefficients that relate gene expression patterns to biology, physiology or
toxicology. Novel compounds can be characterized with regard to toxicity, on-
and off-target effects and mechanism of action by comparison to a large and
growing library of Drug Signatures including, but not limited to, toxicity
endpoints such as hepatocellular damage; organ pathology such as cholestasis or
bile duct hyperplasia; genetic endpoints such as DNA damage; compound, structure
activity, and therapeutic class such as azole antifungals, HMG CoA reductase
inhibitors, or lipid lowering agents; and off-target effects, such as that
induced by the lipid-lowering drug gemfibrozil.

About Cholestasis(1)

According to the NIH, drug-induced cholestasis is the blockage of the flow of
bile from the liver caused by medication. Bile is produced in the liver, moved
to the gallbladder and excreted into the gut through the biliary tract, to aid
in the digestion of fats. Flow from the liver to the gallbladder and ultimately
to the gut can be slowed or stopped by certain drugs. When the flow of bile is
inhibited, an individual may become jaundiced (yellow coloration to the eyes and
skin). Drugs which cause cholestasis may damage the liver.

Many drugs can cause cholestasis. Common culprits include: gold salts,
nitrofurantoin, anabolic steroids, oral contraceptives, chlorpromazine,
prochlorperazine, sulindac, cimetidine, erythromycin, tobutamide, imipramine,
ampicillin and other penicillin-based antibiotics.

If medication is causing cholestasis, physicians will typically withdraw
treatment. There is no medicine to reverse drug-induced cholestasis. Most
patients recover, but severe cases may lead to liver failure. Drug-induced
cholestasis usually reverses after discontinuation of the medication or drug,
although it may take many months for cholestasis to resolve.

1. Source: Medical encyclopedia: Drug-induced cholestasis, Medline Plus(R), a
service of the U.S. National Library of Medicine and the National Institutes of
Health.

About Entelos

Entelos, Inc. (www.entelos.com) is a US-based life sciences company applying
next-generation predictive technologies to revolutionize the way medicines are
discovered, developed, and utilized. The Company leverages its proprietary in
silico disease models, "virtual human" technology, and toxicology reference
systems to develop safer and more effective drugs, improve the quality of
health-related consumer products, and deliver on the promise of personalized
medicine. Entelos provides customized products, technology and research services
to global pharmaceutical, health-care, and consumer products companies in safety
testing, arthritis, cardiovascular diseases, asthma, obesity, diabetes,
hematopoeisis (anemia), cholesterol metabolism, skin sensitization, and personal
care products.
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