Bio Screening Industry News

Archive for December, 2006

December 6, 2006

4SC AG has Received Clinical Trial Approval by Authorities and has Started the Clinical Phase IIa Study

Filed under: Drug-Like Compounds, Europe, ChemInformatics, Press Releases — admin @ 9:28 pm

PLANEGG-MARTINSRIED, Germany, December 4/PRNewswire/ — The drug discovery and development company 4SC AG (Frankfurt, Prime standard: VSC) announced today the beginning of a clinical phase IIa - study of drug candidate SC12267 for the treatment of patients with rheumatoid arthritis. 4SC AG received the necessary approval by the Federal Institute for Drugs and Medical Devices, Germany (BfArM) as well as a positive ethics vote from the Medical Faculty of the Friedrich-Alexander-University Erlangen-Nuremberg, Germany.

The study will take place at twelve centres in Germany, Poland and Serbia. The application process for Serbia and Poland is still under authority review.

“Approval for the phase IIa study on rheumatoid patients is an important step in our corporate development”, remarked Ulrich Dauer, CEO of the 4SC AG. “With the beginning of this clinical study we have reached a very important milestone on the road to opening up the market potential of our drug candidate.”

The participating physicians at centres in Germany are now beginning to recruit patients. Altogether, 120 patients afflicted with Rheumatoid Arthritis are included in the study. The study is randomised and placebo-controlled. SC12267 will undergo random testing using three groups of patients. Two groups will be administered different dosages of the substance; the third group will receive a placebo. An analgesic (paracetamol) will be administered to alleviate arthritis related pain, if required.

The goal of the study is to find the optimal dosage of the drug candidate and to examine its therapeutic potency and security. The results of this study are expected at the end of 2007.

“Quick clinical trial approval by the authorities to start our Phase IIa study is confirmation of the extraordinary achievement of our development team,” stressed Gerhard Keilhauer, CDO (Executive Committee for Development) of 4SC AG. “With this step we are building a foundation for new and promising possibilities for treatment of serious autoimmune diseases such as Rheumatoid Arthritis.”

Rheumatoid Arthritis

Rheumatoid Arthritis is a chronic inflammatory joint disease that afflicts 0.5 - 1% of the population; women are three times more likely to get arthritis than men are. In the late stage of the disease, irreversible damage to joint cartilage and bones occurs. Causes of this disease are genetic as well as autoimmune factors. Besides pain-relieving medicines, so-called disease-modifying medicines (DMARDs = disease modifying anti-rheumatic drugs) can be used in treatment. These drugs are used to induce a healing process.

They differ from other groups of drugs used in the treatment of rheumatoid diseases, since only they are able to stop or reduce damage caused from chronic inflammation to the joint cartilage or bone. In the most favourable cases, some DMARDs can also induce repair of damage to joints and provide support for the repair of changes that have already occurred.

SC12267

SC12267 is a new type of small molecular active agent from the class of DMARDs used for treatment of autoimmune diseases such as rheumatoid arthritis or multiple sclerosis. The substance works as a highly selective inhibitor in the biosynthesis of pyrimidine, which inhibits the proliferation of fast proliferating cells, in particular the important lymphocytes used for immune response.

The drug candidate originates in 4SC AG’s own research pipeline. In prior pre-clinical and clinical studies, an outstanding potency and favourable pharmacokinetic characteristics could already be observed in animal testing, and a tolerable dosage without relevant side effects on test subjects was determined.

About 4SC AG

4SC AG (ISIN DE0005753818) has been listed in the Prime Standard of Frankfurt Stock Exchange since 15 December 2005. Founded in 1997 and now with a staff of 59, the company develops novel drug candidates for inflammatory diseases and cancer using a cheminformatics based technology platform. Traditional high throughput screening of therapeutic agents has been transferred from the lab to the computer. Thus, the company offers substantial cost and time advantages as well as increased success rates in drug development. 4SC AG uses its patented technology platform to create a sustainable product pipeline for active agents that are developed in early clinical phases (”proof of concept”) and subsequently result in upfront and milestone payments as well as participation in sales generated by out-licensed products to the pharmaceutical industry. The pipeline currently has five projects, the first of which, on the treatment of rheumatoid arthritis, has successfully completed clinical phase I. In addition the project pipeline contains three projects in pre-clinical stage as well as one project in discovery stage. Furthermore, the company has its technology platform in co-operation projects with biotech and pharma companies and is already generating initial revenues.

NCE Discovery and DARA BioSciences Join Forces to Develop New Therapies

CAMBRIDGE, England, Dec. 6, 2006–NCE Discovery Ltd (NCED), the specialist medicinal chemistry and drug design service provider, has entered into an agreement with US-based DARA BioSciences, Inc. to work together on the development of new drug target molecules.

DARA BioSciences discovers and develops small molecule treatments for metabolic and CNS diseases and, under the terms of the agreement, will have access to NCED’s full range of medicinal chemistry expertise, initially to address two specific drug targets. Financial terms of the agreement were not disclosed.

“This collaboration is another prime example of NCE Discovery’s successful operations as a service provider in the US pharmaceutical market,” said Chris Sharman, NCED’s CEO. “We welcome the opportunity to work with the team at DARA BioSciences to speed up the discovery and development of important new medicines.”

John Didsbury, Chief Scientific Officer at DARA BioSciences, commented: “We are looking forward to working with NCED and believe that the medicinal chemistry capabilities it brings to the collaboration will help tremendously with our development program of potential new therapies.”

NCE Discovery provides a range of specialist medicinal chemistry services to help its clients to accelerate their drug discovery programs, from initial planning through to target identification of clinical drug candidates.

For more information, contact Chris Sharman at NCE Discovery Ltd., 418 Cambridge Science Park, Milton Road, Cambridge. CB4 0PA Tel: +44 (0)1993 201801 Fax: +44 (0)1993 200401 Email: c.sharman@ncediscovery.com, www.ncediscovery.com

About NCE Discovery NCE Discovery Ltd provides a range of specialist medicinal chemistry services to the biotechnology sector in order to accelerate its clients’ drug discovery and development activities. The Company can support and design comprehensive medicinal chemistry programs - from hit finding through to pre-clinical development. These programs are designed and delivered by experienced medicinal chemists working in fully equipped laboratories, supported by expert computational chemistry using industry-leading software tools. Services offered by NCE Discovery include: * drug discovery program management, from early proof-of-concept studies through to delivery of candidate drugs * medicinal chemistry: hit identification through to lead optimisation * structure-based drug design including small molecule and protein modelling * screening collection design and enhancement * data handling and cheminformatics.

More information on NCE Discovery Ltd can be found at www.ncediscovery.com or info@ncediscovery.com

Halozyme and Roche Enter Agreement for the Application of Enhanze, A Novel Technology to Improve Drug Delivery

BASEL, Switzerland and SAN DIEGO, Dec. 5 /PRNewswire/ — Halozyme Therapeutics, Inc. (AMEX:HTI) and Roche today announced they have entered into an agreement to apply Halozyme’s proprietary Enhanze(TM) Technology to Roche’s biological therapeutic compounds. Enhanze Technology is Halozyme’s proprietary drug delivery technology based on its recombinant human hyaluronidase (rHuPH20). rHuPH20 is an analogue of a human enzyme that temporarily clears space in the matrix of tissues such as skin. This clearing activity should allow rHuPH20 to improve drug delivery by enhancing the entry of therapeutic molecules through the subcutaneous space.

“Roche is a global leader in the development of biologics and we are excited to be applying our rHuPH20 technology to this area with Roche compounds,” said Jonathan Lim, MD, Halozyme’s President and CEO. “We believe that our technology can enhance the clinical benefits that biologics have already been shown to provide. In every respect, both technically and commercially, this represents a landmark agreement for Enhanze Technology and for Halozyme.”

“We are looking forward to working together with Halozyme using their rHuPH20 technology,” said Peter Hug, Roche’s Global Head of Pharma Partnering. “The potential to improve the administration and bioavailability of subcutaneous medicines presents an important advance to make a difference to patients’ lives.”

Halozyme Roche Collaboration

Under the terms of the agreement, Roche will pay Halozyme $20 million as an initial upfront payment for the application of rHuPH20 to three pre-defined Roche biologic targets. Over the next ten years, Roche will also have the option to exclusively develop and commercialize rHuPH20 with an additional ten targets. Pending the successful completion of a series of clinical, regulatory, and sales events, Roche may pay Halozyme further milestones which could potentially reach a value of up to $111 million as well as royalties on potential product sales for the first three targets. For each of the additional ten targets, Roche may pay Halozyme further upfront and milestone payments of up to $47 million per target. In addition, the Roche Venture Fund will make an $11 million equity investment, representing approximately 5% of Halozyme’s outstanding common stock.

Under the collaboration, Roche will also obtain access to Halozyme’s expertise in developing and applying rHuPH20 to Roche targets. Roche will obtain a worldwide, exclusive license to develop and commercialize product combinations of rHuPH20 and Roche target compounds resulting from the collaboration.

About Enhanze Technology

Enhanze Technology is Halozyme’s proprietary drug delivery technology based on recombinant human hyaluronidase (rHuPH20), a recombinant form of the naturally occurring human enzyme approved by FDA for its ability to break down hyaluronic acid (HA), the space-filling “gel”-like substance that is a major component of tissues throughout the body. When combined or co-formulated with certain injectable drugs, Enhanze Technology can act as a “molecular machete” to facilitate the penetration and dispersion of these drugs by temporarily opening flow channels under the skin. Molecules as large as 200 nanometers may pass freely through the perforated extracellular matrix, which recovers its normal density within approximately 24 hours, leading to a drug delivery platform which does not permanently alter the architecture of the skin.

About Roche

Headquartered in Basel, Switzerland, Roche is one of the world’s leading research-focused healthcare groups in the fields of pharmaceuticals and diagnostics. As a supplier of innovative products and services for the early detection, prevention, diagnosis and treatment of disease, the Group contributes on a broad range of fronts to improving people’s health and quality of life. Roche is a world leader in diagnostics, a leading supplier of medicines for cancer and transplantation and a market leader in virology. In 2005 sales by the Pharmaceuticals Division totaled 27.3 billion Swiss francs, and the Diagnostics Division posted sales of 8.2 billion Swiss francs. Roche employs roughly 70,000 people in 150 countries and has R&D agreements and strategic alliances with numerous partners, including majority ownership interests in Genentech and Chugai. Additional information about the Roche Group is available on the Internet (www.roche.com) or in the U.S. (www.roche.us).

About the Roche Venture Fund

The Roche Venture Fund advises Roche on investments in early stage biotech and diagnostics companies to support innovative technologies and medicines. Based in Basel, Switzerland, the Roche Venture Fund manages a portfolio of over 25 companies in 10 countries.

About Halozyme

Halozyme is a biopharmaceutical company developing and commercializing recombinant human enzymes for the drug delivery, palliative care, oncology, and infertility markets. The company’s portfolio of products is based on intellectual property covering the family of human enzymes known as hyaluronidases. Halozyme’s recombinant human enzymes may replace current animal slaughterhouse-derived extracts that carry potential risks of animal pathogen transmission and immunogenicity. The company has received FDA approval for two products: Cumulase(R), the first and only recombinant human hyaluronidase for cumulus removal in the IVF process; and Hylenex for use as an adjuvant to increase the absorption and dispersion of other injected drugs. The versatility of the first enzyme, rHuPH20, enables Halozyme to develop the product as a medical device, drug enhancement agent, and therapeutic drug.

Multiple Myeloma Research Foundation (MMRF) Awards $1 Million Each in Funding to ProChon Biotech and Semafore Pharmaceuticals to Advance Drug Development

NORWALK, Conn., Dec. 5 /PRNewswire/ — The Multiple Myeloma Research Foundation (MMRF), the largest non-profit foundation dedicated to accelerating a cure for multiple myeloma, today announced that Semafore Pharmaceuticals, Inc. and ProChon Biotech Ltd. are the recipients of the organization’s first LEAD (Leveraging Existing Multiple Myeloma Targets to Accelerate Drug Discovery and Development) research and development grants.

The MMRF’s LEAD program is a multi-year research grant commitment intended to drive and accelerate the development of innovative and effective multiple myeloma treatments by funding the development of lead compounds through the early stage drug development process that could have significant impact on existing or future myeloma treatments. The MMRF will commit up to $6 million over the next two to three years in support of this program.

“Today, funding for preclinical research and early-stage clinical trials is extremely limited. As the world’s largest private funder of myeloma research, we decided that we needed to invest directly in this research to ensure myeloma patients, who have a 32% five-year survival rate, have effective options in the future,” said Kathy Giusti, Founder and Chief Executive Officer of MMRF, as well as a myeloma patient. “Through the innovative LEAD program, the MMRF is investing directly to biotechnology companies for this research that is not typically funded by NIH, private foundations, or venture capital firms.”

The LEAD Program grants will be applied to the ongoing development of Semafore Pharmaceuticals’ SF1126 and ProChon Biotech’s PRO-001 compounds, including their testing in human clinical trials throughout 2007-2009.

“This funding will enable Semafore to advance the development of SF1126 as a promising new treatment for multiple myeloma in parallel with our solid tumor development program, instead of it taking a back seat,” said Dr. Joseph Garlich, Semafore President and Chief Scientist. “This funding leverages all the preclinical work performed with SF1126 and comes at a perfect time for the company as we initiate Phase I solid-tumor focused clinical trials and now are in a position to take on this expansion of our target patient population.”

SF1126 is a small molecule that selectively inhibits PI3K Class IA isoforms and other key members of the PI3K pathway such as DNA-PK and mTOR. Recent advances indicate that these targets play a critical role in the progression of cancer and many groups are searching for effective safe inhibitors of these targets. In preclinical studies, SF1126 has been shown to be a key regulator of many of the processes involved in tumor growth and dissemination. Preclinically, SF1126 inhibits angiogenesis, induces apoptosis, controls upstream and downstream signaling and produces synergistic anti-tumor effects in combination with chemotherapy and radiation. SF1126 has demonstrated promising activity in a variety of preclinical cancer models, including prostate, breast, ovarian, lung, leukemia, multiple myeloma, brain and other cancers.

“We are extremely grateful to the MMRF for providing us this research grant through its industry-leading LEAD program,” said ProChon President and Chief Scientist Prof Avner Yayon. “These resources will play a significant role in our development of the new PRO-001 treatment for patients who have a subtype of multiple myeloma that has a very poor prognosis. We are looking forward to working with leading clinical centers at the forefront of treatment for multiple myeloma.”

The association of fibroblast growth factor receptor 3 (FGFR3) expression with t(4;14) multiple myeloma and the demonstration of the transforming potential of this receptor tyrosine kinase (RTK) make it a particularly attractive target for the development of anti cancer drugs. ProChon’s inhibitory anti-FGFR3 antibody, PRO-001, binds to FGFR3 expressed on transformed cells and inhibits receptor autophosphorylation and downstream signaling resulting in the death of the tumor cells. PRO-001 is a completely human, highly specific antibody and this grant will enable preclinical and clinical testing of the promising potential exhibited in cell culture.

About Multiple Myeloma

Multiple myeloma is an incurable cancer of the plasma cell, with a five- year survival rate of only 32 percent — one of the lowest of all cancers. Approximately 50,000 people in the United States are living with multiple myeloma and an estimated 16,000 new cases are diagnosed each year. Although the peak age of onset of multiple myeloma is 65 to 70 years of age, recent statistics suggest that incidence is increasing and at an earlier age.

About the Multiple Myeloma Research Foundation

The Multiple Myeloma Research Foundation (MMRF) was established in 1998 as a 501(c)3 non-profit organization by twin sisters Karen Andrews and Kathy Giusti, a newly diagnosed multiple myeloma patient, with the unique mission of accelerating the search for a cure for multiple myeloma. Today, the MMRF is the largest non-profit foundation dedicated to the single mission of accelerating the search for a cure for multiple myeloma. As the world’s number one funder of myeloma research, the MMRF has raised more than $70 million to fund more than 200 research grants at more than 70 research institutions around the globe. Currently, the MMRF is funding more than 30 new compounds and approaches — in pre-clinical testing and Phase I, II and III clinical trials — that show promise in treating patients at all stages of the disease. For more information about the MMRF, please visit http://www.multiplemyeloma.org/.

About Semafore

Semafore Pharmaceuticals, Inc. is an Indianapolis-based drug discovery and development company focused on small molecule modulators of the PI3 Kinase (PI3K) and PTEN cell signaling pathway, one of the most promising pathways for multiple disorders, including the company’s focus, cancer. Semafore is one of the first biopharmaceutical companies to focus on both PI3K and PTEN and has successfully discovered and is developing a portfolio of drug candidates. The company expects to file an IND for its lead clinical candidate, PI3K inhibitor SF1126, in December 2006. Semafore has also discovered the first drug-like small molecule PTEN modulators for cancer therapy, cell protection and therapeutic angiogenesis. For more information see the company’s website at http://www.semaforepharma.com/.

About ProChon

Established in 1997, ProChon Biotech is an Israeli biotech company devoted to the discovery, development and commercialization of novel therapeutic approaches for tissue regeneration and the treatment of genetic and acquired skeletal disorders. ProChon’s therapeutic approach to cancer exploited through its sister company Fibron Ltd., stems from its proprietary know-how of one of the largest and most versatile growth factor systems in the human body, the Fibroblast Growth Factors (FGF) system. These key regulators of tissue growth regeneration and repair are critically involved in human pathology. For more information visit the company’s website at http://www.prochon.com/.

Wyeth acquires global license for Inpharmatica’s Admensa Interactive™

Inpharmatica Ltd today announces that Wyeth Pharmaceuticals, a division of Wyeth has licensed Admensa Interactive, Inpharmatica’s platform of predictive drug absorption, distribution, metabolism and excretion models and compound prioritization tools.

Wyeth will use Admensa Interactive to support compound selection and optimization in its drug discovery projects.

This new license, agreed after an extensive evaluation, further demonstrates the value that Admensa Interactive brings to pharmaceutical and biotechnology companies.

Under the terms of the agreement, Wyeth will receive a multi-site license to Admensa Interactive.

Admensa Interactive combines predictive models with a desktop interface combining model output with project data from other sources.

This integrated selection and visualization platform drives effective decisions on the best compounds on which to move forward against project criteria.

Admensa Interactive is a major component of Inpharmatica’s range of gene-to-candidate technologies which integrate biology and chemistry-based drug discovery activities.

Inpharmatica’s platform ranges from target selection based on druggability, through rapid identification of hits to selection of high quality leads and pre-clinical candidates, which are prioritized on the basis of good drug-like characteristics.

“We are delighted that Wyeth has opted for a broad deployment of Admensa Interactive in support of its drug discovery projects,” said Matt Segall, Head of the Admensa Business Unit of Inpharmatica.

“The strong uptake of this product by top pharma and biotech companies is a testimony to the unique capabilities it provides for compound optimization.”

Further Information: http://www.inpharmatica.com/admensa.htm

Scientists Identify Synthetic Compound That Keeps Stem Cells Young

A team of scientists from the Scripps Research Institute, the Genomics Institute of the Novartis Research Foundation and the Max Planck Institute for Molecular Biomedicine has discovered a new synthetic compound that can support growth and self-renewal of mouse embryonic stem cells, offering a simple alternative to current growth conditions that may vary batch-to-batch and confuse experimental results.

The findings, reported in this week’s Proceedings of the National Academy of Sciences, should accelerate stem cell research and offer new insights into cell biology that could aid in the development of treatments for diseases such as cancer and Parkinson’s.

Embryonic stem cell research has been plagued by problems arising from undefined conditions for growing and differentiating stem cells. Embryonic stem cell culture dishes are commonly coated with inactivated fibroblast cells known as “feeder cells.” These feeder cells offer embryonic stem cells a suitable attachment surface and also release largely uncharacterized nutrients into the culture medium that support stem cell growth in the undifferentiated state. A variety of other factors are also added to promote stem cell growth and, most importantly, force the cells to maintain their pluripotency-their ability to become a variety of other final, specialized types of cells.

The end result is that such conventional culture conditions often suffer large variability, and make it extremely difficult for scientists to tease out the impact of individual molecules on experimental results.

“Stem cell applications and studies have been hampered by using undefined culture conditions” says Sheng Ding, an assistant professor at Scripps Research who led the research.

Feeder cells can also introduce viral and other forms of contamination that may lead to rejection of stem cells by the human immune system, among other problems.

Ding and his colleagues set out to solve these culturing problems using high-throughput screening of a Scripps Research library of tens of thousands of synthetic small molecules in search of a compound that could eliminate the need for feeder cells and added factors. This initial screening led to the discovery of a class of pyrimidines that improved cell growth. Later, the team produced a library of analogs of this class that proved to include a single compound, dubbed “pluripotin,” that supports self-renewal of mouse embryonic stem cells and maintains their pluripotency alone with only the addition of standard cell culture basal medium.

The Ding group has also shown that pluripotin improves the growth of human embryonic stem cells, although other factors are still required to maintain their pluripotency. However, the team is already screening the Scripps Research library to identify a synthetic compound or compounds that will single-handedly maintain the human cells as pluripotin does for mouse cells. Ongoing research with pluripotin has revealed that the compound controls the stem cells via a novel mechanism. Pluripotin appears to simultaneously block the activity of the proteins RasGAP and ERK1, both of which have cell differentiation inducing activity.

“The mechanism of pluripotin suggests new strategies for maintaining and propagating stem cells,” says Ding. “Such a discovery of a single small molecule that operates through two different classes of targets to achieve a desired biological effect also has fundamental implications for drug discovery.”

Work with pluripotin and compounds that may follow should dramatically improve researchers’ ability to work effectively with stem cell lines, Ding says, and should facilitate the practical application of stem cell research in developing therapies.

The work also offers benefits beyond improved stem cell culture. “Pluripotin and other such molecules are likely to provide insights into the molecular mechanisms that control stem cell fate and ultimately may be useful for in vivo stem cell biology and therapy studies,” says Ding.

In addition to Ding, authors of the paper, titled “Self-renewal of embryonic stem cells by a small molecule,” are: Shuibing Chen, Qisheng Zhang, and Shuyuan Yao of The Scripps Research Institute; Jeong Tae Do and Hans R. Schöler of the Max Planck Institute for Molecular Biomedicine; Feng Yan and Eric C. Peters of the Genomics Institute of the Novartis Research Foundation; and Peter G. Schultz of The Scripps Research Institute and the Novartis Research Foundation.

The project was supported by the Genomics Institute of the Novartis Research Foundation.

Setting The Stage To Find Drugs Against SARS

Scientists at the U.S. Department of Energy’s Brookhaven National Laboratory have set the stage for the rapid identification of compounds to fight against severe acquired respiratory syndrome (SARS), the atypical pneumonia responsible for about 800 deaths worldwide since first recognized in late 2002. Researchers from Brookhaven’s biology department and the National Synchrotron Light Source (NSLS) characterized a component of the virus that will be the target of new anti-SARS virus drugs. The results were published online by Biochemistry on November 17, 2006.

“Although vaccines against viruses are very effective, vaccines for viruses that mutate rapidly - such as the viruses that cause SARS, AIDS, and bird flu - are much more difficult to obtain,” said Brookhaven biologist Walter Mangel, the lead author of the paper. “Even if a vaccine is available, antiviral agents are important in stopping the spread of highly infectious viruses. If antiviral agents for SARS had been available, they could have been used to contain the outbreak to the initial site of the infection.”

The researchers studied the SARS main proteinase, an enzyme used by the virus during infection to cut newly made viral proteins into gene-sized, functioning pieces. If the proteinase is prevented from working, the virus infection is aborted. Previous studies have revealed that the proteinase is inactive when in the form of single molecules. But once two of those molecules bind together to make what is called a dimer, the enzyme becomes active and is able to play its role in SARS virus reproduction. The challenge for researchers, and the focus of the Brookhaven study, was to determine the concentration at which individual proteinase molecules form active dimers. Knowing this concentration, for which estimates at other laboratories have varied greatly, would allow researchers to search for anti-SARS drugs more efficiently by ensuring that the proteinase used in tests is initially in its active form.

Using three different scientific techniques, including x-ray scattering at the NSLS, the Brookhaven researchers obtained almost identical values for this concentration. Now that this crucial value has been narrowed down to a precise range, researchers can focus on finding compounds that bind to the active form of the enzyme.

“Targets for antiviral drugs must be carefully chosen such that binding to it prevents the virus from reproducing,” Mangel said. “Viral proteinases are excellent targets for antiviral drugs. One reason so many people are surviving the AIDS epidemic is the effectiveness of drugs targeted to the proteinase of human immunodeficiency virus (HIV).”

One way to obtain compounds that bind to a proteinase is via high-throughput screening. Chemical libraries containing tens of thousands of small compounds are available that can be searched for effective drugs against various diseases. Small amounts of a target, e.g., an active viral proteinase, are placed in tiny wells in a plate, and a different compound from the library is added to each well.

To determine whether a compound binds to and inhibits the proteinase, an additional molecule is added that changes color in the presence of an active proteinase. Wells that don’t show a color change therefore contain compounds that inhibit the proteinase, and could be effective antiviral agents. Earlier this year, Mangel’s research group published a procedure on the synthesis of a new compound that changes color in the presence of the active form of the SARS main proteinase.

However, for this screening process to work, the SARS proteinase inserted into the wells has to be active to begin with. Knowing the concentration range for dimer formation will therefore help researchers in their search for a compound to stop the virus. “Now that the stage is set, high-throughput screening can begin,” Mangel said. “Hopefully, it will yield an antiviral agent that can be stockpiled before a virulent strain of the virus reappears.”

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This research was supported by the Office of Basic Energy Sciences within the U.S. Department of Energy and the National Institutes of Health.

Definiens Enhances Drug Development Process

Filed under: Europe, ChemInformatics, Press Releases, Medicinal Chemistry — admin @ 8:18 pm

Definiens Cellenger: Flexible and Platform-independent Enterprise Solution Automates and Standardizes Cell Image Analysis Tailored to Specific Assays.

MUNICH, Germany and VIENNA, Austria - November 6, 2006 - Definiens AG, the number one Enterprise Image Intelligence solution provider, today introduced Definiens CellengerR v1.4. It is being announced at the High-Content Analysis Europe, November 6-8, Vienna, the most promising European event of the year focusing on high-content cellular assays for compound screening and pathway analysis. The new version of Definiens Cellenger is designed to help pharmaceutical and biotechnology companies analyze automated cell-based assays from any source, creating a deeper understanding of image data. It provides a simple yet flexible environment to support and accelerate the drug development process across the entire enterprise. Definiens Cellenger v1.4 is available immediately.
Built on the Definiens Cognition Network TechnologyT, Definiens Cellenger enables organizations to go beyond the simple measurement of objects by shape and intensity to the quantification of complex relationships between objects, revealing subtle biological effects. It enables much deeper understanding of image data and complements all workflows, whether they are assay development, screening or informatics. Definiens Cellenger is the first true platform-independent high-content analysis software, bridging the gaps between different vendors and platforms offering an unbiased and objective view of the data. It allows standardization of assays across the enterprise, consolidating training and expertise as well as knowledge to be transferred seamlessly between work groups.
Definiens Cellenger contains highly robust detection and classification algorithms which provide accurate multi-dimensional segmentation of objects, even with heterogeneous cell populations or of imperfect images that were taken under poor conditions. Multiple image analysis experiments can be performed in parallel and export data can be configured to contain the results of one experiment conditional to the results of another. This leads to much higher data confidence levels.
“Definiens Cellenger enables you to go beyond traditional assay development; it gives you faster results and better insight into any biological question you have; independent of platform, assay complexity, and type of stain,” said Dr. Wolfgang Rencken, Vice President Technology and Products at Definiens AG. “It is built to meet the needs of the most demanding global organizations.”
Definiens Cellenger has open interfaces and formats and, as with all DefiniensR products, is designed to seamlessly integrate within existing technology infrastructures, complementing rather than replacing existing investments in software and hardware.
Definiens Cellenger version 1.4 - new features include:

> Modifiable pre-defined solutions for common assay tasks

> New detection, measurement and export actions

> Training based classification

> Plate based statistics and quality control metrics

> Full customization and extension of the Cellenger library

> Tightly integrated data representations

> More seamless support and a wider range of image acquisition systems

> Support for metadata import and use within analysis process.

> Server processing on Linux
A datasheet covering the technical details and all new features of Definiens Cellenger v1.4 is available upon request.

About Definiens AG

Definiens is the number one provider of Enterprise Image Intelligence solutions. Leading corporations deploy Definiens’ solutions across their organizations to automate image-intensive business processes. Definiens’ clients enjoy high return on investments by significantly reducing the cost and risk of image-related information, enabling higher quality decisions faster, speeding time-to-market.
Definiens’ products and solutions are built on its platform technology Definiens eCognitionT that represents a quantum leap in digital image analysis. The advanced and robust image analysis solutions classify images more intelligently, more accurately, and more efficiently than traditional methods. Definiens concentrates on the Life Sciences and Earth Observation/Remote Sensing markets. The Definiens technology is used to accelerate the drug discovery, development, and diagnostics processes and also enables satellite and aerial image classification.

In Life Sciences, Definiens helps address a wide range of challenges including analysis of cells in High Content Screening, detailed quantitative analysis of structure in tissue, normal and abnormal screening in toxicological pathology and interpretation of 3D data in radiology.
Definiens is headquartered in Munich, Germany and has offices located in the USA and Europe.
Definiens, Definiens Cellenger, Definiens Cognition Network Technology, Definiens eCognition, Enterprise Image Intelligence, We Understand Images, Cellenger MVA, Definiens Polymind, Polysoph, amaccs, Definiens Cognitionware, Definiens Arraylogic, WeaverWare and fractal life are trademarks or registered trademarks of Definiens AG in Germany and/or its subsidiaries in other countries. All other names are the trademarks or registered trademarks of their respective companies.

Compatibility of Cell-Based Assays with High-Throughput Screening Proving to Be a Key Challenge

Filed under: Europe, Press Releases, HT Screening — admin @ 8:15 pm

DUBLIN, Ireland–(BUSINESS WIRE)–Research and Markets has announced the addition of Development of Cell-Based Assays (Technical Insights) to their offering.

This Frost & Sullivan research service titled Developments in Cell Based Assays focuses on the technological advancements, emerging trends, drivers, and challenges affecting the development of cell-based assays. The research service provides information on major companies and academic institutions involved in the development of innovative technology and products. A summary of key patents gives an insight into notable activities, technology trends, and important participants in this field.

Market Sectors

Expert Frost & Sullivan analysts thoroughly examine the following market sectors in this research:

  • Healthcare - Drug Discovery

Technologies

The following technologies are covered in this research:

  • High Throughput
  • Multiplexing

Market Overview

Compatibility of Cell-based Assays with High-throughput Screening Proving to be a Key Challenge

The ability to generate significant time and cost savings is pushing many pharmaceutical and biotechnology companies to favour cell-based assays over other methods such as biochemical and in-vitro assays. Cell-based assays are finding numerous applications in target identification and validation, monitoring cellular events, as well as the screening compounds for efficacy and biosafety. Researchers now face the challenge of ensuring greater compatibility with high-throughput screening (HTS), which is emerging as one of the most sought-after technologies to perform cell-based assays. HTS provides ideal support for cell-based assays by not only increasing the number of analyzed samples, but also offering high-quality information. Used in combination with HTS, cell-based assays offer greater quantity of data coupled with superior-quality data assays, leads, screening process, and compound libraries, explains the analyst of this research service.

Going forward, the focus is expected to be on easy-to-use and highly sensitive assays that provide continuous records of cellular activity. Although, most research activities currently concentrate on drug discovery, cell-based assays are expected to gain popularity in diagnostics, molecular biology, biochemistry and neuroscience, genetics, toxicology studies, bioengineering, and proteomics, among other fields as they become more cost-effective and biologically significant.

Focus on Developing Robust and Reliable Cell-based Assays

The increasing demand for higher-quality output, healthier consistent cells, and improved assay data in drug discovery is leading researchers to focus on developing robust and highly reliable assays through the automation of well-characterized cell lines. The automation of cellular assays is also likely to improve the drug discovery process by identifying the right leads and by understanding their chemistry more accurately. Although the automation of cell-based assays is expected to be a hugely popular trend, the key is to ensure strict environment control due to the involvement of live cells. For example, automated incubators store stacks of microplates at a controlled temperature and humidity.

Miniaturization is another step toward more-efficient cell-based assays. Recent advances in assay chemistries and signal detection technology allow the miniaturization of cell-based assays, making it convenient to perform dose-response experiments during primary screens. Simpler and faster screening is also possible though the use of homogenous assay techniques for radioactive, fluorescent, and luminescent assay formats. Homogenous assay formats are user-friendly and also minimize errors by allowing the direct use of cell samples or lysine and other reagents, without having to purify or separate them before taking measurements, says the analyst.

For more information visit http://www.researchandmarkets.com/reports/c46516

Galapagos to acquire Inpharmatica

Filed under: Business and Investment, Europe, Press Releases — admin @ 8:12 pm

Acquisition broadens drug discovery capabilities and services

Webcast Conference Call Scheduled for 10.00 AM CET on 6 December, 2006

• Acquisition price of €12.5 million in all-share transaction

• Acquired assets include an estimated €6 million in cash (of which half is due by December 31, 2006)

• Potential all-share earn out payments of maximum €6.6 million based on pre-agreed commercial milestones

• Technology will accelerate Galapagos’ drug development

• Services will add breadth and depth to BioFocus DPI offering

• Estimated 2006 Inpharmatica revenues of €4.7 million

Mechelen, Belgium, and London, UK, 6 December, 2006; Galapagos NV (Euronext & London AIM: GLPG), an integrated drug discovery company, and UK-based Inpharmatica Ltd. today announced that they have entered into a definitive agreement under which Galapagos will acquire Inpharmatica in an all-share transaction. The acquisition price of Inpharmatica is in three components: the ongoing business is valued at €6.5 million, the estimated cash at an additional €6 million (of which half is due by 31 December 2006), and the potential maximum earn-out related to commercial milestones at €6.6 million.

Galapagos will issue, on the basis of €8.82 per share (the average GLPG share price over the last thirty days prior to 5 December 2006), a maximum of 2,165,532 new shares assuming that all three components are fully delivered. The new shares will be issued to the Inpharmatica shareholders in three tranches. The first tranche of 623,582 new Galapagos shares shall be issued in December 2006. Two subsequent tranches are due to be issued in April and May 2007. The exact number of shares to be issued in these two tranches at that time will be dependent upon certain pre-agreed contractual conditions.

All issued shares will be subject to a lock up agreement ending 10 May 2007. Galapagos shall apply for a listing of the newly issued Galapagos shares on Euronext Brussels and Euronext Amsterdam, subject to the approval by the Belgian Banking Finance and Insurance Commission (BFIC-CBFA) of a prospectus as required under applicable Belgian law, as well as on London AIM.

Inpharmatica is a world-leader in the development and application of powerful, genome-scale predictive products and services for drug discovery research. The company’s technologies for drug discovery will bolster Galapagos’ leading position in this field by improving the Group’s ability to select targets and compounds based on predictive models and expertise. These technologies include ADME services (Admensa™), a novel approach to prioritize chemical compounds in drug screening, as well as chemo-informatics services (Chematica™) to select the best targets for drugability . Both technologies have already been widely adopted by the pharmaceutical industry and enjoy a track record of success. Major new customers brought by Inpharmatica to the Galapagos group include Pfizer and Schering.

Inpharmatica will become part of BioFocus DPI, Galapagos’ drug discovery services business. BioFocus DPI will assume the commercial and scientific management of Inpharmatica, including the execution of all current contracts of Inpharmatica. As a consequence of the acquisition, the companies anticipate downsizing of Inpharmatica’s management, sales and administrative staff positions. The current CEO and CFO will assist in handover until 31 December 2006 and 31 March 2007 respectively. Immediate annualized operational synergies are expected to amount to about €1.5 million. As part of the acquisition, Galapagos will obtain certain downstream financial rights to Inpharmatica’s internal PPAR-delta program, addressing obesity and diabetes, which has reached the stage of candidate selection.

“We are excited to add the distinguished drug discovery capabilities of Inpharmatica to our BioFocus DPI business. Adding proprietary target and compound selection tools to our platform provides an even broader array of drug discovery solutions for both our internal R&D and for our services business,” commented Onno van de Stolpe, CEO of Galapagos. “It will position our company further for additional turn-key deals ranging from target discovery all the way to clinical Proof of Concept.”

“We believe that the merger of our drug discovery service operations into BioFocus DPI creates the best value for our shareholders”, said John Lisle, Inpharmatica’s CEO. “Integrating Admensa and Chematica within the BioFocus DPI offering will greatly increase their commercial potential and opportunity.”

Rationale and strategy of acquisition by Galapagos

Galapagos acquires Inpharmatica as part of its strategy to build a worldwide leader in drug discovery services, ranging from target discovery all the way through to the delivery of compounds with clinical Proof of Concept.

Galapagos will integrate Inpharmatica into its service division BioFocus DPI. Inpharmatica currently employs around 30 people in Cambridge and London, UK; The majority of this staff will join BioFocus DPI and will bring the total Galapagos headcount to over 380 staff in seven countries.

Galapagos will also employ this acquired capability in its own drug discovery programs in bone and joint diseases, where it aims to bring its own candidate drugs into the clinic.

The acquisition of Inpharmatica fits within Galapagos’ strategy to partner with pharmaceutical and biotechnology companies in turn-key drug discovery collaborations, as it strengthens the company’s breadth of technologies and services. Galapagos entered such a turn-key alliance with GlaxoSmithKline in osteoarthritis in June 2006 and intends to complete two more such turn-key deals in the coming three years.

The predictive drug discovery capabilities acquired are expected to accelerate Galapagos’ own R&D pipeline by enabling prioritization of its validated targets and the chemical lead compounds in the process of drug development.

Webcast Conference Call details

Galapagos will host a conference call discussing the transaction on 6 December, 2006 at 10.00 AM CET/ 9.00 AM GMT. To participate in the call, dial +32 2290 1608 ten minutes in advance of the call. A live webcast of the conference call can be accessed on the Galapagos and Inpharmatica websites at www.glpg.com and www.inpharmatica.co.uk, respectively. An archived version of the webcast will be available later today and archived on both company’s websites for 30 days.

About Galapagos

Galapagos is a publicly traded, genomics-based drug discovery company (Euronext Brussels, GLPG; Euronext Amsterdam, GLPGA, London AiM: GLPG) that has drug discovery programs based on proprietary, novel targets in bone and joint diseases - osteoarthritis, osteoporosis and rheumatoid arthritis. Galapagos offers a full suite of target-to-drug discovery products and services to pharmaceutical and biotech companies through its division BioFocus DPI, encompassing target discovery and validation, and drug discovery services through to clinical Proof of Concept. In addition, BioFocus DPI provides adenoviral reagents for rapid identification and validation of novel drug targets and compound libraries for screening. Prior to this transaction, Galapagos employed more than 360 staff, and occupies facilities in the US, the UK, Belgium, Switzerland, Germany and the Netherlands. Galapagos maintains its revenue guidance for 2006 of €33-38 million. More information about Galapagos and BioFocus DPI can be found at www.glpg.com.

About Inpharmatica

Inpharmatica is a privately held drug discovery company. Founded in 1998, the company employs around 30 people at its UK locations in London and Cambridge. Major investors include 3i, GIMV, Advent Venture Partners, Abingworth, Gilde and Reed Elsevier Ventures. The principal capability of Inpharmatica is to effectively manage and leverage the overwhelming gene, protein and drug compound related data generated in drug discovery.

The company offers a full set of predictive capabilities, database products and consultancy services to accelerate the drug discovery process and enable creation of high quality Candidate molecules. Inpharmatica reported an audited operating loss of €11.9 million for the year ended 31 December 2005, mainly attributable to the discovery unit, and net assets of €10.9 million (before preference share debt of €18.5 million, which will be eliminated upon consolidation by Galapagos). The discovery unit was closed during 2006, consolidating operations towards services, and Inpharmatica is in advanced stages of agreeing a partner for its PPAR delta discovery program.

Galapagos acquired the continuing service operations as well as the downstream PPAR-delta rights. It has two remaining service business units:

Chematica™, which enables effective selection of the best biological targets and the most appropriate drug-like chemistry starting points for advancement; and

Admensa™, which enables the highly efficient selection of chemical compounds with the optimal balance of ADME properties.

Inpharmatica is a very well-known and highly-regarded partner to the pharma and biotech industries with excellent connections in most leading companies worldwide.

More information about Inpharmatica can be found at www.inpharmatica.co.uk.

Forward Looking Statements

This release contains certain forward-looking statements that involve risks and uncertainties that could cause actual results to be materially different from historical results or from any future results expressed or implied by such forward-looking statements. You are urged to consider statements that include the words “may,” “will,” “would,” “could,” “should,” “believes,” “estimates,” “projects,” “potential,” “expects,” “plans,” “anticipates,” “intends,” “continues,” “forecast,” “designed,” “goal,” or the negative of those words or other comparable words to be uncertain and forward-looking. Any forward-looking statements made by Inpharmatica or Galapagos speak only as of the date made. Inpharmatica and Galapagos undertake no obligation to publicly update any forward-looking statements, whether as a result of new information, future events or otherwise.

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