Archive for the ‘Drug-Like Compounds’ Category
New Compounds With Anti-Inflammatory Properties Discovered Through Expansive PhytoLogix(TM) Botanical Library
Last Updated on Thursday, 30 August 2007 12:04 Written by Fred Thursday, 30 August 2007 12:04
Lacey, WA – Researchers utilizing one of the world’s largest ethnomedicinal plant libraries recently developed two highly potent flavonoid formulas which convey topical anti-inflammatory effects. The botanicals, a catechin derived from the catechu tree and baicalin extracted from Chinese skullcap, were combined in two different formula ratios and then evaluated for anti-inflammatory and antioxidant effects. The findings1 were shared at the annual meeting of The Society for Investigative Dermatology in May.
The formulas are the final result of screening through the PhytoLogix™ library at UNIGEN® USA, a leading natural products research and development company and proprietary ingredients supplier. Utilizing PhytoLogix, researchers screened over 1,230 organic plant extracts for potential COX-2 inhibition. The final catechin and baicalin formulas, UP566S and UP566U, demonstrated significant COX-1 and COX-2 inhibitory effects. In an in vitro test using human cells, UP566U was far more effective than Ibuprofen in acting as a LOX (5-lipoxygenase) pathway inhibitor.
“These two compounds offer multiple anti-inflammatory properties. They are a completely natural and safe approach to dealing with topical inflammation,†commented Dr. Qi Jia, Chief Scientific Officer at UNIGEN. Dr. Jia explained that the
compounds demonstrated an ability to suppress the gene expression of key pro-inflammatory cytokines, and UP566S also showed antioxidant activity almost four times more powerful than vitamin C, based on ORAC test results. In a human trial, both topicals also tested negative for any skin irritation or photosensitivity.
The Company’s President and CEO, Regan Miles, was impressed with the speed at which the team was able to develop their ideas. “They created the formulas rather rapidly due to the comprehensive data available through PhytoLogix,†said Miles. “We can access not only the chemical structure of a certain botanical, but also information about all of the plant’s traditional health uses too. We’re seeing this research build on itself exponentially every day.â€Â
About Unigen Pharmaceuticals, Inc.
www.unigenUSA.com – Unigen Pharmaceuticals, Inc. is a leading natural products research and development company and proprietary ingredients supplier. The Company is dedicated to the discovery of botanically derived therapeutic compounds that address consumer health needs and help improve quality of life.
Their research and discovery includes extensive work at both the human cell and gene level. Unigen focuses on identifying and studying the unique ingredients of medicinal botanicals and then formulating proprietary raw materials for use in cosmeceutical, nutraceutical, functional food and pharmaceutical products.
Unigen’s global offices include 80 employees, 55 of whom are scientists. Contributing to their vast library of novel botanical ingredients, the current facilities include high-throughput screening and cell culture labs, bioprospecting labs and a large-scale manufacturing facility. Unigen is part of the ECONET global family of health and natural product companies, which has operations in the United States, Canada, Korea, Mexico, Russia and China.
Posted under Discoveries, Innovations and Patents, Drug-Like Compounds, North America, Press Releases | Comments Off
WUSTL creates center to study women’s infectious diseases
Last Updated on Wednesday, 23 May 2007 10:13 Written by admin Wednesday, 23 May 2007 10:13
Washington University School of Medicine in St. Louis is launching a new effort to study infectious diseases that preferentially affect women. The center for Women’s Infectious Disease Research (cWIDR) will focus on issues such as:
• microorganisms that cause urinary tract infections (UTIs) and other conditions that make urination and intercourse painful or difficult
• infections that lead to premature delivery and vaginitis
• potential contributing roles for microorganisms in life-threatening conditions such as cancer, heart disease, neurodegenerative disorders and diabetes.
“Infectious diseases of women is a tremendously underserved area,” says Scott Hultgren, Ph.D., the Helen L. Stoever Professor of Molecular Microbiology and the center’s director and principal investigator. “UTIs, for example, are one of the most common bacterial infections in women. They’re not fatal, but we need new and improved therapeutics because they’re a very significant cause of suffering, lost work days and health-care expenses.”
According to Hultgren, the center continues a University tradition of innovation and leadership in microbiology and infectious diseases. Stephen Beverley, Ph.D., Marvin A. Brennecke Professor and head of molecular microbiology, founded the center’s predecessor, the Center for Infectious Disease Research (CIDR) in 1997. He recently stepped down as director of CIDR and designated Hultgren as his successor.
Hultgren’s research has long been focused on women’s health and infectious diseases, with studies funded by the National Institute of Diabetes and Digestive and Kidney Diseases and the National Institute of Allergy and Infectious Diseases. He has also been active in the Office of Research on Women’s Health, an agency that coordinates and advises on women’s health research throughout the National Institutes of Health.
Given those interests and experiences, Hultgren decided to reconceptualize CIDR and its goals, altering the center’s name to reflect the changes.
The center for Woman’s Infectious Disease Research is part of the University’s BioMed 21 initiative, which is focusing efforts at Washington University on speedy translation of laboratory discoveries into new approaches for diagnosis and treatment of patients.
According to Larry J. Shapiro, M.D., executive vice chancellor for medical affairs and dean at the School of Medicine, studying gender-specific infections can reveal information that is helpful in a much broader range of diseases.
“Scott’s work with urinary tract infections has led to insight into how the bacteria that cause these infections sometimes defend themselves by cooperating to form a protective shield known as a biofilm,” he says. “Many common infections of both men and women employ this defense against antibiotics and the host immune system, and to improve treatment for these infections we have to devise medicines that can penetrate this shield.”
Other major infectious disease issues specific to women include interstitial cystitis or painful bladder syndrome, a condition estimated to afflict hundreds of thousands of females per year. Symptoms are similar to urinary tract infections and include frequent, painful urination and pain during intercourse. Diagnosis and treatment are difficult because scientists don’t yet know the cause of the condition.
Oral and vaginal infections with streptococcus and other bacteria have been linked to premature delivery in pregnant women. Michael Caparon, Ph.D., professor of molecular microbiology and co-director of the center for Woman’s Infectious Disease Research, plans to bring microbiologists and obstetricians to learn why and determine what can be done.
Fostering collaboration between different disciplines to create new perspectives on the big challenges of biomedicine is a primary goal of BioMed 21. Hultgren plans to establish many connections and collaborations between his center and other research centers, noting the potential for synergy provided by the Center of Genome Sciences and other research groups at the University.
“We see the center for Woman’s Infectious Disease Research as part of a multi-disciplinary network combining a powerful blend of microbial pathogenesis, genomics, structural biology, biochemistry and biophysics, and diverse imaging technologies,” Hultgren says.
As an example, Hultgren’s work with urinary tract infections led to detailed study of pili, fibers produced by the bacteria that cause the infections. Pili allow bacteria to adhere to and invade human tissues, and Hultgren’s laboratory has recently found that they help hold bacteria together in biofilms. These discoveries made it possible to design molecules that block pili formation and may one day lead to improved treatments.
Bacteria also manufacture fibers comprised of substances known as amyloids. Like pili, these materials contribute to biofilm formation and host cell colonization, but they’re much more well-known for the role they play in neurodegenerative disorders and other diseases. Hultgren hopes to recruit experts who can use bacteria to model amyloid formation and design compounds that block their assembly.
“Amyloid plaques in the brain are a primary characteristic of Alzheimer’s disease, a terrible disease affecting women and men, so we plan to offer the inhibitors we develop to neurologists as potential treatments for that disorder,” Hultgren says.
Researchers at the center for Woman’s Infectious Disease Research also will study whether microorganisms are playing a role in serious diseases not previously thought to be related to infection. As evidence of why a search for such connections might prove fruitful, Hultgren highlights the surprising discoveries that infectious agents are responsible for all stomach ulcers and most cervical cancers.
In a newer, more tentative link likely to be further probed at the center for Woman’s Infectious Disease Research, scientists have found that a receptor in the circulatory system responds to both fat deposits and bacterial infections. The receptor is believed to help summon an immune response when it detects the bacteria, and cardiologists speculate that its responsiveness to fat may mean the receptor is also triggering inflammatory responses that contribute to heart disease. If so, blocking the receptors could offer a new path to prevention.
To accelerate the search for new treatments for infectious diseases, Hultgren has established close ties with a local biotech firm, Sequoia Sciences, and with Tom Ellenberger, Ph.D., the Raymond H. Wittcoff Professor and head of Biochemistry and Molecular Biophysics.
“Tom has started a program for high-throughput screening of small molecules with pharmaceutical potential, and Sequoia has a library of approximately 250,000 antibacterial compounds isolated from plants in collaboration with the Missouri Botanical Garden,” Hultgren explains. “As we develop assays that help us know what we’re looking for in a treatment, we’ll be using those two resources to rapidly seek out compounds that meet our criteria.”
The new center and five new faculty positions will be supported in part by funding from the school’s Departments of Medicine, Molecular Microbiology, Infectious Diseases and Cardiology as well as general medical school resources and donors.
“If we can get a synergistic effect going on in terms of the interactions between these and other disciplines, then I really feel we’re going to be able to make a significant difference in women’s health,” Hultgren says.
Posted under Compound Libraries, Drug-Like Compounds, Medicinal Chemistry, Press Releases | Comments Off
Amylin invests $10M in BioSeek
Last Updated on Wednesday, 23 May 2007 10:04 Written by admin Wednesday, 23 May 2007 10:02
BioSeek, based in Burlingame, will work with San Diego-based Amylin (NASDAQ: AMLN) on treatments for inflammatory diseases. The work will put Amylin’s proprietary drug compounds through BioSeek’s biological screening systems to seek useful drugs. BioSeek can choose two peptide compounds after screening and develop them if it wishes, paying milestones and royalties to Amylin if it does.
The two companies signed an earlier collaboration last year.
Peter Staple, BioSeek’s CEO, praised the deal as a source of money for his company, as well as a way to gain access to important compounds and research in inflammatory diseases.
Posted under Business and Investment, Compound Libraries, Drug-Like Compounds, Medicinal Chemistry, North America, Press Releases | Comments Off
New compounds promising candidates for neurodegenerative disease drug development
Last Updated on Wednesday, 16 May 2007 08:09 Written by admin Wednesday, 16 May 2007 08:09
Scientists have developed a novel strategy for tackling neurodegenerative diseases such as Huntington’s disease: encouraging an individual’s own cells to “eat” the malformed proteins that lead to the disease.
Huntington’s disease is one of a number of degenerative diseases marked by clumps of malformed protein in brain cells. Symptoms include abnormal movements, psychiatric disturbances like depression and a form of dementia. The gene responsible for the disease was discovered in 1993, leading to a better understanding of the condition and to improved predictive genetic testing, but it has yet to lead to any treatments that slow the neurodegeneration in Huntington’s patients.
Professor David Rubinsztein, a Wellcome Trust Senior Clinical Fellow at the University of Cambridge, has been studying the molecular biology underlying Huntington’s and other neurodegenerative diseases. Huntington’s occurs when a protein known as huntingtin builds up in the brain cells of patients, mainly in neurons in the basal ganglia and in the cerebral cortex. Normally, cells dispose of or recycle their waste material, including unwanted or mis-folded proteins, through a process known as autophagy, or “self-eating”.
“We have shown that stimulating autophagy in the cells , in other words, encouraging the cells to eat the malformed huntingtin proteins , can be an effective way of preventing them from building up,” says Professor Rubinsztein. “This appears to stall the onset of Huntington’s-like symptoms in fruit fly and mice, and we hope it will do the same in humans.”
Autophagy can be induced in mouse and fly models by administering the drug rapamycin, an antibiotic used as an immunosuppressant for transplant patients. However, administered over the long term, the drug has some side effects and Rubinsztein and colleagues are aiming to find safer ways of inducing autophagy long term.
Now, Professor Rubinsztein, together with Professor Stuart Schreiber’s lab at the Broad Institute of Harvard/MIT, Boston in the US, and Dr Cahir O’Kane’s group in the Department of Genetics at the University of Cambridge have found a way of identifying novel “small molecules” capable of inducing autophagy. The research is published today in the journal Nature Chemical Biology.
The screening process involves identifying small molecules that enhance or suppress the ability of rapamycin to slow the growth of yeast, though the selected molecules have no effects on yeast growth by themselves. Yeast is a single-celled organism and therefore less complex to study for initial screening purposes.
Three of the molecules that enhanced the growth-suppressing effects of rapamycin in yeast were also found to induce autophagy by themselves in mammalian cells independent of the action of rapamycin. These molecules enhanced the ability of the cells to dispose of mutant huntingtin in cell and fruit fly models and protect against its toxic effects.
“These compounds appear to be promising candidates for drug development,” says Professor Rubinsztein. “However, even if one of the candidates does prove to be successful, it will be a number of years off becoming available as a treatment. In order for such drugs to be useful candidates in humans, we will need to be able to get them into right places in the right concentrations, and with minimal toxicity. These are some of the issues we need to look at now.”
http://www.wellcome.ac.uk
Source: Medical Research News
Posted under Clinical Trials, Drug-Like Compounds, Europe, Medicinal Chemistry, Press Releases | Comments Off
Vastox Selects Preclinical Candidate In Duchenne Muscular Dystrophy Programme
Last Updated on Wednesday, 16 May 2007 08:01 Written by admin Wednesday, 16 May 2007 08:01
VASTox plc (AIM: VOX), a leading UK biotechnology company, announces that it has selected a candidate to enter into preclinical development in the Company’s Duchenne Muscular Dystrophy (“DMD”) drug discovery programme.
VASTox has a unique therapeutic approach that targets the underlying cause of this disease. Owing to a genetic defect, DMD patients lack an important protein called dystrophin, which results in severe muscle wasting and is ultimately fatal for patients. VASTox is developing a small molecule treatment that replaces the missing dystrophin by increasing levels of a functionally similar protein called utrophin.
A significant benefit of VASTox’s approach of ‘up-regulating’ utrophin is that it should be effective in treating all DMD patients and, importantly, the Company expects any drug it develops to be complementary with current palliative treatments and the variety of other scientific approaches currently aimed at discovering effective DMD therapies.
VASTox’s preclinical candidate, called VOX C1100, was selected from a series of promising compounds after it significantly reduced levels of muscle degeneration during in vivo studies. Other key secondary symptoms of DMD relating to the chronic inflammation and fibrosis of muscles also showed significant improvement in the same investigations. Higher levels of utrophin were identified in treated muscles with these data providing validation of VASTox’s unique approach for developing a treatment for DMD.
The novel candidate, VOX C1100, has advantageous chemical and pharmaceutical properties suitable for a small molecule oral drug. Furthermore, it has successfully completed preliminary safety and toxicity testing after being screened through VASTox’s zebrafish chemical genomics platform. VASTox expects to submit an Investigational New Drug (“IND”) filing for VOX C1100 by mid 2008 with the compound entering first-in-man Phase I clinical trials during the second half of 2008.
Orphan drug designation has been granted for utrophin up-regulation as a mechanism of treating DMD by the European Medicines Agency (EMEA) and this status will provide VASTox with considerable support during drug development by accelerating this process and reducing the associated costs. The Company has also built up a strong patent estate to protect the increasing value of this drug discovery programme with several patents, either granted or filed, covering all of the World’s major markets.
Orphan disease indications are rare diseases with relatively small patient populations but are commercially attractive with current marketed orphan drugs generating average annual sales in excess of $500 million. VASTox is actively pursuing commercial partnering collaborations for the Company’s increasingly valuable DMD preclinical programme.
Richard Storer, DPhil, VASTox’s Chief Scientific Officer, commented: “The selection of this candidate for development is the culmination of over two years of dedicated efforts by our research teams. It is particularly gratifying that a compound initially identified as a result of in vitro utrophin up-regulation produces the benefits observed in vivo and thereby supports our fundamental scientific approach.”
Steven Lee, PhD, CEO of VASTox added “The selection of VOX C1100 represents the achievement of a major milestone for our DMD programme and illustrates the excellent progress this programme has made over the past two years. With the progression of DMD into preclinical development, VASTox now has five programmes across a range of therapeutic areas that are either in clinical or preclinical development and indicates the strength, depth and ever increasing value of our discovery pipeline.”
About VASTox’s DMD programme
DMD is a devastating disease that affects young males for which there is currently no effective treatment. Patients rarely survive beyond the age of 25 years.
VASTox has demonstrated in vivo up-regulation (increased production) of the protein utrophin by a number of small molecules from their proprietary chemical library. This is a significant development as utrophin has been demonstrated to replace the function of dystrophin, which is missing in DMD patients. Up-regulation of utrophin is widely viewed by the scientific community as a highly promising approach for the development of an effective treatment for DMD.
About VASTox plc
VASTox is a leading UK biotechnology company that discovers and develops proprietary new drugs. The Company’s internal drug development programmes are underpinned by its advanced chemistry and drug screening (chemical genomics) technology platforms, which it also provides on a collaborative or fee-for-service basis to the pharmaceutical industry.
VASTox has a broad range of drug discovery programmes in the clinical, pre-clinical and discovery stages of development, which target serious diseases with a high unmet medical need. These therapeutic areas include neuro-disorders (neurodegenerative and neuromuscular), anti-infectives, ophthalmic diseases, oncology and regenerative medicines.
VASTox’s in-house drug development capabilities combine world-class expertise in both medicinal and carbohydrate chemistry with high-volume, high-content screening using its proprietary zebrafish and fruitfly technologies (chemical genomics). These whole organism screens have the potential to dramatically decrease the time and cost of drug discovery and development by delivering data that are highly predictive of the efficacy and toxicity of potential drug compounds in humans.
The company listed on the AIM market of the London Stock Exchange in October 2004 – symbol: VOX
Posted under Drug-Like Compounds, Europe, Medicinal Chemistry, Press Releases | Comments Off
Proprietary Formulation Technologies Advancing in Preclinical Drug Development
Last Updated on Wednesday, 2 May 2007 07:12 Written by admin Friday, 6 April 2007 04:07
New Report by Applied Data Research Analyzes the Impact on Drug Development Timelines
(Nashua, NH) – As the availability of new tools for automating the drug discovery process identifies potential drug candidates at an accelerating rate, the formulation limitations of a majority of these new NCEs is creating a bottleneck in preclinical development. Drug developers are responding by exploring drug formulation technologies – often proprietary processes offered by third parties – to negotiate their way past critical steps in the path to commercializing new chemical entities and driving the financial success of their companies.
Much of the current focus in formulation science is concerned with processes that can improve the solubility of APIs. The importance of solubilization technologies is also underscored by the capability they bestow on formulators attempting to re-formulate approved drugs approaching the end of their patent life.
Issues surrounding water insolubility of active compounds have important business and market implications for new drug development. This impact goes beyond potential future drug therapeutics, effectively limiting reformulation strategies for existing products at a time when extending the market life of proprietary drugs through derivative formulations has become a key business strategy.
Drug formulation technology companies are working with drug developers at pharmaceutical companies to help define the prescription formulations that will enter preclinical development and the clinical trial pipeline in the coming months and years. New formulation capabilities will expand the number of new NCEs that can be formulated to meet pharmacochemical thresholds.
More information is available at www.applieddata.org .
About Applied Data
Applied Data Research is a drug therapeutics consulting firm focused on medical market strategies, product commercialization, venture development, and market research. We assist medical market participants in achieving their business objectives through the creation of detailed business development strategies, product commercialization programs, and comprehensive market and technology research and analysis.
Contact:
Greg Stone
Voice: 603-595-6225
Fax: 603-804-0466
www.applieddata.org
Source: Applied Data Research
Posted under Compound Libraries, Drug-Like Compounds, North America, Press Releases, Reports | Comments Off
4SC AG has Received Clinical Trial Approval by Authorities and has Started the Clinical Phase IIa Study
Last Updated on Wednesday, 6 December 2006 09:28 Written by admin Wednesday, 6 December 2006 09:28
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.
Posted under ChemInformatics, Drug-Like Compounds, Europe, Press Releases | Comments Off
NCE Discovery and DARA BioSciences Join Forces to Develop New Therapies
Last Updated on Wednesday, 6 December 2006 09:23 Written by admin Wednesday, 6 December 2006 09:23
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
Posted under ChemInformatics, Collaborations, Drug-Like Compounds, Europe, Medicinal Chemistry, Press Releases, Targeted Libraries | Comments Off
Halozyme and Roche Enter Agreement for the Application of Enhanze, A Novel Technology to Improve Drug Delivery
Last Updated on Wednesday, 6 December 2006 09:21 Written by admin Wednesday, 6 December 2006 09:21
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.
Posted under Drug-Like Compounds, Europe, Medicinal Chemistry, North America, Press Releases, Targeted Libraries | Comments Off
Multiple Myeloma Research Foundation (MMRF) Awards $1 Million Each in Funding to ProChon Biotech and Semafore Pharmaceuticals to Advance Drug Development
Last Updated on Wednesday, 6 December 2006 09:12 Written by admin Wednesday, 6 December 2006 09:12
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/.
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Wyeth acquires global license for Inpharmatica’s Admensa Interactiveâ„¢
Last Updated on Wednesday, 6 December 2006 09:02 Written by admin Wednesday, 6 December 2006 09:02
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
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EpiCept Announces IND Filing of Novel Compound with Potent Apoptotic and Tumor Selective Vascular Disruptive Activity for Treatment of Cancer
Last Updated on Thursday, 5 October 2006 02:20 Written by admin Thursday, 5 October 2006 02:20
NGLEWOOD CLIFFS, New Jersey, October 2 /PRNewswire/ – – EPC2407 Latest Clinical Candidate from Company’s Apoptosis ScreeningTechnology EpiCept Corporation (Nasdaq: EPCT; OMX Stockholm) today announced that ithas submitted an investigational new drug (IND) application to the U.S. Foodand Drug Administration (FDA) to begin Phase I clinical studies of EPC2407 incancer patients. EPC2407 is the Company’s novel small molecule which inducesapoptosis (cell death) and disruption of tumor blood flow. EPC2407 isintended for the treatment of advanced cancer patients with solid tumors thatare well vascularized. These tumors include the frequently occurring cancersof the lung, ovaries, and breast. These cancers still have a high mortalityrate despite progress in earlier stages of these diseases. (Logo: http://www.newscom.com/cgi-bin/prnh/20020513/NYM112LOGO ) EPC2407 is the first of a new class of microtubulin inhibitors whichcause cell cycle arrest, caspase activation and apoptotic death in cancercells. The compound has demonstrated in pre-clinical studies potentanti-tumor activity against a number of tumor types and is synergistic withcisplatin. EPC2407 also disrupts the vasculature of tumor blood vesselsleading to hypoxia and tumor necrosis. This has been shown to occur inpre-clinical studies in tumored animals at subtoxic concentrations. Theobjectives of this first clinical trial of EPC2407 is to determine themaximum tolerated dose, to characterize the blood levels and biologicaleffects of the drug and to identify any anti-tumor response as measured by CTscans, MRI or PET scans. The study is expected to enroll approximately 30-40patients. One of the investigators for this study is Dr. Daniel von Hoff from theCenter for Translational Drug Development, TGen, the Scottsdale HealthcareClinical Research Institute and the Arizona Cancer Center. Dr. von Hoffcommented, “We are pleased to work with EpiCept Corporation to test thispotential new anti-cancer compound in patients with advanced cancers. Resultsfrom pre-clinical testing of EPC2407 are encouraging, and mechanism studiessuggest two ways that this new agent may add to our treatment options for arange of cancers.”“The filing of an IND for EPC2407 represents an important milestone forour company,” stated Jack Talley, President and Chief Executive Officer. “Webelieve this filing deepens our already promising clinical pipeline of painand cancer treatment candidates and further demonstrates the potential of ourproprietary apoptosis screening technology which led to the discovery anddevelopment of EPC2407. This compound represents the second clinical cancercandidate discovered by EpiCept researchers utilizing this technology. Wehave identified several other promising compounds with the potential forfurther development which we intend to selectively pursue. Our goal is toprogress these product candidates into clinical development and seek partnersprior to the commencement of pivotal scale trials.” About EPC2407 The IND filing for EPC2407 is based on the compound’s effectiveness inseveral pre-clinical animal models of cancer and its potent anti-tumoreffects both in vitro and in vivo. Nanomolar concentrations of the moleculehave been shown to induce tumor cell apoptosis and to selectively inhibitgrowth of proliferating cell lines, including multi-drug resistant celllines. Murine models of human tumor xenografts demonstrated that EPC2407inhibits growth of established tumors of a number of different cancer types.The safety profile of the compound in standard toxicology studies alsosupports its testing in human clinical trials. Pre-clinical studies suggest that the anti-tumor effects of EPC2407 maybe the result of a dual mechanism, a direct effect of tumor apoptosis and asecond effect on disruption of tumor vascular endothelial cells leading tohypoxia and central tumor necrosis, as observed with vascular disruptionagents. About EpiCept’s Apoptosis Screening Technology Cancer cells often exhibit unchecked growth caused by the disabled orabsent natural process of programmed cell death called apoptosis. Apoptosisis a normal process of triggering destruction of cells from within when theyhave outlived their purpose or may be seriously damaged, but cancer cellsgrow out of control when the normal apoptosis process is not functioning. Apromising approach in the fight against cancer is selective induction of orrestoration of apoptosis, thereby checking, and perhaps reversing, theimproper cell growth. EpiCept’s proprietary apoptosis screening technology can efficientlyidentify new cancer drug candidates and molecular targets that selectivelyinduce apoptosis in cancer cells through the use of chemical genetics and itsproprietary live cell high-throughput caspase-3 screening technology.Chemical genetics is a research approach investigating the effect of smallmolecule drug candidates based on the cellular activity of a protein,enabling researchers to determine the protein’s function. With thecombination of chemical genetics and caspase-3 screening, EpiCept’sresearchers identify and test the effect of small molecules on pathways andmolecular targets crucial to apoptosis and gain insights into their potentialas new anticancer agents. The Company’s screening technology is particularlyversatile and can be adapted for many cell types that can be cultured, and itcan measure caspase activation inside multiple cell types (e.g. cancer cells,immune cells, or cell lines from different organ systems or geneticallyengineered cells). This allows researchers to find potential drug candidatesthat are selective for specific cancer types, which may help identifycandidates that provide increased therapeutic benefit and reduced toxicity. EpiCept’s drug discovery and pre-clinical development groups include highthroughput screening (HTS) and informatics, cell biology, medicinalchemistry, and in vivo pharmacology. The HTS group identifies the hits whichupon passing certain criteria are analoged by the chemistry group forsecondary and tertiary assay testing by the cell biology group. Promisingleads are tested in animal models for toxicity, efficacy andpharmacokinetics. An iterative interaction between the various groupsprovides for the rapid advancement from hit compounds to lead candidatessuitable for further development. About EpiCept Corporation EpiCept is an emerging specialty pharmaceutical company focused on unmetneeds in the treatment of pain and cancer. The Company has a staged portfolioof product candidates with several pain therapies in late-stage clinicaltrials, and a lead oncology compound (for acute myeloid leukemia, AML) withdemonstrated efficacy in a Phase III trial; a marketing authorizationapplication for this compound will be submitted in Europe in the near future.EpiCept is based in New Jersey, and the Company’s research and developmentteam in San Diego is pursuing a drug discovery program focused on novelapproaches to apoptosis. Forward-Looking Statements This news release contains certain forward-looking statements thatinvolve risks and uncertainties that could cause actual results to bematerially different from historical results or from any future resultsexpressed or implied by such forward-looking statements. Such forward-lookingstatements include statements regarding the efficacy, safety, and intendedutilization of the Company’s product candidates, the conduct and results offuture clinical trials, the sufficiency of the Company’s existing capitalresources, plans regarding regulatory filings, future research and clinicaltrials and plans regarding partnering activities. Factors that may causeactual results to differ materially include the risk that product candidatesthat appeared promising in early research and clinical trials do notdemonstrate safety and/or efficacy in larger-scale or later stage clinicaltrials, the risk that the Company will not obtain approval to market itsproduct candidates, the risks associated with reliance on outside financingto meet capital requirements, and the risks associated with reliance oncollaborative partners for further clinical trials, development andcommercialization of product candidates. You are urged to consider statementsthat include the words “may,”"will,”"would,”"could,”"should,”"believes,”"estimates,”"projects,”"potential,”"expects,”"plans,”"anticipates,”"intends,”"continues,”"forecast,”"designed,”"goal,” or the negative ofthose words or other comparable words to be uncertain and forward-looking.These factors and others are more fully discussed in the Company’s periodicreports and other filings with the SEC. EPCT-GEN Web site: http://www.epicept.comEpiCept CorporationRobert W. Cook, EpiCept Corporation, +1-201-894-8980, rcook@epicept.com; or Francesca T. DeVellis, Feinstein Kean Healthcare, +1-617-577-8110, francesca.devellis@fkhealth.com /Photo: http://www.newscom.com/cgi-bin/prnh/20020513/NYM112LOGO
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Evotec Discontinues EVT 301 Development Programme
Last Updated on Thursday, 14 September 2006 03:55 Written by admin Thursday, 14 September 2006 03:55
HAMBURG, Germany and OXFORD, England, September 13 /PRNewswire-FirstCall/ — Evotec AG (Frankfurt Stock Exchange: EVT, TecDAX 30) today reported that during the one month safety and tolerability study with EVT 301 in young and elderly volunteers, several cases of asymptomatic elevated liver function tests in the elderly group have been observed. All cases reversed spontaneously. No cases of elevated liver function tests were observed within the young healthy volunteer group.
In the light of these findings Evotec has stopped the ongoing Phase I trials and has decided today to discontinue the development programme. As the planned Phase II trial with EVT 301 will not be executed this will free approximately EUR 20 million of R&D money over the next two to three years for other development programmes.
“Our strategy is to develop high-quality compounds to later stage development with the goal of monetising these assets for partnering. Successful drug development requires discipline. Although advancement of this programme would have been optimal, it is better that the investment in EVT 301 has been capped now rather than after a large investment in later stage trials. We continue to believe there is ample opportunity in our current proprietary portfolio of CNS candidates, including our insomnia drug EVT 201 and the potential of EVT 101 for the treatment of Alzheimer’s disease, neuropathic pain or other indications. The discontinuation of the EVT 301 programme will free up EUR 20 million, which will provide us a lot of flexibility in developing our pipeline,” said Joern Aldag, President & Chief Executive Officer of Evotec.
“Alzheimer’s disease is a large unmet medical need and Evotec continues to believe in the potential of MAO-B inhibition and its role in treating CNS related disorders. We will assess the findings of EVT 301 in full detail. In other respects, our pipeline is progressing well. EVT 201 and EVT 101 continue to meet their clinical milestones and we look forward to apprising you of their developments later this year,” added John Kemp, Chief Research & Development Officer of Evotec.
EVT 301 is an orally active, selective and reversible inhibitor of monoamine oxidase B (MAO-B) which was in development for Alzheimer’s disease.
About Evotec AG
Evotec is a leader in the discovery and development of novel small molecule drugs. Both through its own discovery programmes and through contract research partnerships, the Company is generating the highest quality research results to its partners in the pharmaceutical and biotechnology industries.
In proprietary projects, Evotec specialises in finding new treatments for diseases of the Central Nervous System. Evotec has two programmes in clinical development: EVT 201, a partial positive allosteric modulator (pPAM) of the GABAA receptor complex for the treatment of insomnia, and EVT 101, a subtype selective NMDA receptor antagonist for the treatment of Alzheimer’s disease and/or neuropathic pain.
In contract research, Evotec has established itself as the partner of choice for pharmaceutical and biotechnology companies worldwide. The Company provides innovative and often integrated solutions from drug target to clinic through an unmatched range of capabilities, including early stage assay development and screening through to medicinal chemistry and drug manufacturing.
In 2005, Evotec has generated sales of EUR 80 million with 600 employees located in Hamburg, Germany and near Oxford and in Glasgow, UK.
www.evotec.com Contact: Evotec AG Anne Hennecke Director, Investor Relations & Corporate Communications Phone: +49-40-56081-286 Fax: +49-40-56081-333 E-Mail: anne.hennecke@evotec.com
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Virtual screening services collaboration between Quantum Pharma and TimTec
Last Updated on Wednesday, 6 September 2006 04:58 Written by admin Wednesday, 6 September 2006 04:57
Quantum Pharma, a drug discovery and computational chemistry software and contract services provider, Moscow, Russia, and TimTec, a provider of synthetic organic and natural compounds for bioscreening, Delaware, US, singed up a collaboration agreement. Quantum computational chemistry software with unique capabilities is available now through TimTec. In the future companies will co-develop products for drug-discovery utilizing Quantum Pharma computational capabilities and TimTec in-stock and virtual screening compound resources, and expertise in comprising compound library collections.
Maxim Kholin, Business Development Director at Quantum Pharmaceuticals comments on the collaboration: “We are glad to work with TimTec, the company that has strong expertise and recognized reputation on the market. Our technological breakthrough in software development has huge market potential. Now our main goal is to bring this new generation technology to the market. All our potential customers know very well the limitations of existing approaches and software. We know that once researchers evaluate Quantum software they will enjoy accuracy and benefits of our capable applications. I believe together with TimTec we will introduce better computational tools on the market of drug discovery and computational chemistry software and services.â€
QUANTUM SOFTWARE MODULES
HIT IDENTIFICATION
1. IC50 protein-ligand complex Calculates the free binding energy and thus predicts the IC50 of a given protein-ligand complex.
2. Docking Finds the position of a small molecule in the active site of a given protein with the minimum value of the free binding energy and predicts the IC50 of the ligand.
3. Screening Screens in-silico a library of small-molecules. Finds their positions in the active site with the minimum value of the free binding energy and predicts the IC50 values of these molecules).
4. Scaffold Based Drug Design Designs a De Novo ligand – a potential drug candidate – which will interact specifically with a selected molecular target on the basis of scaffold library.
ADMET
Lead Selectivity Detects broad relative selectivity, potential adverse activity and additional unexpected activity for a library of compounds by screening them against several thousands of proteins.
PROTEOMICS
1. Protein Dynamics does geometry optimization, performs calculations to find stable (local energy minimum) configurations of a protein. Software analyses large-scale protein movements; provides normal mode analysis of proteins and builds their large-scale amplitude movements helping to evaluate the degree of protein flexibility in modeling their conformational changes.
Mutagenesis provides an interface for changing the protein sequence at specific sites through alterations to its amino acids. It is useful tool for activity prediction and the research of mutated proteins with other modules of Quantum.
Superimpose identifies the best fit for two molecules.
2. IC50 Protein-Protein Complex calculates free binding energy and predicts the IC50 of a given protein-protein complex.
COMPUTATIONAL CHEMISTRY
1. Solubility and LogP Prediction calculates the solvation energy and solubility for a library of molecules in a number of solvents (water and DMSO); Predicts LogP.
2. pKa (protonation state) Prediction analyzes a molecule, finds protonation states, calculates pKa values for various protonation reactions and identifies the proper protonation state for a given pH.
Please contact TimTec to request product information:
Kay Denis, Business Development
TimTec
http://ww.timtec.net
Suite A, 301 Ruthar Dr
Newark DE 19711
Tel 302 292 8500 x 206
Fax 302 292 8520
info@timtec.net
About Quantum Pharmaceuticals
Quantum Pharmaceuticals is a drug discovery and computational chemistry software and contract services provider. The areas of technology application are virtual screening, hit/lead identification and optimization, ADMET prediction, computational chemistry and biology, bioinformatics. The Quantum software was developed using a new paradigm in molecular modeling – applying quantum and molecular physics instead of statistical scoring-function-like and QSAR-like methods. The proprietary technology includes the latest achievements in the fields of chemistry, physics and mathematics. It demonstrates outstanding speed and accuracy of affinity and other calculations due to fast quantum calculations, which take into account full flexibility of molecules, solvation effects, and entropy contribution.
About Timtec LLC
Timtec LLC is a privately held company located in Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. Timtec has established a global network of thousands of scientists from many research centers around the world. The company has developed strong in-house expertise assembling general, targeted, and custom library collections for variety of research applications. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use Timtec products for research and development programs.
Posted under ChemInformatics, Collaborations, Compound Libraries, Drug-Like Compounds, Europe, Medicinal Chemistry, North America, Press Releases | Comments Off
BrainCells In-Licenses Clinical-Stage CNS Compound From Mitsubishi Pharma
Last Updated on Friday, 11 August 2006 02:07 Written by admin Friday, 11 August 2006 02:07
SAN DIEGO, Aug. 10 /PRNewswire/ — BrainCells Inc. (BCI) today announced it has in-licensed a clinical-stage compound from Mitsubishi Pharma Corp. (MPC) that BCI will reposition and develop for the treatment of central nervous system (CNS) diseases, including mood disorders.
MPC extensively developed the compound for another CNS indication, then suspended the program when the drug met safety expectations but did not reach the defined efficacy endpoints. BCI applied its proprietary technology in the area of neurogenesis — the process by which endogenous stem cells in the adult human brain produce new brain tissue, including neurons — to identify different indications for the drug. The company expects to begin development and initiate additional Phase 2 clinical trials of the compound, BCI-540, next year.
“This is indicative of the extensive opportunity that exists for us in the CNS drug development space,” said James A. Schoeneck, BCI’s CEO. “We can screen compounds efficiently for neurogenic properties and pursue the development of these compounds for indications that weren’t part of a licensor’s original plans. The license from MPC provides us with the ability to capitalize on the predictive power of our screening platform, enabling us to develop a novel product for CNS disorders that affect millions of patients.”
“BCI has a unique approach to the identification and development of drugs that can be repositioned for a variety of CNS diseases,” said Akihiro Tobe, managing executive officer of MPC. “We believe that BCI has the right mix of cutting-edge science and development expertise to maximize the opportunity for the compound.”
About Mitsubishi Pharma Corp.
Mitsubishi Pharma Corporation (MPC), a research-driven pharmaceutical company, is the core member in the Mitsubishi Chemical Holdings group, under which Mitsubishi Chemical, a leading chemical company in Japan, and MPC exist as wholly-owned subsidiaries. Formed in 2001 by the merger of Mitsubishi-Tokyo Pharmaceuticals & Welfide Corporation (formerly Yoshitomi), MPC is committed to scientific progress, pharmaceutical advancement and the creation of products that benefit worldwide people’s welfare. Its core therapeutic areas are psychiatric and central nervous system diseases, cardiovascular and metabolic diseases, immunological and respiratory diseases and hepatic diseases. More information about the company can be found by visiting http://www.m-pharma.co.jp/.
About BrainCells Inc.
BrainCells Inc. (BCI) is a San Diego-based drug discovery and development company that is applying proprietary neurogenesis-based technology to identify and reposition compounds for the treatment of central nervous system (CNS) diseases. With its predictive screening platform, BCI can direct the selection and development of neurogenic compounds, increasing the opportunity for successful clinical trials in a variety of CNS indications. For more information, visit http://www.braincellsinc.com.
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Chinese chemists synthesize compounds for BASF’s crop protection discovery research
Last Updated on Friday, 11 August 2006 01:30 Written by admin Friday, 11 August 2006 01:30
10 Aug 2006 : Cooperation with partners throughout the world is an important aspect of the research strategy of BASF. The company spends nearly €100 million a year on a current total of 1,300 cooperations. One of them, a cooperative arrangement that has been in place for more than a year with Chinese company WuXi Pharmatech in Shanghai, has proven so fruitful that the number of chemists working there for BASF has now been increased to more than 20. The Agricultural Products division of BASF engages its Chinese partner to synthesize chemical compounds that are needed in the wide-ranging search for new active ingredients. The subsequent modification of the new substances and their screening for biological effectiveness are then conducted in the central research units at Ludwigshafen and Limburgerhof.
â€Purchasing new substances for primary screening and building blocks for synthesis from external partners on the one hand and focusing our internal efforts on developing promising compounds for crop protection active ingredients on the other hand is successful and has stood the test of time,“ says Dr. Peter Eckes, Senior Vice President Agricultural Products Research and Development. “We work with 10 external partners – some of them for several years already – who synthesize new compounds for us.“ Global crop-protection research is the first unit of BASF to work together with a Chinese company in an extensive synthesis cooperation.
The development of innovative products and processes – including new crop protection active ingredients – is indispensable for the profitable growth of BASF. Before identifying an agent that promises to be successful, many thousands of chemical compounds must be run through the numerous optimization cycles each year in the Agricultural Products division. If a new class of substances shows an interesting effect against harmful fungi, insects or weeds, its chemical structure is systematically modified. Then it is run once again through the cycle of chemical synthesis, screening and evaluation of results. An optimized lead structure emerges at the end of this process.
“Cooperation with external partners makes a valuable contribution to the efficient organization of our research processes,“ said Dr. Alfred Hackenberger, President Specialty Chemicals Research. “We enhance flexibility and can thus achieve even more with our research budget, for example by screening more substances in a shorter period of time. That is an important success factor because only a few of those substances turn out to be successful crop-protection active ingredients.â€
All external partners are extensively assessed to make sure that no know-how leaks out and that no potentially new active ingredients are jeopardized. Success factors in cooperation are unconditional reliability and open communication. In addition, product quality and synthetic competence are evaluated because BASF must be able to depend on its partners to do as much as it itself would when trying to solve tricky problems.
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Giving worms a taste of their own medicine
Last Updated on Friday, 21 July 2006 06:41 Written by admin Friday, 21 July 2006 06:41
The humble nematode worm could prove invaluable in screening new compounds for active drugs, new research published today suggests.
Soil-dwelling nematodes have a programmed avoidance response to harmful chemicals, which they detect through nerves exposed to their environment. Scientists led by the Wellcome Trust Sanger Institute have genetically modified the worm C. elegans to make human proteins called receptors in these nerves: the modified worms detect and avoid human signalling molecules and drug candidates.
The exciting results, reported today, 20 July 2006, in the open-access journal BMC Biology, promise a simple assay that can be used to screen thousands of compounds for activity against human proteins – a foundation of drug development.
“The worm is a great tool to understand biology,” said Dr Michelle Teng of the Wellcome Trust Sanger Institute, a lead author on the report. “Because we understand it so well it has a simple well studied nervous system the role for each nerve has been mapped in detail. We also have a good understanding of the signalling mechanisms in nerves that drive the responses.”
“We showed that the biochemical response of the receptors emulated that seen in humans. It is just that, in the worm, the effects of that response are to make them crawl away from the chemical stimulus. This simple response could be used to test many unknown drug candidates.”
Medicines often interact with receptors, which are ‘sensors’ at the surface of cells. The team introduced the somatostatin receptor (Sstr2) and the chemokine receptor 5 (CCR5) in the nerves that respond to environmental cues. Somatostatin is a hormone that mediates a wide range of activities in humans and chemokines play an important role in the immune system. The CCR5 receptor used is also the gateway that HIV/AIDS virus uses to enter cells. Both receptors belong to a receptor family called GPCRs, which represent up to 50% of current drug targets.
The response was specific. In tests, worms responded by avoiding somatostatin or chemokine placed in their paths only when the appropriate receptor was made in the appropriate nerves.
“We have shown that we can hijack the cellular machinery of the worm so that the human receptor proteins drive the avoidance response,” explained Dr John McCafferty, Principal Investigator at the Wellcome Trust Sanger Institute and senior author. “We chose two receptors with widely differing functions in humans. The responses were specific to the compounds we added and could be inhibited in the same way a response in humans could be inhibited.”
The worms could also be desensitized by pre-exposure to somatostatin or chemokine: desensitization is an important part of normal human response, because it ensures that our receptors can recover for a fresh round of stimulus. This is the first time that activation has been programmed in these nerves and the team have shown that the human receptors integrate into the worm signalling machinery.
“Systems exist already to study the response of cells in test-tubes to added compounds,” continued Dr McCafferty. “However, because these are soil-dwelling worms which feed on bacteria, we could test crude samples for drug candidates.”
Together, these results make us very optimistic that these models will be widely applicable and that development of a high-throughput system is feasible.
The team used a rapid sorting system to isolate the genetically modified worms. Although for this study, worm responses were scored under the microscope, automation could be integrated to achieve a higher rate of testing.
The worm model can also help to define which regions of a novel compound are important for its biological effect, which can be crucial for producing effective drugs. The team were able to use the worm assay to identify four important building blocks within somatostatin which are known to be necessary for its effect.
“These results show the power of simple organisms such as the worm to help us not only in our understanding of biology but also in the search for new ways to improve healthcare,” said Professor Ronald Plasterk, Professor of Developmental Genetics at the University of Utrecht and Director of the Hubrecht Laboratory, in the Netherlands. “It is a nice irony of history that the worm was chosen for biomedical research by Sydney Brenner forty years ago in Cambridge, only a few miles from the Sanger Institute. Then twenty years ago John Sulston started to make a gene map of the animal, and eventually read its sequence as the first of all animal genomes.”
“And now a new generation of researchers again in the Cambridge area uses it to test candidate drugs that are immediately relevant to human health.”
Posted under Discoveries, Innovations and Patents, Drug-Like Compounds, Europe, Press Releases, Research Projects | Comments Off
GeneGo and Elsevier MDL Collaborate to Provide Seamless Access to Compound Databases, Patents, Literature and Pathways
Last Updated on Friday, 21 July 2006 06:36 Written by admin Friday, 21 July 2006 06:36
ST. JOSEPH, Mich., July 20 /PRNewswire/ — GeneGo, Inc., a leading provider of software and databases for systems biology and pathway analysis and Elsevier MDL, a leading provider of scientific content, informatics framework and workflow applications for pharmaceutical research, announced the collaboration. The latest version of GeneGo’s data mining platform MetaCore 4.0 will be seamlessly integrated with the MDL(R) suite of databases via the DiscoveryGate(R) content platform. Researchers will be able to identify drug targets and bioactive compounds via pathway analysis and retrieve comprehensive information on their synthesis, biological effects, commercial availability and relevant literature within one application.
“The integration of MDL databases with GeneGo’s pathways information systems enables scientists to bridge the gap between cell biology and organic chemistry,” comments Steve Young, Director of MDL Content Strategy. “For the first time, biologists will be able to quickly review cheminformatics data of small molecules involved in biological pathways and chemists will be able to view molecular pathway information related to their lead compounds.”
“Lately, a number of customers approached us with requests for functional analysis of the effects of drug-like compounds rather than genomic data,” says Julie Bryant, VP Business development at GeneGo. “Although pathways and network analysis of bioactive compounds is a common practice in MetaCore, we partnered with Elsevier MDL for in depth coverage of literature and patent-derived information relevant for compounds. We are very pleased to be working with Elsevier MDL, the market leader in medicinal chemistry knowledge databases, Integration with the Elsevier MDL chemistry space opens up new applications for our products in medicinal chemistry, including high-throughput and high-content screening, hit selection and validation, lead development programs and chemogenomics.”
About GeneGo
GeneGo develops systems biology technology for life science research. The original computational platform allows an integration and expert analysis of different kinds of experimental data (mRNA expression, proteomics, metabolomics, siRNA and other phenotypic data) and relevant bioactive chemistry (metabolites, drugs, other xenobiotics) within the framework of curated biological pathways and networks. GeneGo’s flagship product, MetaCore 4.0, assists pharmaceutical scientists in the areas of target selection and validation, identification of biomarkers for disease states and toxicology. The second product, MetaDrug(TM) is designed for prediction of human metabolism, toxicity and biological effects for novel small molecules compounds. MetaBase(TM) represents the knowledge base for MetaCore. For more information, please visit the company’s web site at www.genego.com.
MetaCore(TM), MetaBase(TM) and MetaDrug(TM) are trademarks of GeneGo, Inc.
About Elsevier MDL
Elsevier MDL provides informatics, database and workflow solutions that accelerate successful life sciences R&D by improving the speed and quality of scientists’ decision making. Researchers around the world depend on Elsevier MDL for innovative and reliable discovery informatics software solutions and services augmented by 400 Elsevier chemistry and life sciences journals and related products. For more information, visit www.mdl.com. Elsevier is a world-leading publisher of scientific, technical and medical information products and services. For more information, visit www.elsevier.com. Elsevier is part of Reed Elsevier Group plc, a world-leading publisher and information provider. Reed Elsevier’s ticker symbols are REN (Euronext Amsterdam), REL (London Stock Exchange), RUK and ENL (New York Stock Exchange). For more information visit www.elsevier.com.
MDL and DiscoveryGate are registered trademarks of MDL Information Systems, Inc. (‘Elsevier MDL’) in the United States and/or other countries. Beilstein Database: Copyright (C) 1988-2006, Beilstein-Institut zur Forderung der Chemischen Wissenschaften licensed to Beilstein GmbH and MDL Information Systems GmbH. All rights reserved.
Source: GeneGo, Inc.
CONTACT: Julie Bryant, VP Business Development and Marketing of GeneGo,
Inc., +1-858-756-7996, julie@genego.com; or Jean Holt, Director, Corporate
Communications of Elsevier MDL, +1-925-543-5400, j.holt@mdl.com
Web site: http://www.mdl.com/
Web site: http://www.elsevier.com/
Web site: http://www.genego.com/
Posted under ChemInformatics, Drug-Like Compounds, North America, Press Releases | Comments Off
Evotec and Roche Form Global Alliance to Jointly Discover Novel Drugs
Last Updated on Monday, 3 July 2006 08:51 Written by admin Monday, 3 July 2006 08:51
Today announced that they have formed an alliance to jointly discover and develop compounds against a target for CNS diseases and other indications.
HAMBURG, Germany | OXFORD, UK| BASEL, Switzerland | Jun 21, 2006 | Roche and Evotec AG (Frankfurt Stock Exchange: EVT,
| TecDAX 30; Evotec) today announced that they have formed an alliance to jointly discover and develop compounds against a target for CNS diseases and other indications.
Leveraging the expertise developed by Evotec on this target, and as part of their CNS drug discovery focus, Evotec and Roche will collaborate to identify inhibitors involved in the potential treatment of a range of diseases. Both companies believe that this target is of high priority and that partnering their respective drug discovery efforts and expertise will bring about the successful and timely discovery of new drugs. Dr John Kemp, Executive Vice President Research & Development at Evotec, said: “This collaboration capitalises on Evotec’s and Roche’s complementary drug discovery capabilities and underlines the value of our drug discovery platform and CNS expertise. We are delighted to join forces with Roche, one of the world’s premier pharmaceutical companies, to discover novel drug candidates that will enrich our companies’ pipelines. We have been working with Roche for many years in an atmosphere of mutual respect – in service agreements and in-licensing of CNS drugs – and are looking forward to now partnering one of our CNS discovery projects into this joint effort.†“This agreement builds on the strategic alliance that Roche and Evotec have established over the last five years“, said Dr Peter Hug, Global Head of Pharma Partnering at Roche. “Through the multiple dimensions of the Roche-Evotec relationship we are endeavoring to develop compounds that will make a difference in patients lives.†Roche and Evotec will jointly progress projects up to clinical development, at which stage Roche will have exclusive rights to the development of the drug candidates. In return, Evotec will be eligible to receive milestone payments that could exceed 100 million Euros in total, plus royalties on the sale of any products. If Roche does not exercise these opt-in rights, Evotec will have the right to opt-in, making adjusted payments to Roche. About Evotec AG About Roche About Roche as a Partner Statements included in this press release which are not historical in nature are intended to be, and are hereby identified as, “forward-looking statements†for purposes of the safe harbour provided by Section 21E of the Securities Exchange Act of 1934, as amended by the Private Securities Litigation Reform Act of 1995. Forward-looking statements may be identified by words including “anticipatesâ€, “believesâ€, “intendsâ€, “estimatesâ€, “expects†and similar expressions. The company cautions readers that forward-looking statements, including without limitation those relating to the company’s future operations and business prospects, are subject to certain risks and uncertainties that could cause actual results to differ materially from those indicated in the forward-looking statements. Factors that may affect future operations and business prospects include, but are not limited to, clinical and scientific results and developments concerning corporate collaborations and the company’s proprietary rights and other factors described in the prospectus relating to the company’s recent public offering. SOURCE: Roche and Evotec AG |
Posted under Collaborations, Drug-Like Compounds, Europe, Press Releases | Comments Off
Ingenium and ASINEX Announce Successful Lead Optimization Program
Last Updated on Wednesday, 7 June 2006 06:04 Written by admin Wednesday, 7 June 2006 06:04
MUNICH and MOSCOW, June 6 /PRNewswire/ — Ingenium Pharmaceuticals AG, a drug discovery and development company, and ASINEX Ltd., a leading provider of lead generation and chemical optimization services, announced today a successful lead optimization project resulting in the generation of novel active compounds, which will expand Ingenium’s current proprietary pipeline of potential treatments for pain and inflammatory diseases. Due to the success of this completed project, the two companies will continue the collaboration throughout 2006.
Commenting on the agreement, Dr. Klaus Dembowsky, Ingenium’s Vice President of Drug Discovery, said, “As Ingenium continues to advance its drug discovery and development programs through preclinical pharmacological evaluation, effective lead optimization is critical. ASINEX has performed rapidly and efficiently to meet our needs and we have filed key patents based on these novel compounds.”
“We are looking forward to continuing our collaboration with Ingenium. After starting on a small scale, our relationship has grown over the last few months. We have successfully completed challenging tasks for Ingenium, and we are delighted that our work has made a positive impact on the company’s pipeline,” said Dr. Andrea Altieri, ASINEX’s Head of Project Management.
Posted under Drug-Like Compounds, HT Screening, Press Releases | Comments Off
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