Archive for the ‘Industry News’ Category
Actelion obtains option to acquire privately-held Trophos
Last Updated on Thursday, 5 August 2010 02:04 Written by Editor Thursday, 5 August 2010 02:04
Late-stage Phase III compound in Amyotrophic Lateral Sclerosis to report data in late 2011 – Novel therapeutic approach to be further explored in drug discovery collaboration
ALLSCHWIL, SWITZERLAND and MARSEILLE, FRANCE – 20 July 2010 – Actelion Ltd (SIX: ATLN) and privately-held Trophos SA announced today that they have entered into a binding agreement whereby Actelion has, for EUR 10 million, obtained an exclusive option to acquire privately-held Trophos SA, a clinical stage pharmaceutical company.
Trophos’ lead compound olesoxime has completed enrollment into a Phase III study in Amyotrophic Lateral Sclerosis (ALS), an orphan disease also known as Lou Gehrig’s disease. This study is expected to report data by the end of 2011; at this time Actelion may exercise the option for an acquisition price between EUR 125 and 195 million in cash, contingent on different regulatory approvals and other clinical progress of Trophos’ pipeline.
Simon Buckingham, President, Global Corporate and Business Development: “Trophos has done an excellent job to enroll more than 500 ALS patients into a well-designed pivotal study. Once study results are available, Actelion is ideally positioned to leverage these achievements with our proven global regulatory and marketing expertise in the area of orphan drugs.”
Trophos is a clinical stage company with a pipeline of new molecular entities in development for the motor neuron diseases ALS and spinal muscular atrophy (SMA) as well as a novel compound for cardiac ischemia-reperfusion injury.
Damian Marron, Chief Executive Officer at Trophos commented: “Since its inception, Trophos has made significant progress in turning its key expertise in neurodegenerative disorders and orphan diseases into achievements that include advancing our lead compound olesoxime into late stage clinical development. The development of olesoxime has benefited from significant support from patient communities, clinical investigators and the European Union (EU), including Trophos spearheading an EU-funded consortium dedicated to improving the treatment of ALS.”
Damian Marron continued: “We are delighted with the option agreement with Actelion, which will bring additional expertise and competencies to enable Trophos’ compound to rapidly reach patients following a successful study outcome.”
Damian Marron concluded: “I am also pleased with the option agreement as it provides the Trophos’ investors an opportunity to realize the value of their investments.”
The two companies also agreed on a research collaboration to allow Actelion access to Trophos’ proprietary CNS assay technology and compound library. The technology mimics neuronal degeneration processes in the test tube and is used to screen chemical compounds for their ability to block these processes.
Martine Clozel, MD and Chief Scientific Officer at Actelion commented: “Trophos has a pioneering approach and proprietary expertise that has enabled the development of high throughput screens using primary neurons as well as the ability to broadly profile more advanced compounds. This is of great value to Actelion as we have developed a large inhouse compound library and significant expertise in the field of neurological disorders.”
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Notes to Editor
About the agreement
On July 19, 2010, Actelion signed an acquisition agreement to purchase Trophos SA, a French clinical stage pharmaceutical company developing drugs for patients with neurodegenerative diseases. The acquisition is contingent on the exercise of an option, whereas Actelion has the right to terminate the agreement at any time during the option period. The option will become effective upon payment of EUR 10 million by Actelion and end two months after Actelion’s receipt of the results of an ongoing Phase III study with olesoxime but not later than December 31, 2012. The purchase consideration will be paid in cash and is partially contingent on market approval of olesoxime by the US Food and Drug Administration (FDA) as well as overall pipeline progression of other compounds. Consequently, the purchase price might vary between EUR 125 million and 195 million.
About Olesoxime
Olesoxime is Trophos’ lead compound of a proprietary mitochondrial pore modulator series. Preclinical studies have demonstrated that olesoxime promotes the function and survival of neurons and other cell types under disease-relevant stress conditions, through interactions with the mitochondrial permeability transition pore (mPTP). Olesoxime has been shown to be active in the SOD1 model of ALS (Bordet et al., JPET 322:709-720, 2007).
Phase I studies in healthy volunteers and Phase Ib studies in ALS patients demonstrated that olesoxime is well-tolerated. These studies also helped to determine the dose regimen used in the pivotal Phase III study.
About the Phase III study in ALS
The study is an 18-month randomized, parallel group, double-blind, placebo-controlled trial evaluating the efficacy and safety of olesoxime against placebo and has benefited from protocol advice obtained from the European Medical Agency EMA. The study completed enrollment in the first quarter of 2010 with 512 patients diagnosed with ALS between 6 and 36 months before enrollment and receiving standard of care. Olesoxime is dosed at 330 mg once-a-day oral capsules. The study is being undertaken in 15 centers in France, Germany, UK, Belgium and Spain and is part of a 3-year collaborative project named MitoTarget (Grant Agreement No: HEALTH-F22008-223388) for which the European Commission has awarded a grant of nearly EUR 6 million.
The primary endpoint of the study is the overall 18-month survival rate. Secondary endpoints include the ALS Functional Rating Scale, time to assisted ventilation, vital capacity (a measure of respiratory function), Manual Muscular Testing and quality of life.
About Amyotrophic Lateral Sclerosis
Amyotrophic Lateral Sclerosis (ALS), often referred to as “Lou Gehrig’s Disease”, is the most common motor neuron disease with a prevalence of 2-3 per 100,000 (30,000 patients in US; 45,000 in Europe at any given time).
Most people who develop ALS are between the ages of 40 and 70 (average age of 55) and over 80% die three to five years after diagnosis. The most common form of ALS is sporadic, but 5-10% of cases are inherited in a dominant manner (familial ALS).
Early symptoms of ALS include muscle weakness in arms and legs; later difficulties in breathing and swallowing are generally the cause of death. There is no treatment today that halts disease progression in ALS patients.
About Trophos’ discovery strategy
The Trophos discovery strategy involves recreating neuronal degeneration processes in the test tube and screening chemical compounds for their ability to block these processes. Diseaserelevant assays are developed using the specific neurons affected in each disease, for example: motor neurons for amyotrophic lateral sclerosis (ALS) and spinal muscular atrophy (SMA), striatal neurons for Huntington’s disease and cortical neurons for Alzheimer’s Disease. In essence, Trophos considers the neuron as a cellular test tube filled with the diverse products of the 30,000 genes expressed by the cell under the conditions that are as close to the physiological environment as possible.
About Trophos SA
Trophos SA is a clinical stage pharmaceutical company developing innovative therapeutics for indications with under-served needs in neurology and cardiology. The company has a novel and proprietary cholesterol-oxime based chemistry platform generating a pipeline of drug candidates with the lead product, olesoxime, fully enrolled in a Phase III study in ALS patients and a second product in the cardiovascular field entering Phase I clinical development. Trophos’ mitochondrial pore modulator compounds enhance the function and survival of stressed cells via modulation of dysfunctional mitochondria through interactions at the permeability transition pore (mPTP). Recently published clinical studies support the therapeutic rationale for mitochondria-targeted drugs in neurology (Alzheimer’s disease) and cardiology (ischemia-reperfusion injury), which Trophos is uniquely placed to exploit. Trophos was founded in 1999 by Antoine Beret and Michel Delaage, former CEO and CSO respectively of Immunotech, and has been financed by funds represented by Amundi Private Equity Funds, Turenne Capital Partenaires, Viveris Management, OTC Asset Management, Sofimac, Sofipaca, CM-CIC Capital Privé, Blue Medical Investment and the Association Française contre les Myopathies (AFM). Trophos has also received non-equity financing from the European Commission, the AFM, the Agence Nationale de Recherche and Oseo Innovation.
About Actelion Ltd
Actelion Ltd is a biopharmaceutical company with its corporate headquarters in Allschwil/Basel, Switzerland. Actelion’s first drug Tracleer®, an orally available dual endothelin receptor antagonist, has been approved as a therapy for pulmonary arterial hypertension. Actelion markets Tracleer® through its own subsidiaries in key markets worldwide, including the United States (based in South San Francisco), the European Union, Japan, Canada, Australia and Switzerland. Actelion, founded in late 1997, is a leading player in innovative science related to the endothelium -the single layer of cells separating every blood vessel from the blood stream. Actelion’s over 2,300 employees focus on the discovery, development and marketing of innovative drugs for significant unmet medical needs. Actelion shares are traded on the SIX Swiss Exchange (ticker symbol: ATLN) as part of the Swiss blue-chip index SMI (Swiss Market Index SMI®).
For further information please contact
For Actelion Ltd:
Roland Haefeli
Vice President, Head of Investor Relations & Public Affairs
Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil
+41 61 565 62 62 begin_of_the_skype_highlighting +41 61 565 62 62 end_of_the_skype_highlighting
+1 650 624 69 36 begin_of_the_skype_highlighting +1 650 624 69 36 end_of_the_skype_highlighting
http://www.actelion.com
For Trophos SA:
Andrew Lloyd & Associates
Andrew Lloyd / Cécilia Derrien
Tel: +33 1 56 54 07 00 begin_of_the_skype_highlighting +33 1 56 54 07 00 end_of_the_skype_highlighting
allo@ala.com / cecilia@ala.com
http://www.trophos.com
Posted under Industry News, Mergers and Acquisitions, Press Releases | No Comments
AstraZeneca signs malaria drug research agreement
Last Updated on Saturday, 24 July 2010 04:24 Written by Editor Monday, 12 July 2010 02:10
* Malaria kills up to 1 million people a year
* Shares up 0.2 percent
LONDON, June 28 (Reuters) – Anglo-Swedish drugmaker AstraZeneca said it was opening up around 500,000 of its chemical compounds to the Medicines for Malaria Venture (MMV) to help speed up development of mosquito-born disease treatments.
The joint venture will allow MMV to try to identify promising compounds with the potential to treat malaria, including drug resistant strains of the disease, AstraZeneca said in a statement on Monday.
It said any promising compounds identified through the screening process would then become starting points for antimalarial drug discovery projects and go to Astra’s research and development unit in Bangalore, India, with the aim of identifying possible drugs for clinical testing.
“Our experience with infection research, and indeed with all of our R&D efforts, has taught us that we will only find solutions to today’s global health challenges through collaborative efforts,” AstraZeneca’s Chief Executive Officer David Brennan said in a statement.
“Opening up our compound library to MMV is an important step toward addressing the enormous unmet medical needs of the developing world.”
Malaria is a parasitic infection transmitted by mosquitoes that kills almost 1 million people a year, most of them children in Africa. Around 40 percent of the world’s population is at risk of malaria, with about 250 million cases every year.
MMV is a not-for-profit public-private partnership which seeks to reduce the malaria burden with the development and delivery of effective and affordable antimalarial drugs.
Under the terms of the agreement, scientists working with MMV will screen 500,000 compounds in AstraZeneca’s library for activity against P. falciparum, the most lethal of the malaria parasites.
A spokesman for Astra said intellectual property of the compounds would remain with the drugmaker. (Reporting by Kate Kelland, editing by Mike Nesbit)
source: cfdspros.com
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SGX Pharmaceuticals Announces Strategic Collaboration To Develop And Commercialize BCR-ABL Inhibitor
Last Updated on Thursday, 13 May 2010 10:22 Written by Editor Thursday, 13 May 2010 10:22
Under the terms of the agreement, SGX will receive from Novartis $25 million in upfront payments and the purchase of SGX common stock. Along with success-based milestones, but excluding royalties, total payments to SGX could exceed $515 million, including a minimum of two years of research funding.
The success of Gleevec(TM) (imatinib), the first targeted therapy in Philadelphia Positive (Ph+CML) proven to inhibit BCR-ABL, has fundamentally changed the treatment of Ph+CML. However, a subset of patients develops resistance to Gleevec or cannot tolerate therapy. For these patients there are currently no other approved treatment options. Drug candidates from SGX’s lead series, developed from its FAST(TM) proprietary drug discovery platform, have exhibited activity against wild-type and drug resistant BCR-ABL mutants, including the most challenging T315I mutant.
“Novartis is the leader in developing novel targeted therapies to treat CML,†said Mike Grey, president and chief executive officer of SGX Pharmaceuticals. “With their extensive experience developing and commercializing Gleevec as well as development of the novel investigational compound, nilotinib/AMN107, we believe they are the ideal partner with whom to develop our series of next-generation BCR-ABL inhibitors. This is a tremendous validation of our FAST technology for generation of novel lead molecules for key therapeutic targets.â€
Background on the Agreement
SGX will be responsible for completing preclinical development of the lead candidate and submitting an Investigational New Drug application with the Food and Drug Administration. SGX will also be responsible for the completion of an initial phase I clinical study, after which time Novartis will be responsible for conducting further clinical development and commercialization of the compound.
In addition to the upfront and milestone payments, SGX will receive royalty payments upon successful commercialization of products developed under the collaboration. SGX retains an option to co-commercialize, in the U.S., oncology products developed under the agreement. If exercised, the option would enable SGX to reinforce the commercial presence in the North American hematology markets which the company plans to establish with the potential launch of Troxatyl(TM) in the second half of 2007, assuming the successful completion of the ongoing Phase II/III clinical trial for the treatment of third-line acute myelogenous leukemia and regulatory approval of Troxatyl for this initial indication in 2007.
Background on CML: Prognosis and Treatments
Chronic myelogenous leukemia is a malignant cancer of the bone marrow causing rapid and abnormal growth of white blood cells. According to the National Institutes of Health, approximately 4,600 new cases of CML are diagnosed annually, accounting for 7 to 20 percent of leukemia cases. CML is associated with a chromosome abnormality called the Philadelphia chromosome. Since its approval in 2001, Gleevec has become the standard of care for Ph+ CML. Results from the IRIS study (International Randomized Interferon versus STI571), the largest clinical trial to date for newly diagnosed adult patients with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase, show that 90.3 percent of patients who were initially randomized to take Gleevec were still alive after 54 months.
The prevalence of CML has increased substantially because Gleevec therapy makes it possible for patients with CML to live with the disease much longer than possible with previously used treatments. Gleevec works directly on leukemic cells by inhibiting the action of BCR-ABL tyrosine kinase, the enzyme responsible for uncontrolled growth of leukemic cells. Despite this clinical success, resistance to Gleevec has emerged in a subset of patients. Once patients lose response to optimized doses of Gleevec, the only currently approved treatment is bone marrow transplantation preceded by high-dose chemotherapy and radiation, for which many CML patients are not eligible.
“We believe that a BCR-ABL inhibitor developed through this collaboration could have the potential to be used both as a monotherapy in second-line treatment of refractory or relapsed CML, and in combination with Gleevec or another agent in first-line treatment of CML,†added Dr. Stephen Burley, chief scientific officer of SGX Pharmaceuticals.
About: FAST, short for Fragments of Active Structures, is SGX’s proprietary fragment-based drug discovery platform for rapid identification of novel, potent and selective small molecule inhibitors of drug targets. FAST addresses many of the limitations of traditional approaches utilized by large pharmaceutical companies to find lead compounds, making it an attractive technology for targets that have not yielded promising leads from high-throughput screening.
FAST is based on a proprietary fragment library of approximately 1,000 structurally diverse, low molecular weight compounds. FAST integrates a series of technologies, including:
* A high-throughput capability to generate many different crystal structures of a target protein in parallel;
* The evaluation of the library of fragments and direct visualization of bound fragments utilizing X-ray crystallography; and
* The use of novel computational and structure-based design methods and iterative synthetic chemistry to optimize these fragments into drug candidates.
SGX believes these combined technologies generate an efficient platform for drug discovery that delivers lead compounds active against a wide range of targets, while accessing high chemical diversity and the potential for good drug-like properties.
About: SGX Pharmaceuticals is a biotechnology company focused on the discovery, development and commercialization of innovative cancer therapeutics. The Company’s lead product candidate, Troxatyl(TM), is currently being evaluated in a pivotal phase II/III trial for the treatment of third-line acute myelogenous leukemia, an indication for which there is currently no approved therapy or standard of care. SGX has developed a pipeline of oncology drug candidates based on its enabling, proprietary FAST(TM) drug discovery platform, including a portfolio of next generation BCR-ABL inhibitors. FAST allows for the rapid identification of novel, potent and selective small molecule compounds for well validated but challenging targets.
source: biotechconnection.com
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Institutional Profile: Sanford-Burnham Sets Up Shop in Florida
Last Updated on Saturday, 24 July 2010 04:09 Written by Editor Thursday, 13 May 2010 10:04
The Sanford-Burnham Medical Research Institute, headquartered in La Jolla, CA, dedicated its new Lake Nona campus in Orlando, FL, last fall. The $85 million building, which opened in April 2009, will employ more than 300 people. Florida attracted Sanford-Burnham in 2006 by offering a $350 million incentive package that included land, construction funds, and in-kind services.
The Lake Nona facility is part of a medical park that includes the University of Central Florida College of Medicine, Nemours Children’s Hospital, and M.D. Anderson Cancer Center-Orlando.
Researchers at Lake Nona will continue to carry out cutting-edge research that will complement areas established at Sanford-Burnham in La Jolla—cancer, infectious and inflammatory disease, aging and stem cells, and neuroscience. In addition, Lake Nona houses a new center for diabetes and obesity research that will cover cardiovascular disease, as well.
Chemical Biology Theme
A strong emphasis on chemical biology underlies all research areas and drives investigations. Chemical biology focuses on identifying small molecules that modulate disease pathways. “That theme weaves itself throughout our research and gets us closer to discoveries that are relevant to small molecule drug discovery,†says John Reed, M.D., Ph.D., president and CEO of Sanford-Burnham.
Finding the correct small molecule can advance a program to prototype medicines and clinical trials. Sanford-Burnham is one of only a few academic centers in the U.S. with advanced high-throughput screening (HTS) systems and access to a large chemical libraries approaching one million small molecules.
Sanford-Burnham’s small molecule drug discovery program is embodied within the Conrad Prebys Center for Chemical Genomics (CPCCG), an effort that involves 75 scientists working on both coasts. The development of HTS assays takes place in La Jolla, while Lake Nona specializes in HTS and houses an ultra-HTS robotic screening center.
The CPCCG provides a one-stop shop whose services span a range of biochemical and cell-based screens to find chemical hits and optimize them into biological probes or potential drugs. The equipment includes a first-in-class, highly flexible HighRes Biosolutions 3-POD nonagon ultra-HTS system and two PerkinElmer Janus workstations. “The robot can run more than one million assays in a workday at Lake Nona,†explains Dr. Reed.
Collaborators Wanted
The newly installed system is capable of handling 50 HTS campaigns a year, yet is currently operating below capacity. This makes Sanford-Burnham an ideal partner for pharmaceutical companies seeking to externalize R&D projects. “We’re looking for corporate partners that fit into our therapeutic research areas,†says Dr. Reed. Collaborations with Sanford-Burnham could identify innovative drug candidates to strengthen pharmaceutical pipelines. Two new partners are Johnson & Johnson Pharmaceutical Research and Development (J&JPRD) and Magellan Bioscience.
Sanford-Burnham will provide J&JPRD with access to HTS assay technologies to investigate drug targets for inflammatory diseases. The collaboration started in January 2009 and is Sanford-Burnham’s first broad-based partnership with a large pharmaceutical company.
Magellan Bioscience began collaborating with Sanford-Burnham in July 2009. The multidisciplinary drug discovery program identifies and develops novel marine microbial compounds that show potential as tools for biological research or new medicines. Marine microbes and their natural products provide a new source of drug candidates for the pharmaceutical industry.
Sanford-Burnham also offers NMR-based screening against targets for which no assay has been developed. “This is unusual in a nonprofit environment, and it’s one of our fortes,†adds Dr. Reed.
The NMR facility at Sanford-Burnham is the largest of its type affiliated with a nonprofit research institution, according to Dr. Reed. Sanford-Burnham’s NMR center includes four fully dedicated high-field magnets with automated sample changers, a library with 4,000 chemical fragments, and three-dimensional (3-D) modeling programs to evaluate hits. Other tools include robotic x-ray crystallography to investigate crystal structures of compounds and their binding to targets and high-content screening microscopy that performs HT phenotype screening.
Engineers at Sanford-Burnham are advancing the field of HT microscopy by developing software for automated image analysis and 3-D imaging systems to monitor cells growing in 3-D conformations in culture.
No Culture Gap
Pharmaceutical firms that collaborate with Sanford-Burnham will not face a cultural divide. A blend of academic and industrial scientists at Sanford-Burnham makes it easier to do business with them. About one-fifth of Sanford-Burnham’s drug discovery researchers have backgrounds in the pharmaceutical and biotechnology industry.
“They bring the discipline and competency of industrial settings,†says Dr. Reed, such as being accustomed to working toward milestone-driven timelines on projects. The same timeline-driven management style guides the workflow at the CPCCG to fulfill contracts with the NIH and the NCI.
Another reason to partner with Sanford-Burnham is its strong reputation for scientific publishing, Dr. Reed says. For the past decade, Sanford-Burnham scientists have ranked first worldwide for scientific citations in biology and biochemistry, according to Thomson Reuters Journal Citation Reports. “The work we do is high quality and has a high impact,†Dr. Reed adds. In addition, Sanford-Burnham ranks second in the number of U.S. patents received for the amount of grant dollars awarded.
Collaborators can work with Sanford-Burnham researchers in California or Florida. The East and West Coast laboratories operate as a fully integrated, single organization, and researchers conduct daily teleconferences. Sanford-Burnham is exploring opportunities to build on this infrastructure to expand to other sites such as Asia in the future.
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Glaxo shows the way in making research pay
Last Updated on Wednesday, 12 May 2010 01:27 Written by Editor Wednesday, 12 May 2010 01:27
The world’s top 10 pharmaceutical companies spend around $50bn a year on research & development…but have very little to show for it.
The cost of bringing a new drug from the laboratory to market has risen to around $1bn and, in an influential study released last year, McKinsey estimated that the industry’s return on R&D over the past decade has averaged just 7 per cent, below its cost of capital. It is startling that companies boasting operating margins of 30 per cent or more are actually destroying value in their core activity. No wonder the sector has been de-rated so substantially over the past 10 years.
It was meant to be very different. The introduction of “industrial†technologies, including genomics and high-frequency screening of chemical compounds in the 1990s was supposed to lead to an explosion in productivity. Pharma companies built huge research compounds and started to think of their scientists as engineers, perhaps even factory workers that would reliably churn out new medicines. That turned out to be a blind alley: drug discovery remains an almost personal process, based on intuition and serendipity as much as technology.
Now the industry, led by GlaxoSmithKline, is reversing course. Over the past few years, GSK has progressively started to break up its research clusters again, from thousands of people, to 300-400 and most recently units as small as 60-80 people, with more responsibility. At the same time, it is saving money by trimming the gold-plated physical infrastructure with which its boffins like to surround themselves. And it is becoming better at killing off drugs early that have a poor chance of making it to market. Each research project now has to pass a “Dragons Denâ€-type committee before it gets substantial funding.
The early results look encouraging. GSK had no new products approved in the US between 1998 and 2007 but 15 since then with another six in its late-stage pipeline. And at yesterday’s results presentation, chief executive Andrew Witty said that the group’s return on investment in R&D had risen from the 7 per cent industry average to 11 per cent in 2009 and that he “aspired†to 14 per cent. The fact that GSK – first among its peers – has revealed a proper measure of research productivity is as encouraging as the numbers. It may even tempt investors back into the sector.
source: blogs.ft.com
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Conference Proceedings Preview – 2nd Annual Ocular Diseases and Drug Discovery
Last Updated on Tuesday, 4 May 2010 12:05 Written by Editor Tuesday, 4 May 2010 12:05
The conference proceedings preview is composed of speaker biographies and abstracts, along with selected PowerPoint presentations. Registered attendees receive a CD with the full version of the proceedings on May 27, 2010. In addition, registered attendees will receive an updated online version two weeks after the conference.
To view the preview, please click on the following link:
http://www.gtcbio.com/Ocular_Preview/main.htm
Click here to register! Register two, the third goes free.
CONFERENCE HIGHLIGHTS
Keynote Presentation – Megan McLaughlin, Discovery Medicine, Ophthiris DPU, GlaxoSmithKline
Pazopanib Eye Drops for Neovascular AMD
Keynote Presentation – Stephen Tsang, Edward S. Harkness Eye Institute, Columbia University
Transplantation of Reprogrammed Embryonic Stem Cells Improves Visual Function in a Mouse Model for Retinitis Pigmentosa
Conference Sessions:
I:Â Â Â Age-Related Macular Degeneration
II:Â Â Recent Drug Developments & Mechanisms in Ocular Diseases
III:Â Â Ocular Diseases
IV:Â Future of Ocular Diseases Therapeutics
V:Â Â Novel Drug Delivery Methods
For a full agenda visit: http://gtcbio.com/userAgenda.aspx?id=148
Register 2, the 3rd person goes free! Click here to register.
Distinguished Presenters:
+ Megan M. McLaughlin – Keynote Speaker, Ophthiris Discovery Performance Unit, GlaxoSmithKline + Stephen Tsang, M.D., Ph.D. – Keynote Speaker, Edward S. Harkness Eye Institute, Columbia University + Barbara Marie Wirostko, M.D. – Featured Speaker, Senior Medical Director, Team Lead Ophthalmology, Pfizer + Charles S. Tressler, M.D. – Featured Speaker, Senior Director, Global Medical, Pfizer + Richard L. Beckman, M.D., Senior Vice President, Development, Lux Biosciences + Robert M. Burk, Ph.D., Senior Research Investigator, Allergan + Bo Chen, Department of Genetics, Howard Hughes Medical Institute, Harvard Medical School + Daniel C. Chung, DO, MA, Instructor of Ophthalmology, University of Pennsylvania School of Medicine + Robert J. Collier, Ph.D., Associate Director, Retina Drug Discovery, Alcon Research + Valeriu Damian, Manager, GlaxoSmithKline + Darlene A. Dartt, Scepens Eye Research Institute, Department of Ophthalmology, Harvard Medical School + Philip D. Gregory, Ph.D., Chief Scientific Officer, Sangamo BioSciences + Avner Ingerman, M.D., M.Sc, Senior Vice President, General Manager, ORA Clinical R&D + Konrad Kauper, Director, Tissue Engineering, Neurotech + Ivan B. Lobov, Ph.D., Staff Scientist, Ophthalmology Therapeutics, Regeneron + Karen Meerovitch, Ph.D., Senior Director, Mimetogen Pharmaceuticals + Takahiro Ogawa, Ph.D., Senior Vice President, Research and Development, Senju USA + George W. Ousler III, Director of Dry Eye, ORA Clinical Research and Development + Michael A. Patane, Ph.D., Chief Scientific Officer, EyeGate Pharmaceuticals + Przemyslaw Mike Sapieha, Ph.D., Assistant Professor, Ophthalmology, University of Montreal + Abraham Scaria, Ph.D., Senior Scientific Director, Genzyme + David Sherris, Ph.D., President and Chief Executive Officer, Paloma Pharmaceuticals + Craig Struble, Ph.D., Associate Technical Director, Drug Metabolism, Covance + Jennifer Sun, M.D., MPH, Beetham Eye Institute, Joslin Diabetes Center + Corinne G. Wong, Ph.D., Principal, Chief Scientific Officer, SCLERA + Wai T. Wong, M.D., Ph.D., Chief, Unit on Neuron-Glia Interactions in Retinal Disease, National Eye Institute, NIH + David F. Woodward, Ph.D., Senior Director, Allergan
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Ligon Discovery Announces Appointment of Errol B. De Souza as Executive Chairman
Last Updated on Monday, 11 January 2010 05:36 Written by Editor Monday, 11 January 2010 05:36
20-year Industry Veteran Brings Extensive Experience in Drug Discovery and Development
CAMBRIDGE, Mass., Nov. 23 /PRNewswire/ — Ligon Discovery, Inc., which uses proprietary small molecule microarray technology to find drugs against high-value targets, today announced the appointment of pharmaceutical industry veteran Errol B. De Souza as Ligon’s Executive Chairman of the Board.
“I’m very pleased to welcome Errol De Souza as Executive Chairman of the Board,” said Patrick Kleyn, Ligon’s chief executive officer and co-founder. He added, “Errol’s breadth of experience in the life sciences industry — particularly his leadership taking drug candidates from exploratory research through clinical development — will be an asset to Ligon as we advance our current drug discovery campaigns targeting cancer and coagulations disorders, utilizing our proprietary small molecule microarray platform.”
Dr. De Souza commented, “I look forward to chairing Ligon’s Board, and contributing to the forward momentum being built by the company in discovering small molecule drugs against disease targets that others have found intractable. Ligon’s unique and proprietary small molecule microarray technology offers compelling advantages, including broad applicability to all target classes, unprecedented scale of parallel screening, and minimal protein requirements. I believe Ligon has what it takes to leverage this already validated technology.”
Errol B. De Souza, Ph.D. is a seasoned pharma and biotech industry leader with 20 years of experience in senior level Research & Development (R&D) and management positions at Aventis, Hoechst Marion Roussel (HMR), DuPont Merck, Neurocrine Biosciences, Synaptic Pharmaceuticals and Archemix. His R&D experience spans from leading large R&D organizations at DuPont Merck (Director of CNS Diseases Research), HMR (Senior Vice President and Head of Global Lead Generation) with worldwide responsibilities for chemistry, chemical development, biotechnology, high throughput screening and core research functions to Aventis (Senior Vice President and Site Head of US Drug Innovation and Approval) where he had worldwide responsibilities for managing the CNS, Immunology and Inflammatory Diseases pipeline as well as administrative responsibilities for the entire R&D organization in the US including the Global Drug Development Center.
Dr. De Souza’s particular focus has been on the developing innovative approaches to accelerate progression of compounds from the candidate to clinical proof-of-concept stage and beyond through development of biomarker and pharmacogenomic strategies and utilization of imaging techniques. His experience on the biotech side spans from starting companies (Founder, Chief Scientific Officer and Executive Vice President of R&D at Neurocrine), to leading companies (President & CEO of Synaptic Pharmaceuticals and Archemix, Inc) and experience on several Boards of Directors and Scientific Advisory Boards of both public and private companies. In these capacities, he has successfully raised capital in both private and public environments and been involved in multiple collaborations with large pharmaceutical companies.
About Ligon Discovery
Ligon Discovery is a Harvard spinout that leverages a patented platform technology to identify pre-clinical drug candidates. The company’s high-throughput microarray “chip” transforms the speed of the drug discovery process and expands the scope of new drug prospecting to include previously intractable targets. With funding from incTANK Ventures, the team has deployed the SMM technology, originally invented at Harvard University and further developed at the Broad Institute (founded by MIT and Harvard University) in Cambridge, and has established one of the largest small molecule screening capabilities in the industry. Using this facility, Ligon has successfully completed screens in the fields of coagulation and cancer, and is actively pursuing drug discovery in other areas of high unmet medical need. For more information, visit www.ligondiscovery.com.
SOURCE Ligon Discovery, Inc.
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DG-AMMOS: A New tool to generate 3D conformation of small molecules using Distance Geometry and Automated Molecular Mechanics Optimization for in silico Screening.
Last Updated on Monday, 11 January 2010 12:27 Written by Editor Monday, 11 January 2010 12:27
Discovery of new bioactive molecules that could enter drug discovery programs or that could serve as chemical probes is a very complex and costly endeavor. Structure-based and ligand-based in silico screening approaches are nowadays extensively used to complement experimental screening approaches in order to increase the effectiveness of the process and facilitating the screening of thousands or millions of small molecules against a biomolecular target.
Both in silico screening methods require as input a suitable chemical compound collection and most often the 3D structure of the small molecules has to be generated since compounds are usually delivered in 1D SMILES, CANSMILES or in 2D SDF formats.
Results: Here, we describe the new open source program DG-AMMOS which allows the generation of the 3D conformation of small molecules using Distance Geometry and their optimization via Automated Molecular Mechanics Optimization. The program is validated on the Astex dataset, the ChemBridge Diversity database and on a number of small molecules with known crystal structures extracted from the Cambridge Structural Database.
A comparison with the free program Balloon and the well-known commercial program Omega generating the 3D of small molecules is carried out. The results show that the new free program DG-AMMOS is a very efficient 3D structure generator engine.
Conclusions: DG-AMMOS provides fast, automated and reliable access to the generation of 3D conformation of small molecules and facilitates the preparation of a compound collection prior to high-throughput virtual screening computations.
The validation of DG-AMMOS on several different datasets proves that generated structures are generally of equal quality or sometimes better than structures obtained by other tested methods.
Author: David LagorceTania PenchevaBruno VilloutreixMaria Miteva
Credits/Source: BMC Chemical Biology 2009, 9:6
Lumpy Assay Results
Last Updated on Monday, 11 January 2010 12:23 Written by Editor Monday, 11 January 2010 12:23
When we screen zillions of compounds from our files against a new drug target, what can we expect? How many hits will we get, and what percentage of those are actually worth looking at in more detail?
These are long-running questions, but over the last twenty years some lessons have been learned. A new paper in J. Med. Chem. emphasizes one of the biggest ones: if at all possible, run your assays with some sort of detergent in them.
Why would you do a thing like that? Compound aggregation. The last few years have seen a rapidly growing appreciation of this problem. Many small molecules will, under some conditions, clump together in solution and make a new species that has little or nothing to do with their individual members. These new aggregates can bind to protein surfaces, mess up fluorescent readouts, cause the target protein to stick to their surfaces instead, and cause all kinds of trouble. Adding detergent to the assay system cuts this down a great deal, and any compound that’s a hit without detergent but loses activity with it should be viewed with strong suspicion.
The authors of this paper (from the NIH’s Chemical Genomics Center and Brian Shoichet’s lab at UCSF) were screening against the cysteine protease cruzain, a target for Chagas disease. They ran their whole library of compounds through under both detergent-free and detergent conditions and compared the results. In an earlier screening effort of this sort against beta-lactamase, nearly 95% of the hits (many of them rather weak) turned out to be aggregator compounds. This campaign showed similar numbers.
There were 15 times as many apparent hits in the detergent-free assay, for one thing. Some of these were apparently activating the enzyme, which is always a bit of an odd thing to explain, since inhibiting enzyme activity is a lot more likely. These activators almost completely disappeared under the detergent conditions, though. And even looking just at the inhibitors, 90% of the hit set in the detergent-free assay went away when detergent was added. (I should note that control cruzain inhibitors performed fine under both sets of assays, so it’s not like the detergent itself was messing with the enzyme to any significant degree).
They point out another benefit to the detergent assay – it seems to improve the data by keeping the enzyme from sticking to the walls of the plastic tubes. That’s a real problem which can kick your data around all over the place – I’ve encountered it myself, and heard a few horror stories over the years. But it’s not something that’s well appreciated outside of the people who set up assays for a living (and not always even among some of them).
So, let’s get rid of those nasty aggegators, right? Not so fast. It turns out that some of the compounds that showed this problem during the earlier beta-lactamase work didn’t cause a problem here, and vice versa. Even using different assays designed to detect aggregation alone gave varying results among sets of compounds. It appears that aggregation is quite sensitive to the specific assay conditions you’re using, so trying to assemble a blacklist of aggregators is probably not going to work. You have to check things every time.
One other interesting point from this paper (and the previous one): curators of large screening collections spend a lot of time weeding out reactive compounds. They don’t want things that will come in and react nonspecifically with labile groups on the target proteins, and that seems like a reasonable thing to do. But in these screens, the compounds with “hot” functional groups didn’t have a particularly high hit rate. You’d expect a cysteine protease to be especially sensitive to this sort of thing, with that reactive thiol right in the active site, but not so. This ties in with the work from Benjamin Cravatt’s group at Scripps, suggesting that even fairly reactive groups have a lot of constraints on them – they have to line up just right to form a covalent bond, and that just doesn’t happen that often.
So perhaps we’ve all been worrying too much about reactive compounds, and not enough about the innocent-looking ones that clump up while we’re not looking. Detergent is your friend!
Source: corante.com
Posted under Cell Analysis, Cell-based Assays, Compound Screening, Industry News, Press Releases | No Comments
Commonwealth Biotechnologies, Inc. Acquisition of GL Biochem: Market Update
Last Updated on Saturday, 24 July 2010 04:09 Written by Editor Tuesday, 1 December 2009 11:24
Shareholders approve sale of the Richmond, Virginia assets as required under the
GL Biochem Asset Purchase Agreement
RICHMOND, Va.–(Business Wire)–
Commonwealth Biotechnologies, Inc. (“CBI”) (NASDAQ Capital Market: CBTE) has
recently announced a definitive share purchase agreement to acquire
Shanghai-based GL Biochem and associated businesses (the “GL Group”), the
largest global supplier of research-grade peptide products and peptide reagents.
Management is pleased to provide a market update regarding the history,
operations and strategy of the GL Group, the industry and marketplace for
peptides and peptide reagents, and progress of the merger transaction.
Background
The GL Group was established in Shanghai by Dr. Hongyan Xu in 1998 and has grown
to become the largest supplier of pre-clinical peptide reagents and custom
peptide synthesis services in the world. The Company has achieved rapid growth
without debt financing or additional capital investment and has expanded the
scale and scope of its operations using only free cash flow from its operations.
Today, the GL Group employees over 800 staff, operates 35,000 ft2 and 120,000
ft2 manufacturing facilities in Shanghai and is in the process of jointly
commissioning a third Shanghai manufacturing facility, `Mimotopes-China`. Over
the past 5 years, the GL Group has demonstrated compound annual revenue growth
of over 40%. Despite the global economic downturn, the GL Group reported a 20%
increase in revenues in the first half of 2009 (unaudited) compared to the same
period last year.
Industry Context
Peptides play an important role in modulating many physiological processes in
the body and therefore have excellent potential as therapeutic agents. Peptide
drugs have a number of advantages over both small molecules and proteins,
including low toxicity and immunogenicity, excellent specificity, high potency
and a low probability of drug-drug interaction problems. Several technical
challenges in the use of peptides as drugs have been overcome in recent years
and they now represent one of the key growth areas in the drug discovery
industry.
Marketplace
GL Biochem caters for the outsourcing requirements of universities, research
institutes, pharmaceutical and biotechnology companies for reagents as well as
research and development services. Large pharmaceutical and biotechnology
companies typically have some capabilities in-house but choose to outsource much
of their research and development work to specialist providers such as GL
Biochem. Pharmaceutical companies are now unable to generate the large number of
necessary candidate compounds in-house and this has led to an increasing trend
for outsourcing of drug discovery research. The worldwide market for custom
peptides was estimated to be between US$250m and US$450m in 2003 and is
projected to grow at an annual average rate of 11.9%, valuing the market between
$550m and $990m by 2010.
Business and Operational Strategy
In recent years, GL Biochem has achieved cost leadership in the research grade
custom peptide industry through exploiting its scale of production, cumulative
experience, competitive labor costs and the manufacture of its own raw
materials. This production cost advantage has allowed GL Biochem to price its
products and services below other major manufacturers and therefore establish a
prominent position in the pre-clinical custom peptide and reagent markets. GL
Biochem sells a portion of its custom peptides and reagent products directly to
the public but also generates significant revenues through an original equipment
manufacturer (“OEM”) strategy, whereby peptides or reagents produced by GL
Biochem are sold to peptide or chemical companies in the West and retailed under
the Western company’s brand name.
Products and Services
GL Biochem develops, manufactures, markets and distributes peptides, peptide
reagents and related services for the life-science sector. GL Biochem`s
offerings include:
* Research-grade peptides: Custom-made peptide molecules for biological research
and drug development applications;
* Peptide libraries: Large numbers of peptides produced in small quantities for
various screening applications in immunology and drug discovery;
* Catalogue peptides: Commonly requested off-the-shelf peptides, typically for
pharmaceutical or cosmetic applications;
* Peptide reagents: Including amino acids, peptide coupling reagents, protecting
reagents and linkers peptide synthesis; and
* Antibodies: Tailored monoclonal and polyclonal antibody production services
for immunology applications.
Merger Progress
On September 3, 2009 CBI entered into a definitive share purchase agreement to
acquire all of the outstanding stock of GL Biochem (Shanghai) Ltd, as well as
all of the outstanding shares of GL Biochem (Danyang) Ltd, GL Peptide (Binhai)
Ltd, and 86% of the shares of GL Peptide (Shanghai) Ltd. Completion of the
transaction is subject to a number of conditions precedent, which among other
things include the sale of the Richmond businesses-CBI Services and Fairfax
Identity Laboratories (collectively, the “Divisions”). The sale of the Divisions
was approved by CBI`s shareholders at the annual meeting of shareholders held on
October 9, 2009. Another material condition is completion of the GL GAAP
qualified audited accounts. These are scheduled for completion on October 15,
2009. Upon fulfillment of these key conditions, CBI anticipates being able to
put the proposed merger to its shareholders for approval by years` end.
About CBI
CBI offers cutting-edge research and development products and services to the
global life sciences industry. CBI now operates through: (1) CBI Services, a
discovery phase contract research organization; (2) Fairfax Identity
Laboratories, a DNA reference business; (3) Mimotopes Pty Ltd, Melbourne,
Australia, a peptide and discovery chemistry business; and (4) Venturepharm
(Asia), a contract research consortium specializing in drug discovery and
development, process scale-up, formulation development, cGMP manufacturing and
clinical trial management. For more information, visit CBI on the web at
www.cbi-biotech.com.
About GL Biochem (Shanghai) Ltd
GL Biochem (Shanghai) Ltd is an international leader in the research,
development, manufacture and marketing of diverse biochemical and fine
chemicals, with a particular strength in peptides, peptide reagents and related
products. With over 800 highly-trained staff and state-of-the-art facilities, GL
Biochem is now the largest manufacturer of research-grade peptides and peptide
reagents globally. For more information visit www.glschina.com.
Forward Looking Statements
No statement made in this press release should be interpreted as an offer to
purchase any security. Such an offer can only be made in accordance with the
Securities Act of 1933, as amended and applicable state securities laws. Any
statements contained in this release that relate to future plans, events or
performance are forward-looking statements that involve risks and uncertainties
as identified in CBI`s filings with the Securities and Exchange Commission.
Actual results, events or performance may differ materially. Specifically, CBI
cannot guaranty that:
* the transaction referenced herein will close;
* the combined companies will perform as anticipated on an ongoing basis;
* the market for peptide drugs will continue to grow as referenced herein; or
* CBI`s shareholders and lenders will approve this transaction.
Readers are cautioned not to place undo reliance on these forward-looking
statements, which speak only as the date hereof. Further, all forward-looking
statements included in this press release are based upon information available
to CBI as of the date hereof. CBI assumes no obligation to update any such
forward-looking statements.
Commonwealth Biotechnologies, Inc.
Richard Freer, COO
804-648-3820
Copyright Business Wire 2009
Posted under Business and Investment, Industry News, Mergers and Acquisitions, Press Releases | No Comments
Eurogentec Announces Agreement to Acquire AnaSpec, Inc.
Last Updated on Saturday, 24 July 2010 04:09 Written by Editor Thursday, 29 October 2009 10:24
Liège, Belgium—October 23, 2009.
Eurogentec S.A. (“Eurogentecâ€) announces today a final agreement for the acquisition of AnaSpec Inc (“AnaSpec†or the “Companyâ€), a privately held proteomics company based in Fremont, California. Founded in 1993, AnaSpec is a leading provider of integrated proteomics solutions for life science research and diagnostics with expertise in peptides synthesis, labeled peptides and antibodies, fluorescent dyes and enzyme activity assays. AnaSpec has developed one of the world’s largest collections of catalog and dye-labeled peptides in the fields of Alzheimer Disease, Multiple Sclerosis and enzyme inhibitor screening. Leveraging its expertise in peptide, antibodies and fluorescent dyes, AnaSpec has established a leading edge portfolio of integrated proteomics solutions such as FRET based assays and SensoLyteâ„¢ assays for basic research, high-throughput screening and drug discovery. Furthermore, AnaSpec’s proprietary fluorescent dyes are being used by the world’s leading diagnostic companies to enhance their diagnostic solutions.
“Bringing AnaSpec into the Eurogentec Group is a strategic decision for our company,†explains Jean-Pierre Delwart, CEO of Eurogentec. “Through this acquisition, Eurogentec becomes a leading integrated solution provider for the Life Science and Diagnostics sectors. Our combined expertise enables Eurogentec to provide innovative solutions in the fields of Genomics and Proteomics for basic research in the biotech and pharmaceutical sectors, as well as applied solutions in the diagnostics sector. As an example, the HiLyte Fluorâ„¢ dyes and QXLâ„¢ quenchers that are part of AnaSpec’s high performance detection assays will be integrated into Eurogentec’s comprehensive portfolio of oligonucleotides. This will establish a license-friendly alternative to most dye-labeled oligonucleotides from competitors for commercial and diagnostic applications. Moreover, AnaSpec considerably strengthens Eurogentec’s geographical presence in the US and Eurogentec will directly market and support AnaSpec’s products in the EU.†The founders of AnaSpec, Anita Hong, President, and Frank Hong, CEO, comment: “It is important for the sustained development of AnaSpec to integrate into a larger organization where its current assets and competencies can bring real added value. The total complementarities between Eurogentec’s and AnaSpec’s existing businesses and the cross-fertilization opportunities for future developments are a key factor for the success of this partnership. We are very much looking forward to closely working with the Eurogentec Team from this perspective.”
AnaSpec’s founders and senior management, Anita and Frank Hong, will remain aboard the Company in leading roles in continuing to grow AnaSpec’s businesses, further expanding the high value detection reagents focus and facilitating integration with Eurogentec. Eurogentec intends to maintain the Company’s state-of-the-art Fremont facility, to which AnaSpec recently moved operations, and its valued employees.
Troutman Sanders LLP served as legal counsel, and Achelous Partners, LLC, served as financial advisers to AnaSpec. DLA Piper LLP served as legal counsel to Eurogentec on this transaction.
About Eurogentec
Eurogentec is a leading global supplier of innovative reagents, kits, specialty products and custom services to scientists in the life science, biotechnology, pharmaceutical and diagnostic markets. Eurogentec provides a wide range of expertize in small- and large-scale DNA, RNA, PCR and qPCR kits, peptide synthesis and antibody supply for research applications. Our ISO13485:2003-certified manufacturing facilities in Belgium provides a wide range of high value oligonucleotide-based components for diagnostic and therapeutic applications. Eurogentec’s Belgium manufacturing facility is complemented by additional production facilities in North America and Japan. Eurogentec is also an experienced Contract Manufacturing Organization (CMO) for Biopharmaceuticals, operating a full-service, state-of-the-art GMP facility in Belgium.
Eurogentec is a privately held company headquartered in Liège, Belgium, with subsidiaries in North America, France, Germany, the UK, the Netherlands and Switzerland and has additional production facilities in North America, Japan and Singapore. Eurogentec employs 400+ people globally.
Contact Information:
Jean-Pierre Delwart
Chief Executive Officer, Eurogentec
Ph: +32-475-607-884
Philippe Cronet
Chief Scientific Officer, Eurogentec
Ph: +32-4-372-7411
Albert Hong
Business Development Specialist, AnaSpec Inc.
Ph: (800) 452-5530 x243
Posted under Business and Investment, Industry News, Mergers and Acquisitions, Press Releases | No Comments
ERGONEX Pharma receives Frost & Sullivan’s European Orphan Diseases Entrepreneurial Company Award 2009
Last Updated on Thursday, 22 October 2009 12:02 Written by Editor Thursday, 22 October 2009 12:02
Appenzell, Switzerland, October 19, 2009 / b3c newswire / – ERGONEX Pharma received one of the prestigious ‘European Orphan Diseases Entrepreneurial Company Award’ on the occasion of Frost & Sullivan’s ’2009 Excellence in Healthcare Awards Banquet,’ held in London on 8th October 2009. The highly competitive award was presented to ERGONEX Pharma in recognition of the company’s innovative therapeutic concept, its impressive display of technological know-how and targeted vision.
ERGONEX Pharma is focused on the clinical development and commercialisation of Terguride for the treatment of distinct orphan diseases. Terguride is currently being evaluated for the treatment of pulmonary arterial hypertension (PAH) in a Phase II trial in Europe and headline results are expected in 2010.
Dr. Rudolf Reiter, CEO of ERGONEX Pharma comments: “This award comes at an exciting and challenging time for ERGONEX Pharma. I see it as recognition of the vision, the commitment and work of the company, which would not have been possible without the continued support, expertise and out-of-the-box thinking of our partners in the on-going clinical trial. We believe that Terguride has the potential to contribute a new quality to emerging combination therapies for patients, who do not tolerate, have become resistant to or are insufficiently controlled by current treatment options in PAH.â€
The Frost & Sullivan Healthcare Awards Banquet honours Europe’s best healthcare companies for their achievements over the course of this year. Frost & Sullivan’s highly competitive awards recognise companies in a variety of regional and global markets for demonstrating outstanding achievement and superior performance in areas such as leadership, technological innovation, customer service, and strategic product development.
About Pulmonary Arterial Hypertension
Pulmonary arterial hypertension is a disorder of the blood vessels in the lung, in which the pressure in large blood vessel rises above normal. Walls of the blood vessels are thickened and hardened, becoming less elastic. Hence, the decrease in lumen leads to increases in pressure. Patients with PAH suffer from extreme shortness of breath as the heart struggles to pump against these high pressures causing such patients to ultimately die of heart failure.
About Terguride
Terguride acts as a potent antagonist on 5-HT2B and 5-HT2A receptors: It has anti-proliferative and anti-fibrotic activities and drives reverse remodelling processes. Serotonin is a signal molecule in the body with many functions. In the blood vessel walls of the lung, it stimulates proliferation of smooth muscle cells and narrowing of the blood vessels, which has been implicated in PAH. Furthermore, trophic effects of serotonin on the heart contribute to right heart hypertrophy and progression towards heart failure. Terguride is approved in Japan for hyperprolactinemia acting as a partial dopamine agonist on the pituitary gland.
About ERGONEX Pharma – www.ergonex.com
ERGONEX Pharma is a pharmaceutical company focused on developing and commercialising well-tolerated and effective products for novel and typically underserved indications. This is being achieved by forging collaborations with commercial and academic partners with expertise in the field of interest and through outsourcing activities to service providers.
Contact
ERGONEX Pharma GmbH
Ruetistr. 20
CH-9050 Appenzell
Switzerland
Phone: +41 71 788 4065
E-mail: info@ergonex.com
www.ergonex.com
Posted under Grants and Awards, Industry News, Press Releases | No Comments
Scripps Research scientists awarded $3.9 million grant to develop new compound screening platform
Last Updated on Tuesday, 20 October 2009 10:04 Written by Editor Tuesday, 20 October 2009 10:04
Bicoastal effort could help revolutionize the search for new therapies
La Jolla, CA, and Jupiter, FL, October 5, 2009 –A pair of scientists from The Scripps Research Institute, one on each coast, has been awarded a five-year $3.9 million grant from the National Institutes of Health (NIH) to develop a new technology to accelerate the search for new protein ligands – compounds that bind to proteins and alter their function.
Current screening technology, which is slow and expensive, has caused what the NIH calls a “major bottleneck” in the search for these basic tools that are key for the broader study of biological processes and that lay the groundwork for development of most drugs.
The grant, awarded as part of the NIH’s new Roadmap Transformative R01 Program, will be shared between the laboratories of Tom Kodadek, Ph.D., a professor in the Scripps Research Departments of Chemistry and Cancer Biology in Jupiter, Florida, and Benjamin Cravatt III, Ph.D., professor and chair of the Department of Chemical Physiology and member of The Skaggs Institute for Chemical Biology and Helen L. Dorris Child and Adolescent Neuro-Psychiatric Disorder Institute at Scripps Research in La Jolla, California.
“Ben and I are extremely pleased to win this highly competitive award and to be among the first selected for the new Transformative Grant program from the NIH,” Kodadek said. “This is a perfect example of the tremendous collaborative possibilities available within Scripps Research. We worked on the proposal together and the fact that we’re both part of the same national institution will make the work that much easier as we move ahead.”
Cravatt added, “This project is a good reflection of what those of us at Scripps Research in La Jolla and in Florida are trying to accomplish – fostering collaborative interaction and working on complimentary research projects. This will help cement the strong working relationship between our two campuses.”
The NIH Roadmap Transformative R01 (T-R01) Program awards were launched this year to support exceptionally innovative, high risk, original, and/or unconventional research projects that have the potential to create or overturn fundamental scientific paradigms.
“The appeal of the Pioneer, New Innovator, and now the T-R01 programs, is that investigators are encouraged to challenge the status quo with innovative ideas, while being given the necessary resources to test them,” said NIH Director Francis S. Collins, M.D., Ph.D. “The fact that we continue to receive such strong proposals for funding through the programs reflects the wealth of creative ideas in science today.”
Two Innovative Methods and a Cab Ride
The new Scripps Research project will combine two separate technologies from each laboratory – a peptoid library synthesis and screening platform developed in the Kodadek laboratory and an activity-based protein profiling system developed in the Cravatt laboratory.
Kodadek’s screening platform involves the creation of vast libraries of peptoids (peptoids are synthetic molecules that are similar to peptides, compounds that when joined together make up proteins) displayed on microscopic beads that are screened against fluorescently tagged proteins that light up after binding with a high affinity, highly selective ligand.
“Our screening technology simulates the cellular environment,” Kodadek said, “because the tagged proteins, which represent only a small fraction of the total, are mixed in with un-tagged competitors. There is a specificity filter built into the process from the beginning.”
The Cravatt Laboratory has pioneered the Activity-Based Protein Profiling technology, which allows scientists to identify protein classes based on their activity. The basic technology attaches a single label or probe to proteins from a particular subset of the proteome, which allows access to what are considered low abundance proteins and makes it ideal for massive parallel screening experiments. So far, Activity-Based Protein Profiling probes have been developed for more than a dozen distinct enzyme classes.
Cravatt’s technology makes it possible to target what he calls “interesting classes of proteins” but in a highly parallel fashion – hundreds of screens at a time of those multi- million member peptoid libraries. Although both scientists have known one another for some time, many of the details of the collaboration were worked out on a cab ride from England’s Heathrow airport to London last summer.
“Tom and I had an editorial board meeting in London, and shared a cab from the airport,” Cravatt said. “The fact that Tom had recently joined Scripps Florida helped get us energized about the project.”
“It’s true,” Kodadek added. “The ideas behind the grant proposal just popped out of that ride.”
A Transformational Marriage
The combination of the Kodadek and Cravatt advanced technologies will allow the screening of massive peptoid libraries (1-10 million synthetic compounds) in parallel fashion, a novel strategy that the scientists predict will increase the rate of ligand discovery by several hundred times over current methods.
“The gist of our proposal is quite simply marrying these two beautifully worked out technologies,” Kodadek said. “We have a good track record on both sides, plus we’re building off these innovative platforms, so if this works, and I’m certain it will, it will definitely be transformational.”
That transformation, when it comes, should result in more lead drug candidates, Kodadek said, because while the scientists’ success rate has been lower than those using current high throughput screening technology, the quality of the ligands identified has been significantly better. Some of this is due to the fact that simple synthetic compounds like peptoids have many advantages over other ligands such as antibodies. They can be modified easily for attachment to surfaces and can be produced in relatively large amounts at lower cost and rather quickly – a multi-million member peptoid library, for example, can be created in around three days.
“The way most science works today,” Cravatt said, “is that researchers tend to huddle around those areas where there are tools available. By combining our technologies, we will have a streamlined, unbiased way to identify high quality protein ligands and that will give us access to a large part of the proteome that others can’t study right now because the current technology is inadequate.”
About The Scripps Research Institute
The Scripps Research Institute is one of the world’s largest independent, non-profit biomedical research organizations, at the forefront of basic biomedical science that seeks to comprehend the most fundamental processes of life. Scripps Research is internationally recognized for its discoveries in immunology, molecular and cellular biology, chemistry, neurosciences, autoimmune, cardiovascular, and infectious diseases, and synthetic vaccine development. Established in its current configuration in 1961, it employs approximately 3,000 scientists, postdoctoral fellows, scientific and other technicians, doctoral degree graduate students, and administrative and technical support personnel. Scripps Research is headquartered in La Jolla, California. It also includes Scripps Florida, whose researchers focus on basic biomedical science, drug discovery, and technology development. Scripps Florida is located in Jupiter, Florida.
Source: eurekalert.org
MALDI-Based Method May Reduce Cost of Rx-Screening Assays, Speed Drug Development
Last Updated on Tuesday, 20 October 2009 09:44 Written by Editor Tuesday, 20 October 2009 09:44
This story originally ran on Oct. 6.
By Tony Fong
Researchers from the University of Cincinnati and MDS Analytical Technologies have used mass spectrometry to develop a high-throughput screening method for drug discovery they say can be more precise and cost-effective than existing techniques.
The technique is based on a MALDI triple-quadrupole platform and exploits the selective multiple-reaction monitoring transition features of the platform. By doing so, the new method is able to lower the cost of high-throughput screening for drug compounds to pennies per well from as much as $1 per well currently, Ken Greis, associate professor of cancer and cell biology and director of proteomics and mass spectrometry at the University of Cincinnati College of Medicine, told ProteoMonitor recently.
A study detailing the method was published Sep. 15 in the online edition of Rapid Communications in Mass Spectrometry.
In the paper, Greis and his co-authors said that drug discovery typically begins with a validated target enzyme “with the initial goal of finding appropriate molecular scaffolds with inhibitory activity via high-throughput screening.” The scaffolds are then subsequently used for lead compound optimization, and “ideally for the development of a safe and effective therapeutic compound.”
The most common methods of high-throughput screening have been fluorescence- and chemiluminescence-based approaches. Such approaches, Greis said, have been “very successful” because the same reagents can be used for many different enzymes.
But that same characteristic also creates a risk for interference.
“When one’s evaluating a compound repository for inhibitors, you often have a series of compounds that will fluoresce themselves,” Greis said. “If they fluoresce, they’re going to give you a false signal. Alternatively … there are compounds that inhibit the fluorescent properties, or what’s called quenching fluorescence, [that] also give false read-outs.”
Another problem is in the way the assays get generalized so that the reagents work for a wide range of enzymes. Such assays are called coupled assays: “You have a product being formed from your enzyme reaction but that’s not what actually triggers the fluorescence,” Greis said. “That product gets converted to another enzyme to another product through another enzyme to another product that then can be fluoresced.â€
This series of enzyme step, or coupled assays, ultimately results in a read-out. “The problem is any compound that interferes with any of those steps along the way also gives you false read-outs,” which tend to be false positives, he added.
But by using mass spectrometry to measure enzyme activity, Greis and his colleagues are able to get a direct read-out, “so a mass spectrometer effectively can give you a quantitation and a mass of a compound.”
By taking a ratio of the substrate being converted to a product — the essence of an enzyme assay, Greis said — and measuring that directly on a mass spec, there is no interference either from quenching or auto-fluorescence.
“And what we’ve found thus far is we’ve not seen any false positive read-outs. If we get a compound that shows that it’s active, even in single-point assays, it’s been demonstrated that it’s a dose-dependent inhibitor.”
And because the method uses native peptides or small-molecule substrates, the method can be done for “at most, pennies per sample well,” Greis said. By comparison, fluorescent and chemiluminescence reagents cost between 50 cents to $1 per well.
“So if you run a million compounds, you can run up a half-million dollars of reagents costs right away, whereas the label-free read-out is going to cost you maybe a couple thousand dollars for the reagents,” he said. “That’s a mass spec advantage.”
A prior study by researchers in China had demonstrated the utility of a MALDI-Fourier transform mass spectrometer for high-throughput screening of small-molecule substrate/product conversion.
The researchers chose AChE because of its long history of enzyme assay development, including colorimetric assays, pH-change assays, and most recently aggregation-induced fluorescence assays and mass-spec assays.
Speed is of the Essence
They also chose a MALDI platform, rather than an electrospray platform, because of the higher speed that can be achieved on the MALDI. Most enzymatic reactions contain salts that can interfere with mass spectrometry. An ESI platform requires a desalting step, which limits the throughput to five to 10 seconds per sample. A MALDI-based approach skips the desalting step, however, because the technology is less sensitive to salts.
“Essentially all that we do is run the enzyme reaction on a 384-well format,” Greis said. “We transfer all at once into a matrix plate mix and onto our MALDI target plate.”
Because there are no cleanup steps on the MALDI triple-quad, samples can be scanned at up to three samples per second, he said.
Greis acknowledged that the MALDI technology, especially the MALDI triple-quad, is not a popular tool for drug discovery. In his opinion, that’s because drug-discovery researchers were trained on electrospray mass specs and are comfortable with them.
“To then move them into a MALDI platform that they don’t understand, they’ve got a bias that it can’t be quantitative, and all these sorts of things from earlier studies using MALDI-based approaches that have been demonstrated time and time again to not be true anymore — I think there’s a cultural thing,” he said.
A criticism of a MALDI approach is that while it works well for peptide substrate screening, it doesn’t for small-molecule substrate products because of matrix interference in the low mass range.
“And we show very directly … that by taking advantage of the transition,” a chemical fragmentation that is diagnostic of a substrate or product “that one can do in a triple-quad, that matrix interference completely goes away,” Greis said.
The researchers tested their method by screening a library of 1,008 structurally diverse compounds across 384-well microtiter plates as an example of a single-dose primary screen, and reported that all known AChE inhibitors resulted in complete inhibition of enzyme activity, as expected. The hits were then validated “by demonstrating concentration-dependent inhibition and the rank order of inhibitory potency in hit follow-up assays,” they said in their study.
The technique they’ve developed can also be used on a simple MALDI instrument, though it works best for peptide substrate enzymes. With low molecular-weight enzymes, sensitivity can be an order of magnitude lower on a simple MALDI “because you’d have to be using enough enzyme substrate product to see your substrate products down in those low mass ranges in amongst all of the matrix peaks,” Greis said.
Also, Greis said there will be enzymes — such as fatty acids and long-chain hydrocarbons —that will not be amenable to a MALDI-based approach.
“The fact of the matter is that any mass spectrometry-based technique is only as good as the molecule that it’s trying to evaluate,” he said. “We have to be able to ionize the substrate and/or the product to be able to measure and quantify it.”
In ongoing work, he and his team members are developing multiplex assays. The typical screening approach is to take a target enzyme and pass the whole repository across it to look for inhibitors, and then validate the inhibitors. The next therapeutic target is then set up and the process is repeated.
With a mass spec-based approach, “as long as your enzymes reactions are compatible … you can run multiple enzymes in one pot and pass your repository against it once and get hits for all those different enzymes,” Greis said.
In conferences, Greis and his colleagues have presented proof-of-concept studies that show that “this in fact works quite well using a kinase and acetylcholinesterase or a kinase with a protease all in the same part,” he said. “We’ve shown that we can get selective inhibitors for each of them individually without interference in the multiplex format.”
Source: genomeweb.com
Posted under Compound Screening, HT Screening, Industry News, Press Releases | No Comments
EPA seeks broad powers to regulate chemical industry
Last Updated on Monday, 19 October 2009 03:49 Written by Editor Monday, 19 October 2009 03:49
By RANDY LEE LOFTIS / The Dallas Morning News
rloftis@dallasnews.com The Obama administration announced Tuesday that it is seeking broad new powers to regulate toxic substances in commerce, products and the environment, including clear authority to ban unsafe chemicals.
Environmental Protection Agency Administrator Lisa Jackson laid out the administration’s principles for rewriting the nation’s main toxic chemicals law, which has not been revised significantly in 33 years.
During that time, thousands of new chemicals, processes and even types of substances have entered the economy, many with little or no health and safety review by manufacturers or the government. Researchers have found the chemicals in millions of Americans’ bodies; one study found big increases in the levels of a widely used flame retardant in the blood of Dallas residents.
“Today, everything from our cars to the cellphones we all have in our pockets are constructed with plastics and chemical additives,” Jackson said. “Chemicals are ubiquitous in our economy and our products as well as our environment and our bodies.”
House and Senate Democrats are expected to introduce bills to strengthen the Toxic Substances Control Act soon. Among the anticipated changes is one that Jackson endorsed: letting the EPA act on its own to restrict or outlaw chemicals that do not meet health and safety standards.
A 1991 federal appeals court ruling on asbestos essentially gutted the agency’s power to ban chemicals under the existing law. Congress banned further use of polychlorinated biphenyls, or PCBs, when it passed the toxic substances law in 1976, but the 1991 asbestos ruling has kept the EPA from acting against other risky chemicals.
Jackson said new chemicals and scientific breakthroughs had rendered the law weak and obsolete. Those include the discovery that some chemicals can disrupt the human endocrine system, new knowledge of the risks of some flame retardants, and increasing production of extremely small nanoscale materials that have undergone virtually no health screening.
While some substances might be proved harmless, Jackson said, the widespread discovery of many synthetic chemicals in virtually the world’s entire population demands safety assurances that an outdated law cannot provide.
“Over the years, not only has [the toxics law] fallen behind the industry it’s supposed to regulate, it’s been proven an inadequate tool for providing the protection against chemical risks that the public rightly expects,” she said in remarks prepared for delivery in San Francisco on Tuesday evening.
The administration wants to change the current chemical safety system, which puts new chemicals under more scrutiny than the 80,000 already believed to be in use, Jackson said. Sorting through all existing chemicals could take decades at the current pace, with the public possibly facing undue risk while the process drags on.
Jackson said the EPA would prioritize reviews of existing chemicals by requiring more information from industry on health and safety, use and human exposure. She added, however, that the agency would not skip over possible risks in the interest of speed.
“None of the 80,000 should be exempt,” Jackson said. “I think industry understands that.”
Texas is the heart of the U.S. chemical industry, especially along the Gulf Coast from Beaumont-Port Arthur to Corpus Christi. The federal toxics law regulates chemicals as they come into contact with people through products or industrial uses. Risks from chemical emissions into the air fall under the Clean Air Act.
The chemical industry has endorsed reform of the toxics law along the general lines that Jackson mentioned, in part to boost confidence among consumers worried about compounds in their bodies and their children’s. The industry said its principles include imposing more stringent requirements for health and safety information from manufacturers and giving more weight to risks for children and other vulnerable groups, both mirroring the EPA’s goals
“We are convinced today, through our own testing in the industry, that our products are safe,” Cal Dooley, president and CEO of the American Chemistry Council, the trade group that represents most Texas chemical manufacturers, told reporters. “But we need that validation by the government regulatory agency that is doing the scientific assessments.”
While Congress works to rewrite the law, Jackson said, the EPA plans special reviews of chemicals that have raised particular human health concerns since the law was passed. They include bisphenol A, or BPA, used in polycarbonate plastics and epoxy resins; polybrominated diphenyl ether (PBDEs), used as flame retardants; perfluorinated compounds, used in soil- and water-repellant coatings on many consumer products; and phthalates, used in many plastics.
The EPA will issue action plans for managing risks from four of the compounds in December and will publish others in four-month intervals, Jackson said.
“This is very good news,” said Dr. Arnold Schecter of the University of Texas School of Public Health, Dallas, who studies persistent organic pollutants such as the ones the EPA singled out for special review. He has found PBDEs in 100 percent of American mothers’ breast milk tested, with some women carrying “orders of magnitude” more than women in Europe, where the compounds have been phased out since 2004.
A joint study by the School of Public Health, where Schecter is professor of environmental sciences, and the UT Southwestern Medical Center found a “very large increase” in the PBDEs in Dallas residents’ blood in 2003 compared with blood tested in 1993, Schecter said.
Schecter said stronger federal action on risks from persistent organic compounds was overdue.
“What a refreshing change,” he said.
Source: Dallas News
Posted under Biotech & Pharma Law, Industry News, Press Releases | No Comments
Trophos launches the new generation of its fast plate imaging instrument, the Plate RUNNER HD
Last Updated on Thursday, 22 October 2009 11:09 Written by Editor Monday, 12 October 2009 03:31
Marseille, FRANCE, 2009 September 29 – Trophos SA, a clinical stage pharmaceutical company developing innovative therapeutics for indications with under-served needs in neurology and cardiology, announced today the launch of the new generation of its fluorescence fast plate imaging system, the Plate RUNNER HD(R).
Trophos originally developed the Plate RUNNER HD(R) to speed up its own screening campaigns for drug discovery and development. The company has now implemented an improved version which offers much better resolution and allows imaging of the 7mm well of the standard 96 plate in matrices of up to 8192 x 8192 pixels. This positions it as the superior alternative to the traditional automated microscope in a wider area of cellular and small organism imaging applications such as neurite outgrowth or C.elegans screens. The Plate RUNNER HD(R) is protected by patents granted in the USA and Europe.
“The Plate RUNNER HD(R) has now reached both a performance and an operational level that allows it to be widely used in various imaging platforms,” said Damian Marron, CEO of Trophos. “We have optimized it by regular use in our screening and research platforms. Use in other labs such as the Neuronal Cell Biology & Pathology research unit directed by Dr Christian Neri at the Inserm Psychiatry and Neurosciences Centre (Paris, France) and the Laboratory of Motor Neuron Biology directed by Dr Alvaro G. Estévez at the Burke Medical Research Institute (NY, USA) has confirmed its performance.” (For further information, see http://www.broca.inserm.fr and http://www.burke.org).
The Plate RUNNER HD(R) fills the gaps between the low sensitivity/low resolution/cell consuming fluorescence plate readers, the high sensitivity but non-imaging flow cytometer, and the slow, poorly automated and small field fluorescence microscope. It does this by allowing whole well/full plate imaging in just 2 minutes 40 seconds for 96 images of 1024 x 1024 pixels, 8 minutes at 4096 x 4096 resolution and 25 minutes at the extremely powerful 8192 x 8192 resolution. The maximum resolution gives details as fine as 1 micron, which covers the vast majority of cellular imaging applications.
“The instrument is not only the source of our pipeline – nearly 1 million compounds screened in eight years – but also an everyday research tool that does in two minutes a job that usually requires a week manually,” said Pierre Delaage, Head of Development of Trophos Instruments. “Using exclusively open data formats, the Plate RUNNER HD(R) integrates smartly and smoothly with all existing imaging and data processing environments with no hidden extra costs. It is also a “green product” using at least ten times less electrical power for illumination than its competitors. It has the important advantage of having a lower price and TCO than the traditional microscope-based instruments.”
Dr Christian Neri, Research Director at the Psychiatry and Neuroscience Center of Inserm in Paris, stated “We have been using the Trophos screening system since its first commercial version; it allowed us to simply and rapidly automate our screening protocols on C.elegans worms and on cells. To move further in C.elegans screens we needed a far higher resolution without sacrificing light, sensitivity and field. We have now seen that Trophos’ latest instrument meets perfectly our very stringent requirements.”
“We continue to directly sell and support the Plate RUNNER HD(R) and are now looking to set up a commercial and industrial partnership to address more widely the global market opportunity,” added Marron. “The Plate RUNNER HD(R) offers unique performance and can be a great fit for imaging solutions manufacturers and vendors, to exploit opportunities for example in the area of small organism or angiogenesis screens as well as cellular screens.”
About the Plate RUNNER HD(R): Developed by Trophos since 1999 initially for its own HTS platform, The Plate RUNNER HD(R) is a rapid fluorescence 96-plate imager giving full 7mm well images in single snapshots (ie no mosaic reconstruction), embedding three commonly used wavelength illumination lamps using fast-switching LED technology, thus leading to more homogeneous light, very long life time (100 000 hours against 5000 hours for xenon or mercury lamps), higher speed and dramatically reduced maintenance costs. Images are given in standard 1024 x 1024 definition but also in higher 2048 x 2048, 4096 x 4096 and even 8192 x 8192 pixels definition, leading to details of about 1 micron in size.
Compared to classic automated microscopes, The Plate RUNNER HD(R) is much more simple, integrated, automated, robust and fast; it has no oculars (eyepieces), no huge frame, no complicated auto focus system, no complicated settings, no complicated software, and does not need any cooling/heating delay between illumination sessions nor painful recalibration between sessions. Built on modular, open and interoperable design and data formats, it is compatible with any existing image processing platform. Training for common tasks is achieved in less than 1 hour, and there is no need of high skilled people to install or set it up.
Driven by Trophos proprietary software running on standard low cost PCs and using advanced real time programming techniques coming from the industry, the device reliably acquires 96 images at 1024 x 1024 definition in just 2 minutes 40 seconds (for a standard 488nm excitation and 200ms exposure time), 8mn for 4096 x 4096 images and 25mn for 8192 x 8192 images.
The device is patent protected in France, Europe and USA. Patent is pending in Canada and Japan. Detailed specifications are available here (http://www.trophos.com/download/pr_datasheet.pdf).
About Trophos: http://www.trophos.com Trophos is a clinical stage pharmaceutical company developing innovative therapeutics from discovery to clinical validation for indications with under-served needs in neurology and cardiology. The Company has a novel and proprietary cholesterol-oxime based chemistry platform generating a pipeline of drug candidates, with the lead product, olesoxime (TRO19622), in phase II clinical trials and a second product, TRO40303, planned to enter the clinic in 2010. Trophos’ mitochondrial pore modulator compounds enhance the function and survival of stressed cells via modulation of dysfunctional mitochondria through interactions at the permeability transition pore (mPTP). Recently published clinical studies support the therapeutic rationale for mitochondria targeted drugs in neurology (Alzheimer’s disease) and cardiology (ischemia-reperfusion injury), which Trophos is uniquely placed to exploit.
Trophos has not only invested in science but also in technology such as the Plate RUNNER HD(R), which is a key reason why Trophos was able to bring products into phase II clinical trial after only 8 years, instead of the 12-15 or even 20 years commonly observed”.
For further information, please contact:
Andrew Lloyd & Associates Andrew Lloyd / Neil Hunter Tel: +44 1273 675100 allo@ala.com
Source: medadnews.com
Posted under Compound Libraries, Compound Screening, Industry News, Press Releases | No Comments
GENFIT identifies compounds which modulate clock genes for the treatment of cardiometabolic disease and CNS disorders
Last Updated on Monday, 12 October 2009 02:29 Written by Editor Monday, 12 October 2009 02:29
Lille (France), Cambridge (Massachusetts, United States), September 28, 2009 – GENFIT (Alternext: ALGFT; ISIN: FR0004163111), a biopharmaceutical company at the forefront of drug discovery and development, focusing on the early diagnosis and preventive treatment of cardiometabolic and neurodegenerative diseases, today announces the successful identification of Hit compounds for an orphan nuclear receptor which plays a key role in the regulation of circadian cycle in different organs. These Hits were identified through the screening of chemical libraries performed at GENFIT facilities in Lille.
In humans, many aspects of behavior and physiology are coordinated by an endogenous circadian rhythm (circa diem, meaning approximately one day) that is generated by an internal clock system which synchronizes daily variations in gene expression to rhythms such as sleep and wake alternance, variations in body temperature, blood pressure, heart rate, as well as cognition, attention and mood.
A large body of evidence from both human and animal studies now points to a relationship between circadian disorders and altered metabolic response, suggesting that circadian and metabolic regulatory networks are tightly interconnected.
As a consequence, misalignment of the internal timing system versus environmental stimuli, such as day/night cues, as experienced during jetlag or shift work, may result in dysregulation of physiological cycles of fuel utilization and energy storage, and has been associated with increased risk to develop obesity, type 2 diabetes, hyperlipidemia, high blood pressure and cardiovascular disease. As well, modulating, resetting and stabilization of central circadian rhythms have been proposed as therapeutic strategies for certain CNS disorders.
“This is an important milestone in our drug discovery programs in the field of cardiometabolic disease and CNS disorders”, says Dean Hum (CSO of Genfit). “Deorphanisation of this nuclear receptor further demonstrates our expertise in this class of therapeutic targets, and provides novel series of compounds to address the focus therapeutic areas of Genfit with a very innovative approach via modulation of clock genes and the circadian rhythm”.
About GENFIT:
GENFIT is a biopharmaceutical company focused on the Discovery and Development of drug candidates in strategic therapeutic fields linked to cardiometabolic and neurodegenerative disorders (prediabetes/diabetes, atherosclerosis, dyslipidemia, obesity, Alzheimer’s…). GENFIT uses a multi-pronged approach based on early diagnosis, preventive solutions, and therapeutic treatments to address these major public health concerns and their unmet medical needs. GENFIT’s proprietary research programs and its partnerships with leading pharmaceutical companies, including Sanofi-Aventis, Solvay Group, Pierre Fabre, and Servier, have resulted in the creation of a rich and diversified pipeline of drug candidates at different stages of development. GENFIT’s lead proprietary compound, GFT505, is currently in Phase II and two other compounds, in partnership with Sanofi-Aventis (AVE0897) and SOLVAY (SLV341), are in the advanced stages of Phase I.
With facilities in Lille, France, and Cambridge, MA (USA), the Company has about 130 employees, including over 100 scientists. GENFIT is a public company listed on the Alternext trading market by Euronext(TM) Paris (Alternext: ALGFT; ISIN: FR0004163111). www.genfit.com
Contacts:
GENFIT
Jean-Fran̤ois Mouney РChairman of the Management Board
+33 (0)3 20 16 40 00
Milestones – Press Relations
Bruno Arabian
+33 (0)1 75 44 87 40 / +33 (0)6 87 88 47 26 – barabian@milestones.fr
Copyright Hugin
The appendixes relating to the press release are available on:
http://www.hugingroup.com/documents_ir/PJ/CO/2009/158601_88_7960_20090928-PR-GENFIT.pdf
This announcement is originally distributed by Hugin. The issuer is solely responsible for the content of this announcement.
Source: euronext.com
Agilux Laboratories Hires New Associate Director to Lead In Vitro ADMET Services Division
Last Updated on Thursday, 8 October 2009 12:22 Written by Editor Thursday, 8 October 2009 12:22
- Adrian Sheldon, Ph.D., Positions Contract Research Organization for Growth - WORCESTER, Mass.--(Business Wire)-- Agilux Laboratories, Inc., a Contract Research Organization (CRO) that provides bioanalytical and in vitro Absorption Distribution Metabolism Excretion Toxicology (ADMET) services for the biotechnology and pharmaceutical industries, has appointed Dr. Adrian Sheldon as associate director of In Vitro ADMET Services. In this role, Dr. Sheldon will build the In Vitro ADMET Services division offering testing services that allow biotechnology and pharmaceutical companies to screen drug candidates for desirable ADMET properties. Dr. Sheldon will leverage more than 17 years of industry experience, including establishing new business units for In Vitro ADMET and Immunochemistry within an established CRO. He will extend Agilux`s emphasis on customer service, rapid turnaround and exceptional data quality to the company`s newly formed In Vitro ADMET Services Testing Division. "We are excited to have someone with Adrian`s expertise, successful track record and demonstrated abilities at Agilux," said Jim Jersey, president and CEO at Agilux. "Adrian brings the right balance of scientific expertise and customer focus, which is consistent with Agilux`s mission of delivering high quality data at unprecedented speeds. We are confident that both the Agilux team and our clients will benefit from his unique skill set." Prior to Agilux, Dr. Sheldon served as associate director of In Vitro ADMET at Charles River Laboratories. Prior to Charles River Laboratories, Dr. Sheldon was group leader in Assay Development/HTS/In Vitro ADMET at ArQule where he co-managed a team responsible for screening compounds generated by the industry-leading combinatorial chemistry laboratory. He received his Ph.D. from Boston University and his A.B. from Harvard University. Dr. Sheldon has authored numerous scientific publications and holds two patents. "I am very pleased about joining the team at Agilux," stated Dr. Sheldon. "We have an incredible opportunity to change the way early stage development services are delivered and I am confident that I will be able to contribute to Agilux`s continuing success." About Agilux Laboratories, Inc. Agilux Laboratories, Inc. is a privately held contract research organization (CRO) focused on bioanlaytical and PK/PD testing services for the biotech and pharmaceutical industries. Leveraging industry and contract research experience of its management team, the company delivers high quality bioanlaytical chemistry and PK/PD data more rapidly. Agilux helps clients make better decisions during drug discovery and development by providing quality data earlier in the research process by using technologies and systems that increase turnaround speed well beyond industry standards. Founded in 2007 by industry experts Jim Jersey, Steve Guyan and Peter Glick, Agilux is headquartered in Worcester, MA and is funded by private equity firm, Ampersand Ventures. For more information, call 508-753-5000 or email sguyan@agiliuxlabs.com. Online at www.agiluxlabs.com. Agilux Laboratories, Inc. Steve Guyan Vice President, Sales and Marketing 508-762-4402 sguyan@agiluxlabs.com
Source: Reuters
Ore Pharmaceuticals Announces Upcoming Publication of Research Study on ORE1001
Last Updated on Thursday, 8 October 2009 12:19 Written by Editor Thursday, 8 October 2009 12:19
Ore Pharmaceuticals Inc. (Nasdaq:ORXE), announced today the publication of an article in the online version of the journal Inflammation Research titled, "Effects of the ACE2 inhibitor GL1001 on acute dextran sodium sulfate-induced colitis in mice." This article discussed the efficacy of Ore`s lead drug candidate, ORE1001 (formerly GL1001), in the dextran sodium sulfate animal screening model for inflammatory bowel disease drugs. The results show that treatment with ORE1001 displayed efficacy on par with that of the oral standard, sulphasalazine. ORE1001 improved common measures of the extent of damage, such as histopathology, in a dose-related and statistically significant manner. Moreover, ORE1001 markedly decreased tissue myeloperoxidase activity, a well-known marker of inflammation. The findings, when considered along with other studies of ORE1001, support further development of the compound in gastrointestinal inflammatory conditions. ORE1001 has progressed through multiple dose clinical phase I testing in the U.S. and is on track to commence a Phase Ib/IIa trial in ulcerative colitis, one of the two main disorders that comprise inflammatory bowel disease (IBD), in the second half of 2009. It is estimated that up to one million Americans are affected by IBD. With typical onset in childhood or early adulthood, these disorders cause many decades of pain and suffering and result in significant lost productivity, in addition to the direct costs of medical and surgical care. The burden on the U.S. healthcare system alone is significant; IBD is associated with health care costs estimated at more than $1.7 billion. Ore believes that ORE1001, if approved, could represent a significant enhancement to current therapies for treating this debilitating disease. The print article is expected to be published in an upcoming issue of Inflammation Research. The full text article is currently available online at: http://www.springer.com/birkhauser/biosciences/journal/11. Ore Pharmaceuticals Overview Ore Pharmaceuticals Inc. (the "Company") is a pharmaceutical asset management company. The Company acquires interests in pharmaceutical assets whose value, it believes, it can significantly enhance through targeted development, with the goal of then monetizing these assets through a sale or out-licensing. Initially, the Company will focus on developing and monetizing its current portfolio, which includes four clinical-stage compounds in-licensed from major pharmaceutical companies. The Company`s four compounds in its development portfolio are: ORE1001, its lead compound, ORE10002, ORE5002 (tiapamil) and ORE5007 (romazarit). Safe Harbor Statement This press release contains "forward-looking statements," as such term is used in the Securities Exchange Act of 1934, as amended. Such forward-looking statements include our ability to identify strategies for making its businesses successful and the impact of such strategies on our business and financial performance and on shareholder value. Forward-looking statements typically include the words "expect," "anticipate," "believe," "estimate," "intend," "may," "will," and similar expressions as they relate to Ore Pharmaceuticals or its management. Forward-looking statements are based on our current expectations and assumptions, which are subject to risks and uncertainties. They are not guarantees of our future performance or results. Our actual performance and results could differ materially from what we project in forward-looking statements for a variety of reasons and circumstances, including particularly risks and uncertainties that may affect the Company`s operations, financial condition and financial results and that are discussed in detail in the our Annual Report on Form 10-K and our other subsequent filings with the Securities and Exchange Commission. They include, but are not limited to: whether the compounds we develop will be commercially viable; whether we will be able to begin to generate sufficient new revenue from licensing or other transactions early enough to support our operations and continuing compound development; whether there will be valid claims for indemnification from the buyers of our Genomics Assets; whether there will be claims from the landlords of the leased properties we have assigned, the buyer of our Preclinical Division or the assignee of our Cambridge facility lease, that we would be required to pay as guarantors of such leases; whether we will be able to collect amounts due under the terms of promissory notes from the buyers of our Genomics Assets and molecular diagnostic business; whether we will be able to manage our existing cash adequately and whether we will have access to financing on sufficiently favorable terms to maintain our businesses and effect our strategies; whether we will be able to maintain our NASDAQ listing; whether we will be able to attract and retain qualified personnel for our business; and potential negative effects on our operations and financial results from workforce reductions and the transformation of our business. Ore Pharmaceuticals Inc. undertakes no obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Ore Pharmaceuticals Inc. Benjamin L. Palleiko SVP & CFO 617-649-2001 bpalleiko@orepharma.com
Source: Reuters
KINAXO launches KinAffinity® services for efficient profiling of kinase inhibitors in cells or tissue
Last Updated on Thursday, 8 October 2009 10:53 Written by Editor Thursday, 8 October 2009 10:53
Martinsried, Germany, October 01, 2009 / b3c newswire / - KINAXO Biotechnologies GmbH announced today that it added KinAffinity® to its service portfolio. KinAffinity® provides invaluable information about a kinase inhibitor’s selectivity in a cell or tissue of interest. It simultaneously determines affinities for native kinases expressed within a cellular proteome and thus overcomes the limitations of traditional biochemical assays that only use recombinant proteins.
Kinase inhibitors with favorable pharmaceutical properties are extensively pursued as therapeutics in numerous oncological, neurological and inflammatory indications. However, their development faces significant challenges such as target specificity for the disease-relevant target proteins. Here, KinAffinity® provides critical information to select the right lead compound for clinical development.
KinAffinity® combines proprietary chemical proteomics methods with state-of-the-art quantitative mass spectrometry (see Sharma et al., Nature Methods 2009). Endogenously expressed, post-translationally modified kinases are enriched by a ready-to-use affinity matrix in the presence of native binding partners and competed with the kinase inhibitor of interest. Subsequently, bioinformatic methods are used to reveal the inhibitor’s quantitative cellular target profile. The inhibitor’s targets are ranked by their affinities and reported to the customer.
KinAffinity® is applicable for type I and type II kinase inhibitors. It facilitates selectivity analysis on an organism level that accounts for differences in protein expression between different cells, as well as their mutational and modification status that might affect drug binding.
Link to the news release
About KINAXO – www.kinaxo.com
KINAXO Biotechnologies GmbH is a privately-held biotechnology company based in Munich/Martinsried, Germany. As a spin-off of the Max Planck Institute of Biochemistry in Martinsried, we closely cooperate with several of the Institute’s most outstanding scientists in the field of chemical proteomics and quantitative mass spectrometry, namely Dr. Henrik Daub, Prof. Jesper Olsen and Dr. Jürgen Cox. KINAXO’s technology portfolio delivers direct insights into a compound’s cellular interactions and its mode of action and is routinely applied to decrease drug development times and improve therapeutic strategies. To expand its KinAffinity® platform, KINAXO recently received financial funding from the Bavarian Ministry of Economics. The underlying technology was licensed from the Max Planck Society and co-developed by scientists of the Max Planck Institute of Biochemistry and KINAXO’s scientists.
KINAXO has several ongoing collaborations with major pharmaceutical and biotechnology companies such as Boehringer Ingelheim, Johnson & Johnson and Bayer, and is financed by European investors BioM, High-Tech Gründerfonds, KfW, the Max Planck Society, and Mountain Partners.
Source:Â B3C Newswire
Posted under Drug Development, Drug-Like Compounds, Industry News, Press Releases, R & D | No Comments
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