Archive for March, 2009
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 27 March 2009 10:00 Written by admin Friday, 27 March 2009 10:00
BERKELEY, Calif.–(BUSINESS WIRE)–Plexxikon Inc. today announced the issuance of key composition-of-matter patents covering novel compounds discovered through the company’s Scaffold-Based Drug Discoveryâ„¢ platform. Plexxikon’s pipeline of preclinical and clinical stage product opportunities currently span potential treatments for cardio-renal disease, CNS disorders, inflammation, metabolic disease and oncology. Two of the three recently issued patents (U.S. patents no. 7,498,342 and no. 7,504,509) cover compounds derived from the company’s discovery efforts to target protein kinases for the treatment of multiple indications including oncology and inflammation. The third patent (U.S. patent no. 7,476,746) covers novel compounds from the company’s PPAR (peroxisome proliferator-activated receptor) program yielding novel therapeutic opportunities for metabolic disorders and other diseases.
“We are pleased to be adding these additional patents to our growing and broad intellectual property portfolio,†stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “Plexxikon’s novel approach to drug discovery has enabled the company to advance multiple first-in-class drug candidates which are covered by strong intellectual property, and as a result, to secure significant pharmaceutical industry interest in our programs.â€
In contrast to fragment-based approaches, Plexxikon’s platform has generated multiple product opportunities by mining the relatively unexplored chemical space of scaffold-like cores and by utilizing co-crystallography early in the discovery process to guide chemical optimization of these scaffolds. Further, the company has developed methods to make highly selective kinase inhibitors as yet rarely seen. Plexxikon has demonstrated the ability to develop selectivity between two targets with as little as one amino acid difference in their catalytic domains. This capability has created the opportunity for the development of new targeted drugs not only for oncology, but also for chronic disease indications outside oncology where safety hurdles are even higher. To date, Plexxikon’s platform has led to the development of a targeted medicine for the treatment of melanoma, a drug candidate for polycystic kidney disease (PKD), an oral agent for rheumatoid arthritis and a broad spectrum oral diabetic therapeutic, all representing novel agents addressing significant unmet needs.
Dr. Prabha Ibrahim Promoted to Vice President of Chemistry
In other news, Prabha N. Ibrahim, Ph.D., was promoted to the position of vice president of chemistry, bringing over 15 years of experience to her position. As head of chemistry since 2002, she has played a key role in building the company’s synthetic and medicinal chemistry capabilities leading to the discovery of Plexxikon’s novel drug candidates now in the clinic and in preclinical development. Prior to Plexxikon, Dr. Ibrahim was a senior scientist at CV Therapeutics, where she was responsible for the identification and development of preclinical candidates for cardiovascular indications. She also previously worked at Amgen, where she played an integral role in small molecule drug discovery for inflammation therapeutics. Dr. Ibrahim earned her Ph.D. at the University of Victoria, Canada, and was a Welch Foundation Fellow at Rice University in Houston.
Plexxikon Profile
Plexxikon is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s clinical stage programs include PLX4032 for the treatment of melanoma and colorectal cancer, PLX5568 for the treatment of PKD and PLX204 for the treatment of diabetes. Among the company’s preclinical development programs, candidates are being developed for the treatment of rheumatoid arthritis, multiple sclerosis and other autoimmune diseases.
Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform is being applied to build a pipeline of product opportunities in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in varied disease areas addressing significant unmet needs in each therapeutic category.
Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.
Posted under ChemInformatics, Clinical Trials, Compound Libraries, Discoveries, Innovations and Patents, Drug-Like Compounds, North America, Press Releases, Targeted Libraries | Comments Off
Molecular Fingerprints Point The Way To Earlier Cancer Diagnosis And More Targeted Treatment
Last Updated on Friday, 27 March 2009 09:52 Written by admin Friday, 27 March 2009 09:52
ScienceDaily (Mar. 27, 2009) — Metabolites are molecular fingerprints of what your cells are up to and Dr. Arun Sreekumar wants to know the impression made by cancer.
You’ve likely heard about metabolites; your physician probably screens for some known ones such as triglycerides or cholesterol at your annual physical. Scientists suspect we have about 3,000 metabolites that come from our food or are synthesized from different compounds in our bodies.
Dr. Sreekumar, a cancer researcher at the Medical College of Georgia Cancer Center, wants those screens of the blood or urine to also detect early signs of cancers such as leukemia, bladder, kidney and breast when the chance for cure is best.
He’s already begun to identify metabolites that indicate not only the presence of prostate cancer, but its aggressiveness, a tool that could help tailor optimal treatment. The search began in men at risk: those with elevated prostate specific antigen, or PSA, levels. A PSA test along with a digital rectal exam is today’s standard for prostate screening so physicians typically do both in men age 50 and older. But PSA levels are actually better at helping determine if prostate cancer has returned, Dr. Sreekumar says.
Elevated levels of PSA, a protein, are not always predictive of cancer, which means a lot of men get unnecessary biopsies. PSA measurements also can’t distinguish between tumors that have a good outcome versus those with a poor one.
“The physician does not really have the tools in hand to really say that this tumor will spread to other organs or not.” says the Georgia Cancer Coalition Distinguished Cancer Scholar. “We want to find clinical markers that supplement PSA.”
Aggressiveness is a major factor in prostate cancer treatment. In fact some men with slow growing disease likely won’t even need treatment. So he wants to provide a complement of biomarkers that accurately diagnose and categorize the disease then help monitor success of treatment. These early studies indicate a urine test may one day be possible to do just that.
He and colleagues at the University of Michigan reported in the Feb. 12 issue of Nature what appears to be one of the first metabolites implicated in cancer invasion. They looked at 1,126 metabolites in 262 samples taken from men with high PSA levels. They consistently found elevated levels of the amino acid sarcosine in the prostate tissues of men with cancer; levels were highest in what appeared to be the most aggressive tumors.
Sarcosine, a modified form of the amino acid glycine, was a known entity but its function was unclear. Scientists thought it might be a dumping ground for excess methyl groups needed to enable chemical changes of genes, proteins and other body components that can affect what and how much they do.
This process called methylation can be a good thing – like when it’s helping an embryo develop – but when it goes badly, it can cause disease such as cancer. While sarcosine’s dumping role seemed to protect from cancer, the Michigan scientists found its action actually helps induce tumors. In fact, when they added it to prostate cancer cells, the cells became more aggressive. Exactly how that process works is still under study but the findings were pretty consistent.
“When we looked at patients with metastatic disease, sarcosine levels were sky high compared to patients with localized tumors,” says Dr. Sreekumar. “It’s enabling invasion.”
Because cancer and people are both very heterogenous, measures need to be taken in larger population samples, he says. Also, they found a small group of patients with negative biopsies and high sarcosine levels. “We don’t know how many of them have missed cancer,” says Dr. Sreekumar who joined the MCG faculty in February.
These are among the reasons he believes in strength in numbers. “In the real world of biomarkers, you want 100 percent sensitivity. If the patient has cancer, you want to pick it up. We need to have a kind of multiplex test where you can test for say10 different entities and have a greater confidence that what you are stating about the tumor is true. Our goal is to develop such a panel and research on sarcosine is a first step toward achieving this.”
In his new position at MCG, he’s looking to expand the number of metabolites known to be predictive of prostate and other cancers. In prostate cancer, he’s beginning with follow up on other metabolites identified in the Michigan study in which researchers identified a total of six metabolites, including sarcosine, linked to increased tumor progression. A total of 89 metabolites were different in metastatic prostate cancer compared to localized disease.
He’s excited about what metabolites will one day tell cancer physicians and patients but adds that they are just a piece of what our bodies can tell us about a potential cancer growing inside. Scientists also need to continue to look at genes expressed by tumors and the proteins expressed by those genes to get the bigger picture. “It’s basically a systems approach you need to take,” he says.
The young scientist has worked with all those pieces in his relatively short career. He started his postdoctoral fellowship at the University of Michigan in1999, when the ability to look at gene expression was new. With his mentor, Dr. Arul M. Chinnaiyan, director of Michigan Center for Translational Pathology, Pathology Research Informatics and Cancer Bioinformatics at Michigan, he helped develop the next step: the ability to look at expression of hundreds of proteins at a time, instead of a handful, an important advance in light of the fact that there are about 1 million proteins. Recently they were among the first to venture into the world of metabolites, which are made by proteins.
“Previous technology was looking at a cell from a narrow perspective and cells never act in isolation, proteins never act in isolation, they always form complexes, act in pathways,” Dr. Sreekumar says.
His inspiration to follow those pathways is a fellow Ph.D. student who died too young and quickly of an aggressive leukemia and the fact that cancer is a leading cause of death worldwide.
Posted under Cancer Research, ChemInformatics, North America, Proteomics | Comments Off
GTCbio Announces 4th Annual Assay Development and Screening Conference taking place June 8-9, 2009.
Last Updated on Friday, 27 March 2009 09:40 Written by admin Friday, 27 March 2009 09:40
San Francisco, CA – GTCbio Announces its 4th Annual Assay Development and Screening Conference taking place June 8-9, 2009. As compounds derived from high throughput screening increasingly find their way into clinical trials, drug screening has become widely accepted as a critical step in the drug discovery process. After more than a decade of rapid growth, tremendous progress has been made in assay technology, laboratory automation, and informatics. These technological developments have not only facilitated a drastic increase in throughput and efficiency in drug screening, but have also provided novel solutions in other areas of drug discovery and development. As screening has also become prominent in biological research, screening facilities have become increasingly popular in academic institutions.
As the pharmaceutical industry continues to face the challenges of developing more new chemical entities and reducing the cost of R&D, the demand for novel technologies and creative approaches for improving the efficiency of screening has intensified. Cell-based assays used in compound screening and high-content screening technologies have gained popularity in the industry. Years of intensive research have finally resulted in label-free technologies in the drug screening market place. These technologies provide new ways of interrogating cellular and molecular binding events and enable orthogonal screening approaches to drug targets.
The goal of the 4th annual Assay and Screening Technologies Conference is to provide a forum for academics and professionals in the drug discovery industry to stay abreast of exciting new developments in assay technologies while exchanging ideas and developing more efficient approaches to the drug discovery and development process.
For more information, visit http://gtcbio.com/conferenceDetails.aspx?id=123
Posted under Clinical Trials, Compound Screening, Drug Development, HT Screening, North America, Press Releases, USA and Canada | Comments Off
Salk Forms Stem Cell Partnership With Sanofi-Aventis
Last Updated on Friday, 27 March 2009 09:35 Written by admin Friday, 27 March 2009 09:35
The Salk Institute says it has formed a new stem cell research partnership with Sanofi-Aventis, the international pharmaceutical giant based in Paris. Financial terms of the five-year alliance were not disclosed, and some details of the deal remain to be worked out, Salk spokesman Mauricio Minotta told me this afternoon.
The Sanofi-Aventis regenerative medicine program will sponsor grants in promising research areas, and is intended to provide long-term, multi-participant collaborations between scientists at San Diego-based Salk and Sanofi-Aventis. “It’s meant to be a true collaboration, it’s not just funding,†says Michael White, who oversees the institute’s office of technology management and development. Sanofi-Aventis has about 16,000 employees in the United States, mostly at its U.S. headquarters in Bridgewater, NJ, and about 100,000 employees worldwide.
The program also will provide unrestricted support for the Salk Institute’s stem cell facility, which was created as a separate laboratory supported by private funding during the years the Bush Administration had placed restrictions on federal stem cell funding.
In a statement, Salk president William Brody says there are no preconditions concerning the collaborative alliance. “Our scientists will continue to freely explore cutting-edge research and publish their work,†Brody says. (That’s important to academic freedom, because companies have been known to try to squelch research findings if they don’t support the company’s marketing message.) Under this deal, Salk will also gain access to “extensive resources†at Sanofi-Aventis, which includes a large-scale facility in Tucson, AZ, for screening compounds with potential to be new drugs.
“That’s something that’s very attractive to us, to be able to screen our targets with their drugs,â€White says.
Such industry collaborations could be a sign of the times. In January, San Diego’s Burnham Institute for Medical Research announced a multi-year agreement with Johnson & Johnson’s Pharmaceutical Research and Development unit.
Source: xconomy.com
Posted under Collaborations, Compound Libraries, Compound Screening, Europe, North America, Press Releases | Comments Off
Thermo Fisher Scientific Accelerates Drug Discovery Process With New Maybridge Quick2Leadâ„¢ Compound Kits
Last Updated on Friday, 27 March 2009 09:32 Written by admin Friday, 27 March 2009 09:32
Thermo Fisher Scientific, the world leader in serving science, announced recently that it has introduced a novel tool to accelerate hit-to-lead programmes in the drug discovery process. Its Maybridge Quick2Leadâ„¢ Compound Kits are designed to save time and money by enabling rapid compound library synthesis around bioactive “hits” emerging from screening assays. The kits are made up of pre-weighed, diverse building block selections, facilitating rapid capture of structure-activity (SAR) data from the closely related structural analogues within the library.
Quick2Lead Compound Kits are available as five functionality-based kits, with each one containing 48 carefully selected compounds. This enables the exploration of a wide area of chemical space to maximise credible SAR data acquisition for the successful conversion of an initial hit into a genuine, optimisable lead. Since these compounds are all pre-weighed, the kits are ready to use by simply adding solvent and transferring straight to a synthesiser.
The five functional groups available include: carboxylic acids, sulfonyl chlorides, amines, anilines and boronic acids. Each of these different functional groups is applicable to a wide range of tried and trusted parallel synthesis methodologies. Furthermore, although each kit taps into the hugely diverse Maybridge collection, they all include compounds from the top levels of the relevant Topliss Tree, thereby ensuring quality and rigour in interaction testing.
Each of the pre-selected compounds is supplied as 0.1mMol in a 5mL vial. This saves time and money at several levels — minimising stock, avoiding disposal and reducing storage footprint. The pre-selection process also avoids the “dead time” that can be experienced whilst waiting for multiple building blocks from internal and external sources. Maybridge Quick2Lead Kits arrive as a complete library, delivered rapidly ex-stock.
“Our aim with the Maybridge product range is to help shorten the discovery process, from screening to scale-up, and the introduction of our Quick2Lead Compound Kits is the latest addition to our broad product portfolio of pharmacophorically relevant compounds and services,” said Dr. Mick Durrant, Director of Business Development for Maybridge products at Thermo Fisher Scientific. “We recognise that identifying, sourcing and weighing building blocks to feed the library production process around an initial hit can be time consuming and expensive. Our new Quick2Lead Kits offer a novel approach to drive these costs down by providing pre-weighed, diverse building block selections which are simply ready-to-go.”
About Maybridge
Maybridge, part of Thermo Fisher Scientific, is well known for providing highly innovative drug-like molecules and screening compounds for drug discovery and development. With products available for both lab and development scale, they specialise in producing new heterocyclic and phenyl ring-based chemical building blocks, including a unique and expanding range of reactive intermediates.
About Thermo Fisher Scientific
Thermo Fisher Scientific Inc. is the world leader in serving science, enabling our customers to make the world healthier, cleaner and safer. With annual revenues of $10.5B, we have more than 34,000 employees and serve over 350,000 customers within pharmaceutical and biotech companies, hospitals and clinical diagnostic labs, universities, research institutions and government agencies, as well as environmental and industrial process control settings. Serving customers through two premier brands, Thermo Scientific and Fisher Scientific, we help solve analytical challenges from routine testing to complex research and discovery. Thermo Scientific offers customers a complete range of high-end analytical instruments as well as laboratory equipment, software, services, consumables and reagents to enable integrated laboratory workflow solutions. Fisher Scientific provides a complete portfolio of laboratory equipment, chemicals, supplies and services used in healthcare, scientific research, safety and education. Together, we offer the most convenient purchasing options to customers and continuously advance our technologies to accelerate the pace of scientific discovery, enhance value for customers and fuel growth for shareholders and employees alike.
SOURCE: Thermo Scientific Brand Products, Part of Thermo Fisher
Posted under Compound Libraries, Diversity Libraries, Drug-Like Compounds, Europe, New Products, Press Releases | Comments Off
Conference focuses on potential new drugs for malaria, leishmaniasis, and trypanosomiasis
Last Updated on Thursday, 26 March 2009 09:52 Written by admin Thursday, 26 March 2009 09:52
A meeting in Colorado, USA has brought together chemists, biologists, pharmacologists, and clinicians in an attempt accelerate the discovery of new drugs for diseases caused by protozoan parasites. These include some of the major infectious diseases of poverty – malaria, leishmaniasis, human African trypanosomiasis and Chagas’ disease.
The organizers of the meeting, “Drug Discovery for Protozoan Parasites†held 22-26 March, point out that recent years have seen the welcome development of public-private research partnerships focused on diseases caused by protozoa – in most cases on malaria. However, these partnerships have mainly been concerned with translational research. As a result, several drugs have been advanced into clinical evaluation but, in the meantime, development of several apparently promising new drugs has not proved successful, “…thus leaving a sparse pipeline of new chemical entities that have potential for registration in the next few yearsâ€.
The objectives of the meeting were to discuss current methods to identify and validate new drug targets and to screen libraries of compounds to discover novel chemotypes; assess the potential for chemical biology and medicinal chemistry to optimize compounds that are specific and avoid resistance mechanisms; and identify critical paths for compound progression and to discuss the utility of key models for assessing preclinical drug leads.
Key problems addressed included identification and validation of new targets, chemical biology and medicinal chemistry approaches to characterize new compounds, novel screening techniques to identify new chemotypes, mechanisms of drug resistance, and cutting edge strategies to progress new drug candidates into clinical trials.
Several potentially important findings were reported. To give just one example, oral administration of an amphotericin B formulation, iCo-009, has been shown to have significant efficacy with no evidence of toxicity in mice infected with Leishmania donovani. Manufacturers iCo Therapeutics Inc, claim that “iCo-009 has overcome amphotericin B’s significant physicochemical barriers to absorption and holds promise for the development of a self-administered oral therapy for the treatment of visceral leishmaniasisâ€.
The meeting was supported by the Bill & Melinda Gates Foundation.
Posted under Compound Libraries, Compound Screening, Press Releases, USA and Canada | Comments Off
First auto carbohydrate synthesiser
Last Updated on Tuesday, 24 March 2009 12:24 Written by Editor Tuesday, 24 March 2009 12:24
German researchers have unveiled the first fully automated carbohydrate synthesiser, which they hope will advance development of carbohydrate-based vaccines for the developing world.
The new machine was announced at this week’s meeting of the American Chemical Society in Salt lake City, Utah, and could significantly reduce the amount of time it takes for researchers to build complex carbohydrates for vaccine research. Currently, synthesis of multiple carbohydrates for screening causes a bottle neck in efforts to discover new carbohydrate-based vaccines.
‘A chemical synthesis of a single carbohydrate typically takes months to years,’ explains Peter Seeberger from the Max Planck Institute of Colloids and Interfaces, Potsdam. His team has now revealed a next generation synthesiser, building on an earlier partially automated model announced in 2001, that Seeberger says is ‘entirely reliable, very fast and can be operated by somebody with no experience of chemistry at all’. And when he says fast, he means fast: ‘we have repeated a synthesis of a carbohydrate that initially took two years in the lab in less than 20 hours.’ He also claims to have fixed protection and deprotection issues, major hurdles in carbohydrate synthesis, that plagued the earlier version of the synthesiser.
The concept of the machine is very simple, solid phase chemistry. The starting point is a polystyrene bead with a single sugar attached and ‘we add to that one sugar at a time like threading beads on a necklace,’ explains Seeberger. ‘The bead’s only role is to stop the sugar from being dissolved, and using this methodology we can build up chains between six and 15 sugars. The addition of each sugar takes about two hours, meaning that in 1.5 to two days we can make pure, useable quantities of carbohydrates.’ In a single run they can make 25-50mg of carbohydrate. Seeberger also claims that the sugar building blocks can be made easily in 50-100g bulk quantities.
Carbohydrates surround every cell in humans, bacteria and viruses and play a crucial role in the body’s immune response to disease-causing viruses and bacteria. They have been used for medicinal purposes before, including in some blockbuster vaccines used to inoculate small children against bacterial diseases, such as meningitis, explains Seeberger. The current vaccines are based on isolated carbohydrates – meaning drug companies have to grow bacteria, harvest the carbohydrates, isolate mixtures of compounds and put them into a carrier protein – and Seeberger is looking to simplify this process by using carbohydrates that can be chemically synthesised and therefore help drive down the cost of these vaccines.
The 2001 version of his machine was used to develop a carbohydrate-based vaccine for malaria, scheduled to enter clinical trials in 2010. Malaria kills two million children a year in the developing world, explains Seeberger, and ‘we have a cost target of under $1 per child’. Using their technique the team now have ‘approximately 15 carbohydrates that are entering different phases of development for potential clinical purposes such as tuberculosis.’
The price is pretty attractive too – according to Seeberger the machine itself will cost somewhere in the region of $25,000 (£17,000), approximately one quarter the price of the analogous peptide synthesiser owned by most labs.
Geert Jan Boons, University of Georgia, Athens, US, an expert in carbohydrate synthesis, says that this technology is ‘very sophisticated and has great potential’. Explaining that there is nothing similar available, he says ‘most complex carbohydrates are made in solution, and any solid phase chemistry that is done uses manual approaches – where you add the reagents one by one yourself.’ Seeberger’s fully automated system handles everything, including cooling and warming of each step as required, he adds. Boons does however say that he is not entirely convinced that the chemistry is yet robust enough to make every type of carbohydrate, but adds that Seeberger does claim to have fixed these issues in research he is yet to publish. ‘I think the biggest hurdle will be when he tries to make a bigger molecule,’ he explains, adding that the separation of the desired product from its isomeric compounds is another hurdle that needs to be overcome.
Posted under Biotech & Pharma Law, Discoveries, Innovations and Patents, Europe, Events, Industry News, Press Releases, USA and Canada | Comments Off
The French Institute I-Stem Realizes First Innovative Screens Using Stem Cells to Identify Drugs for Myotonic Dystrophy
Last Updated on Friday, 20 March 2009 05:02 Written by Editor Friday, 20 March 2009 05:02
EVRY, France, March 19 /PRNewswire/ –    Four research teams of I-STEM[*] have joined forces in a collaborative project that has just achieved a first pilot therapy-oriented screen of compounds and RNA interference aiming at reversing the altered phenotypes observed in human embryonic stem cells carrying the mutant gene for myotonic dystrophy type1. This assay inaugurates a series of R&D planned in 2009.Human embryonic stem (hES) cells lines carrying the mutant gene responsible for diseases may replicate associated molecular defects associated and be used, therefore, to analyse pathological mechanisms and search for treatments. I-STEM teams have shown that hES cell lines carrying the mutant gene responsible for myotonic dystrophy type1 (DM1) -the most frequent myopathy in adult- present known cellular and molecular abnormalities. hES capacity of self-renewal and pluripotency provides an unlimited and highly versatile cell resource, relevant for large-scale analyses. In order to exploit fully these potentials of hES cell lines within the framework of its exploration of therapeutics for monogenic diseases, I-STEM has set up a screening department through a close partnership with the companies Velocity11, Discngine and Prestwick Chemical. I-STEM has installed at its site, in Evry-Genopole, a powerful automation platform using the innovative Velocity11 BioCel1800(R) technology, coupled to a specific data management system designed by Discngine. The Conseil Régional d’Ile-de-France and the Association Française contre les Myopathies (thanks to the French Telethon donations) co-funded this platform[**]. The investments to build  this facility assays have been developed in order to screen the “FDA  approved” Prestwick Chemical library and a subset of the in house designed  siRNA (small interferent RNA) library.
Using this screening platform, the I-STEM teams have looked for compounds and siRNA that would provoke the disruption of abnormal aggregation seen in the nucleus of human embryonic stem cells carrying the DM1 mutation. Several of the 1120 compounds and 50 siRNA assayed were identified as candidates.
I–STEM intends to perform five to ten similar screening campaigns per year on other genetic diseases, using its library of human stem cell lines carrying genetic mutations[***].
About I-STEM
The Institute for Stem Cells in the Treatment and Study of Monogenic Diseases- is a laboratory which has set out to explore the therapeutic potential of stem cells in the treatment of rare genetic diseases. Headed by Marc Peschanski (an INSERM Research Director), I-STEM was in early 2005, the first lab in France to be allowed to work on (imported) human embryonic stem cell lines. Then, in June 2006, it was authorized by the French Agency for Biomedicine to set up a library of mutated cell lines that can serve as models in the study of monogenic diseases. For more information: http://www.istem.eu
Posted under Collaborations, Compound Screening, Europe, Press Releases, RNA Reasearch, Stem Cell Research | Comments Off
EPA Presents Initial Results from Caliper Life Sciences’ ToxCast Screening Effort
Last Updated on Friday, 20 March 2009 04:59 Written by Editor Friday, 20 March 2009 04:59
HOPKINTON, Mass., March 19 /PRNewswire-FirstCall/ — Caliper Life Sciences, Inc. (NASDAQ: CALP) , a leading provider of tools and services for drug discovery and life sciences research, today announced that the United States Environmental Protection Agency (EPA) presented initial analyses of Phase I data generated by Caliper Discovery Alliances and Services (CDAS) under the EPA’s ToxCast(TM) screening program at the annual meeting of the Society of Toxicology (SOT) held this week in Baltimore, MD. Separately, the EPA notified Caliper that it has exercised the first additional option year under Caliper’s ToxCast contract with the EPA. Task orders under this contract have already generated approximately $3.5 million in total revenues for Caliper since the initiation of the contract in April, 2007, $1.2 million of which was recognized in 2008.
“We are pleased with the preliminary findings presented by the EPA,” said Kevin Hrusovsky, President and CEO of Caliper Life Sciences. “These results, coupled with the EPA’s third year option exercise, reinforce the likelihood for Phase II efforts to begin at Caliper in the third quarter of this year, which supports our expectation of receiving approximately $3 million of service task orders under this contract in 2009.”
Caliper works with the EPA under its ToxCast initiative to develop new in vitro (laboratory) approaches to identify chemicals that are potentially toxic to the environment. The initial phase of the EPA ToxCast program was aimed at creating a database of in vitro assay data on a broad set of compounds for which in vivo (animal) safety data already existed. Key goals for this phase were to assess overall data quality and establish that the database was predictive of in vivo toxicity profiles. Initial analyses of the data generated at CDAS indicate that the goals for high quality data and potential predictive power have been met. For the 11 replicate controls included in the initial 320 compound set, there was greater than 99% concordance in the screening results across 240 assays tested, and more than 200 correlations between the in vitro results generated at CDAS and in vivo toxicity parameters have already been identified. In addition, 75% of the assays tested showed activity for one or more compounds, reinforcing the need for broad in vitro profiling.
“We believe this data presentation validates the importance of in vitro profiling as a tool for predicting potential toxicity liabilities of compounds and highlights the high quality data generated by Caliper,” said David Manyak, Ph.D., Executive Vice President of Discovery Services at Caliper Life Sciences. “Our access to the entire Phase I ToxCast database makes Caliper an ideal partner for collaborative data mining projects. We also believe that the assay screening panel employed by Caliper for the ToxCast initiative will be broadly applicable for product development programs within the agricultural chemical and pharmaceutical industries.”
The ultimate goal of the ToxCast program is to develop a set of predictive in vitro assays that can supplement or replace in vivo tests currently used for regulatory approval of new environmental chemicals. If successful, the ToxCast initiative will reduce the cost and improve the speed of regulatory approval of new environmental chemicals. More extensive data analysis from the EPA is expected in mid-May of this year.
About Caliper Life Sciences
Caliper Life Sciences is a premier provider of cutting-edge technologies enabling researchers in the life sciences industry to create life-saving and enhancing medicines and diagnostic tests more quickly and efficiently. Caliper is aggressively innovating new technology to bridge the gap between in vitro assays and in vivo results and then translating those results into cures for human disease. Caliper’s portfolio of offerings includes state-of-the-art microfluidics, lab automation & liquid handling, optical imaging technologies, and discovery & development outsourcing solutions. For more information please visit www.caliperLS.com.
Posted under Clinical Trials, Compound Libraries, North America, Press Releases | Comments Off
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 20 March 2009 04:54 Written by Editor Friday, 20 March 2009 04:54
BERKELEY, Calif.–(BUSINESS WIRE)–Plexxikon Inc. today announced the issuance of key composition-of-matter patents covering novel compounds discovered through the company’s Scaffold-Based Drug Discoveryâ„¢ platform. Plexxikon’s pipeline of preclinical and clinical stage product opportunities currently span potential treatments for cardio-renal disease, CNS disorders, inflammation, metabolic disease and oncology. Two of the three recently issued patents (U.S. patents no. 7,498,342 and no. 7,504,509) cover compounds derived from the company’s discovery efforts to target protein kinases for the treatment of multiple indications including oncology and inflammation. The third patent (U.S. patent no. 7,476,746) covers novel compounds from the company’s PPAR (peroxisome proliferator-activated receptor) program yielding novel therapeutic opportunities for metabolic disorders and other diseases.
“We are pleased to be adding these additional patents to our growing and broad intellectual property portfolio,†stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “Plexxikon’s novel approach to drug discovery has enabled the company to advance multiple first-in-class drug candidates which are covered by strong intellectual property, and as a result, to secure significant pharmaceutical industry interest in our programs.â€
In contrast to fragment-based approaches, Plexxikon’s platform has generated multiple product opportunities by mining the relatively unexplored chemical space of scaffold-like cores and by utilizing co-crystallography early in the discovery process to guide chemical optimization of these scaffolds. Further, the company has developed methods to make highly selective kinase inhibitors as yet rarely seen. Plexxikon has demonstrated the ability to develop selectivity between two targets with as little as one amino acid difference in their catalytic domains. This capability has created the opportunity for the development of new targeted drugs not only for oncology, but also for chronic disease indications outside oncology where safety hurdles are even higher. To date, Plexxikon’s platform has led to the development of a targeted medicine for the treatment of melanoma, a drug candidate for polycystic kidney disease (PKD), an oral agent for rheumatoid arthritis and a broad spectrum oral diabetic therapeutic, all representing novel agents addressing significant unmet needs.
Dr. Prabha Ibrahim Promoted to Vice President of Chemistry
In other news, Prabha N. Ibrahim, Ph.D., was promoted to the position of vice president of chemistry, bringing over 15 years of experience to her position. As head of chemistry since 2002, she has played a key role in building the company’s synthetic and medicinal chemistry capabilities leading to the discovery of Plexxikon’s novel drug candidates now in the clinic and in preclinical development. Prior to Plexxikon, Dr. Ibrahim was a senior scientist at CV Therapeutics, where she was responsible for the identification and development of preclinical candidates for cardiovascular indications. She also previously worked at Amgen, where she played an integral role in small molecule drug discovery for inflammation therapeutics. Dr. Ibrahim earned her Ph.D. at the University of Victoria, Canada, and was a Welch Foundation Fellow at Rice University in Houston.
Plexxikon Profile
Plexxikon is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s clinical stage programs include PLX4032 for the treatment of melanoma and colorectal cancer, PLX5568 for the treatment of PKD and PLX204 for the treatment of diabetes. Among the company’s preclinical development programs, candidates are being developed for the treatment of rheumatoid arthritis, multiple sclerosis and other autoimmune diseases.
Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform is being applied to build a pipeline of product opportunities in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in varied disease areas addressing significant unmet needs in each therapeutic category.
Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.
Posted under Clinical Trials, Compound Screening, Discoveries, Innovations and Patents, Drug-Like Compounds, North America, Press Releases, Targeted Libraries | Comments Off
Thermo Fisher Scientific Accelerates Drug Discovery Process with New Maybridge Quick2LeadT Compound Kits
Last Updated on Thursday, 19 March 2009 01:17 Written by Editor Thursday, 19 March 2009 01:17
TINTAGEL, England, (17 March 2009) – Thermo Fisher Scientific, the world leader in serving science, announced today that it has introduced a novel tool to accelerate hit-to-lead programmes in the drug discovery process. Its Maybridge Quick2Lead™ Compound Kits are designed to save time and money by enabling rapid compound library synthesis around bioactive “hits†emerging from screening assays. The kits are made up of pre-weighed, diverse building block selections, facilitating rapid capture of structure-activity (SAR) data from the closely related structural analogues within the library.
Quick2Lead Compound Kits are available as five functionality-based kits, with each one containing 48 carefully selected compounds. This enables the exploration of a wide area of chemical space to maximise credible SAR data acquisition for the successful conversion of an initial hit into a genuine, optimisable lead. Since these compounds are all pre-weighed, the kits are ready to use by simply adding solvent and transferring straight to a synthesiser.
The five functional groups available include: carboxylic acids, sulfonyl chlorides, amines, anilines and boronic acids. Each of these different functional groups is applicable to a wide range of tried and trusted parallel synthesis methodologies. Furthermore, although each kit taps into the hugely diverse Maybridge collection, they all include compounds from the top levels of the relevant Topliss Tree, thereby ensuring quality and rigour in interaction testing.
Each of the pre-selected compounds is supplied as 0.1mMol in a 5mL vial. This saves time and money at several levels — minimising stock, avoiding disposal and reducing storage footprint. The pre-selection process also avoids the “dead time†that can be experienced whilst waiting for multiple building blocks from internal and external sources. Maybridge Quick2Lead Kits arrive as a complete library, delivered rapidly ex-stock.
“Our aim with the Maybridge product range is to help shorten the discovery process, from screening to scale-up, and the introduction of our Quick2Lead Compound Kits is the latest addition to our broad product portfolio of pharmacophorically relevant compounds and services,†said Dr. Mick Durrant, Director of Business Development for Maybridge products at Thermo Fisher Scientific. “We recognise that identifying, sourcing and weighing building blocks to feed the library production process around an initial hit can be time consuming and expensive. Our new Quick2Lead Kits offer a novel approach to drive these costs down by providing pre-weighed, diverse building block selections which are simply ready-to-go.â€
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PerkinElmer Announces Collaboration with Korea’s Sangmyung University for Drug Discovery Research
Last Updated on Thursday, 19 March 2009 01:14 Written by Editor Thursday, 19 March 2009 01:14
WALTHAM, Mass. & CHEONAN, South Korea–(BUSINESS WIRE)–PerkinElmer, Inc., a global leader focused on the health and safety of people and the environment, today announced that it has entered into a drug discovery research collaboration with Sangmyung University (Republic of Korea), based on applying PerkinElmer’s AequoScreen® aequorin assay technology to cutting-edge G-protein coupled receptor (GPCR) research.
It is estimated that GPCRs are associated with at least 30% percent of addressable diseases, and continue to be a key focus in drug discovery. Aequorin assays are a sensitive and flexible cell-based assay technology used to detect GPCR activation with several advantages over conventional fluorescence based dyes, including fewer false positives, much simpler protocol and significantly increased assay windows.
AequoScreen will be used by Sangmyung University as part of its efforts to establish an academic GPCR screening facility together with the Korea Chemical Bank, a national repository library of over 100,000 small molecule compounds. The aequorin technology will be used as part of nationwide GPCR screening campaigns and drug discovery programs in Korea.
“We are very pleased to be working with the distinguished faculty of Sangmyung University in providing our AequoScreen technology in support of their Korea-wide GPCR screening campaign implementation,†said Richard M. Eglen, Ph.D., president, Bio-discovery, PerkinElmer, Inc. “Given the wide range of potential drug targets linked to GPCR research, the University’s project presents tremendous promise in terms of advancing potential new drugs.â€
According to Professor Sunghou Lee, Ph.D., of the Department of Biomedical Technology at Sangmyung University, “Screening programs have begun to increase in Korea, partly through the support of institutions such as the Center for Biological Modulators (CBM), the Frontier R&D Program for drug discovery research. For a nationwide academic screening research laboratory such as ours, the ability to reliably and accurately deploy a sensitive, flexible and easy-to-use GPCR detection platform like AequoScreen is of prime importance. This is especially true when dealing with small molecules, where conventional technologies such as fluorescence techniques tend to result in issues such as artifacts and interference that distort results.â€
Professor Lee added, “We are delighted to be working with a partner of PerkinElmer’s caliber in this effort, and look forward to compelling results in our screening program.â€
Posted under Asia, Biotech & Pharma Law, Collaborations, Events, Industry News, Press Releases, USA and Canada | Comments Off
New Report Further Demonstrates Ultra-Gloâ„¢ Luciferase is Less Susceptible to Compound Interference
Last Updated on Thursday, 19 March 2009 01:12 Written by Editor Thursday, 19 March 2009 01:12
Research results just published in the Journal of Medicinal Chemistry demonstrate the superior performance of Promega Ultra-Gloâ„¢ Luciferase. The research, conducted by the NIH Chemical Genomics Center (NCGC), describes Ultra-Glo recombinant luciferase as approximately 90% less susceptible to small molecule inhibition compared to another commercially available luciferase. The NCGC is leading the US government-sponsored efforts aimed at developing biological probes and expanding the use of HTS assays in academic settings.The studies reveal why most screeners prefer Ultra-Glo as the luciferase enzyme formulation in their screening and profiling regimens. Ultra-Glo was derived by directed evolution and is the key component in Kinase-Glo Assay and a suite of other bioluminescent assays for high throughput screening and profiling of small molecule compound libraries.
At the 2007 SBS meeting in Montreal, Dr. Mohammed Kashem from Boehringer Ingelheim Pharmaceuticals, first reported similar findings when he compared Kinase-Glo and a second commercially available ATP-detection luminescent reagent for tolerance to interference by compounds in the BI screening deck. When asked to comment on the NCGC findings, Dr. Kashem replied, “The findings of Auld et al. are consistent with ours (Kashem et al., SBS 2007 Poster #PST1C016) that Kinase-Glo is much less prone to interference from library compounds than PKLight reagent, making it a superior ATP-detection reagent for identifying small-molecule modulators of kinases by HTS”.
Promega Corporation is a leader in providing innovative solutions and technical support to the life sciences industry. The company’s 2,000 products enable scientists worldwide to advance their knowledge in genomics, proteomics, cellular analysis, molecular diagnostics and human identification. Founded in 1978, the company is headquartered in Madison, WI, USA with branches in 14 countries and over 50 global distributors
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BIO-Europe Spring 2009 Presenter and Exhibitor Profiles
Last Updated on Friday, 13 March 2009 01:34 Written by Editor Friday, 13 March 2009 01:34
Company: Addex Pharmaceuticals Ticker Symbol & Exchange: ADXN Media Contact: Chris Maggos Phone:41 22 884 15 11
E-mail: chris.maggos@addexpharma.com Web: www.addexpharma.com Addex Pharmaceuticals discovers and develops allosteric modulators for human health. Allosteric modulators are a different kind of orally available small molecule therapeutic agent, which we believe will offer patients better results than classical drugs. The lead product in our pipeline, ADX10059, has achieved clinical proof of concept and is in Phase IIb testing for the treatment of GERD (e.g. heartburn) and, separately, migraine headache. ADX10059 is a first-in-class mGluR5 inhibitor, a therapeutic strategy that also is being pursued for multiple indications by large pharma competitors. ADX10059 is not yet partnered but we have established drug development deals with Merck & Co., Inc. (2 deals: schizophrenia & Parkinson's) and Ortho McNeil Pharmaceuticals, a J&J company (anxiety/schizophrenia). Roche Ventures and SR One (GlaxoSmithKline's VC investing unit) have invested in Addex. Company: Allon Therapeutics Inc. Ticker Symbol & Exchange: TSX:NPC Media Contact: Aaron Keay, Director, Investor Relations Phone:
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EPIX Pharmaceuticals Achieves Milestone from Collaboration with Cystic Fibrosis Foundation Therapeutics
Last Updated on Friday, 13 March 2009 01:31 Written by Editor Friday, 13 March 2009 01:31
LEXINGTON, Mass.–(BUSINESS WIRE)–Mar 11, 2009 – EPIX Pharmaceuticals, Inc. (NASDAQ:EPIX), a biopharmaceutical company focused on discovering and developing novel therapeutics through the use of its proprietary and highly efficient in silico drug discovery platform, today announced that it has achieved another milestone in its collaboration with Cystic Fibrosis Foundation Therapeutics, Inc. (CFFT), the nonprofit affiliate of the Cystic Fibrosis Foundation. Under the terms of the collaboration EPIX has earned an additional $500,000, bringing the total amount of milestone payments achieved under this collaboration to $5 million. The milestone payment is part of a research, development and commercialization agreement between EPIX and CFFT that focuses on discovering potential drug therapies targeting the Cystic Fibrosis Transmembrane conductance Regulator (CFTR) ion channel. Under the terms of the agreement, EPIX will own all worldwide rights to any compound that results from the collaboration.To earn the milestone, EPIX successfully completed in silico high throughput screening at four distinct sites in the delta F508 mutational form of CFTR for small molecules that may correct the defects in the mutation’s cellular processing and chloride channel gating. The delta F508 is the most common mutation of the key protein associated with cystic fibrosis. EPIX and CFFT believe that ligands to CFTR may act as molecular chaperones, stabilizing the folded structure and modulating CFTR activity.
“We continue to make progress in our collaboration with CFFT and believe that our research may eventually lead to significant advances in the treatment of cystic fibrosis,†said Elkan Gamzu, Ph.D., president and chief executive officer of EPIX. “This achievement, coupled with our announcement in September 2008 regarding the identification of dual-acting compounds that act as both potentiators and correctors, moves us one important step closer to lead optimization and the identification of clinical candidates.â€
Early in the collaboration, EPIX became the first company to generate a 3-D model of the CFTR, a considerable step forward in the CF research field. All of these milestones resulted from EPIX’s highly efficient discovery platform which integrates proprietary in silico modeling techniques with hypothesis-driven approaches for the design and synthesis of compounds.
“Our collaboration with EPIX continues to yield important scientific advances in the field of cystic fibrosis research,†added Robert J. Beall, Ph.D., president and chief executive officer of Cystic Fibrosis Foundation. “This is the first time that a 3-D model has been used to test for compounds that may bind to multiple sites on the CFTR and play a key role in a future treatment for CF. We are pleased with the tangible results stemming from our relationship with EPIX and we look forward to continuing our work together as we focus on our goal of creating new therapies to treat CF.â€
Cystic fibrosis (CF) is a life-threatening genetic disease that affects approximately 30,000 children and adults in the United States and nearly 70,000 people worldwide. It causes life-threatening lung infections and serious digestive complications. A mutation in the CFTR gene is one of the key factors that ultimately leads to the symptoms, complications and premature mortality in people with CF.
Posted under Biotech & Pharma Law, Collaborations, Events, Industry News, News by Region, North America, Press Releases, USA and Canada | Comments Off
10-K: ALEXZA PHARMACEUTICALS INC.
Last Updated on Friday, 13 March 2009 01:29 Written by Editor Friday, 13 March 2009 01:29
he following Management’s Discussion and Analysis of Financial Condition and Results of Operations contains forward-looking statements that are based upon current expectations. In some cases, you can identify forward-looking statements by terminology such as “may,” “will,” “should,” “expect,” “plan,” “anticipate,” “believe,” “estimate,” “predict,” “intend,” “potential” or “continue” or the negative of these terms or other comparable terminology. Forward-looking statements involve risks and uncertainties. Our actual results and the timing of events could differ materially from those discussed in our forward-looking statements as a result of many factors, including those set forth under “Risk Factors” and elsewhere in this Annual Report on Form 10-K.
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Waters Corporation Continues to Meet Today’s Challenges for Improved Laboratory Operations with New Products at Pittcon 2009
Last Updated on Friday, 13 March 2009 01:26 Written by Editor Friday, 13 March 2009 01:26
Waters Gives Scientists, Business and Laboratory Managers More of What They Want: Efficiency, Data Quality, Productivity and Profitability
CHICAGO, March 9 /PRNewswire-FirstCall/ — Against a backdrop of a worldwide economic recession, Waters Corporation (NYSE: WAT) is demonstrating how its industry-leading analytical instruments and informatics products address today’s greatest scientific and business challenges at the 60th Pittsburgh Conference (Pittcon) on Analytical Chemistry and Applied Spectroscopy, March 8 – 13, 2009.
“Pittcon 2009 promises to be like no other in its past simply because today, the stakes are higher,” said Dr. Rohit Khanna, Vice President of Worldwide Marketing, Waters Division. “In no uncertain terms, our customers are telling us they need to achieve more: more productivity, more efficiency, and more speed in all of their efforts. ACQUITY UPLC and Xevo MS systems, combined with Waters informatics and consumable chemistries, are responding to the full range of current laboratory challenges through unrivalled performance and proven reliability to truly redefine the analytical process.”
Waters’ headline offerings at Pittcon 2009 include the Xevo(TM) family of mass spectrometers, the Xevo TQ and Xevo QTof MS Systems, and an expanded suite of products for UltraPerformance LC(R) (UPLC(R)) aimed at bringing laboratories new levels of efficiencies. Additionally, Waters shares the spotlight with its latest technology addition, supercritical fluid chromatography (SFC), by featuring products from TharSFC at the exhibition.
Xevo Family of Mass Spectrometers – Bringing the Power of Advanced MS to More Scientists
With Xevo benchtop mass spectrometers, Waters is making advanced-performance MS more accessible than ever — regardless of who uses the instrument. Xevo mass spectrometers are designed around the philosophy of Engineered Simplicity(TM) which combines outstanding instrument performance with simplicity enabled by IntelliStart(TM) technology to allow scientists to convert data into business-critical knowledge faster and with greater assurance.
New to Pittcon this year, Waters(R) Xevo quadrupole time-of-flight (QTof) mass spectrometer (MS) is an exact mass MS/MS benchtop instrument that is the most sensitive benchtop QTof system ever developed. Paired with Waters ACQUITY(R) UPLC system, the Xevo QTof MS is the only commercially-available MS system to give scientists one-of-a-kind UPLC/MS(E) performance – a novel method of data acquisition that captures “all of the data all of the time” at unparalleled speeds to maximize the amount of information collected from minimal sample amounts.
Also new to Pittcon is the Waters Xevo TQ MS System, an advanced tandem quadrupole mass spectrometer that tackles the most demanding quantification applications for target compounds at low concentrations in highly complex and diverse samples. Waters Xevo TQ MS System is uniquely qualified to allow laboratories to conform to the new US Food and Drug Administration’s guidelines for bioanalytical method validation. The intent of the guidance is to prevent errors due to matrix effects made during the toxicological assessment of a target compound or its metabolites; errors than can have life-threatening consequences during clinical trials.
With the Xevo family of mass spectrometers, Waters is combining advanced performance with ease-of-use to answer the need for laboratories to get more out of their investment in analytical technology.
“According to our customers, the effects of the world’s economic, resource and globalization challenges are felt in the laboratories as much as any other part of an organization’s mission-critical operations,” said Brian Smith, Vice President of Mass Spectrometry Operations for the Waters Division. “These challenges put even greater burdens on labs to answer complex questions faster with greater confidence using fewer resources than ever before. Consequently, today’s laboratory technology should be measured on its ability to improve lab productivity and decision-making if our customers are to be successful.”
UPLC Technology – Changing the Analytical Laboratory Since 2004
Five years ago at Pittcon 2004, Waters sparked a wave of innovation in analytical chemistry when it introduced its ACQUITY UPLC System, an entirely new category of liquid chromatograph based on novel, patented sub two-micron chromatography particles that has transformed the analytical laboratory in many ways.
“The introduction of the Waters ACQUITY UPLC system in 2004 was more than an innovative product introduction, it spurred a revolution in high performance liquid chromatography,” remarks Larry Schmid, President, Strategic Directions International, Los Angeles, California, consultants and advisors to the analytical instrument industry and publishers of Instrument Business Outlook newsletter. “ACQUITY UPLC inspired most other major HPLC suppliers to develop similar systems that have changed the dynamics of liquid separation in the lab, especially in relation to mass spectrometry sample introduction. The ACQUITY UPLC and other so-called “fast LCs” provide greatly improved resolution and faster analysis, something laboratory scientists desperately needed. So five years on, the HPLC marketplace is now fundamentally different thanks to Waters’ groundbreaking product development effort.”
Since its introduction, Waters has installed thousands of UPLC systems, and the thousands of laboratories that have replaced HPLC with UPLC and as an inlet to mass spectrometers are enjoying the benefits.
“The speed that we’re getting is incredible and in our business, speed is money. We’re a production lab so we don’t have time to wait around or run samples overnight and pick up the results in the morning. Now I can run ACQUITY in one shift, get my results, and release the product–all in one day. This is a huge gain in productivity for us,” says Steve Lunetta, Manager, Quality Control Laboratory, PharmaVite LLC, San Fernando, California, the makers of Nature Made(R) brand vitamins and nutritional supplements.
A Newly Enhanced UPLC Product Portfolio
Marking the fifth anniversary of its launch, Waters has expanded its award-winning UPLC product portfolio and will have its entire complement of UPLC products on display during Pittcon 2009, March 8 – 13 in Chicago. They include the nanoACQUITY UPLC(R) system for life science applications; the PATROL(TM) UPLC Process analyzer, an at-line version for process monitoring; numerous compatible LC and quadrupole mass detectors; compatible high-performance triple, tandem, and quadrupole time-of-flight/ion mobility research-grade mass spectrometers; more than 50 column configurations and chemistries including newly-redeveloped ACQUITY UPLC columns, the result of Waters Designed for Six Sigma (DFSS) quality process; the TRIZAIC(TM) UPLC System with nanoTile(TM) Technology designed to deliver exceptional sensitivity for limited-sample, direct-flow, nanoscale protein separations; a new hand-held controller for managing system operations; and applications-specific UPLC/MS and UPLC/MS/MS system solutions for food safety, amino acid, intact protein, oligonucleotide, peptide, metabolite profiling, bioanalysis, impurity profiling, ADME screening, and proteomics analyses.
UPLC for At-Line Process Analysis
Designed with the same enabling technology platform as Waters ACQUITY UPLC System, PATROL UPLC Process Analyzer moves existing liquid chromatography (LC) analysis from off-line Quality Control (QC) laboratories directly to the manufacturing floor resulting in significant improvements in production efficiency with real-time analysis, reducing both process cycle times and assuring product quality.
At Pittcon 2009, Waters is introducing the PATROL UPLC Process Analyzer for at-line analysis to complement the on-line version introduced at Pittcon 2008.
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Last Updated on Tuesday, 10 March 2009 12:24 Written by Editor Tuesday, 10 March 2009 12:24
CHICAGO – (Business Wire) Agilent Technologies Inc. (NYSE:A) today introduced major enhancements to its flagship gas chromatography (GC) line that enable users to run more samples and increase performance with challenging samples at lower cost. The second generation of Agilent’s HPLC-Chip/MS is also making its debut here, offering double the life of existing HPLC-Chips. In addition, Agilent announced a Cooperative Research and Development Agreement (CRADA) with the U.S. Environmental Protection Agency (EPA) to study perfluorinated compounds in the environment.“Analytical labs need to run more samples in less time without sacrificing quality, and Agilent has always responded with breakthrough GC designs,†said Shanya Kane, Agilent vice president and general manager, Gas Chromatography Systems and Workflow Automation. “Today we’re announcing just the latest examples of a long history of Agilent innovations helping GC customers maximize the value of their instrument investments.â€
Agilent Introduces 7693A Series GC Automated Liquid Sampler (ALS)
The 7693A ALS is a completely new design, offering substantial gains in throughput, flexibility, sample preparation automation and serviceability for all current Agilent benchtop GC models. The new ALS is modular, letting users configure the exact autosampler they need – starting from a basic injector with a 16-sample turret, and later adding capabilities as needs expand. Options include a second injection tower, a 150-vial sample tray and a vial heater/mixer/barcode reader for long unattended operation.
Agilent’s exclusive fast-injection technology is twice the speed of any competitive ALS. Injection time of less than 100 milliseconds minimizes sample degradation and the effects of needle discrimination. The two-injector configuration doubles sample throughput.
Agilent offers an optional Heater/Mixer/Barcode Reader module that can automate a number of pre-injection procedures. This offers substantial savings in time and labor, and operator-to-operator variability is eliminated. Solvent consumption and waste expense can be trimmed by as much as 90 percent.
New Multimode GC Inlet Delivers Higher Performance at Lower Cost
Agilent also introduced the Multimode GC inlet with split, splitless and programmable temperature vaporization (PTV) capability, costing approximately $2,500 less than the previous version and featuring much lower maintenance requirements.
Temperature programming capability facilitates a wide range of injection volumes, analysis of thermally unstable samples and better productivity through fewer sample-preparation steps. The new inlet incorporates Agilent’s Turn-Top feature, which allows liners to be changed in seconds without special tools or training.
A major benefit of PTV is the ability to inject high matrix samples with little or no cleanup into a GC or GC/MS. Productivity is enhanced and maintenance is further reduced when this is combined with the backflush function available with the Agilent 7890A GC and 5975C GC/MS.
“Dirty†samples can be injected into the GC or GC/MS. When the compounds of interest have reached the detector, gas flow is reversed in the precolumn, where the high boiling compounds are flushed out of it and the inlet before they reach the analytical column. The results are longer column life and reduced maintenance requirements. The new inlet shares common liners, septa, ferrules, nuts and o-rings with the standard inlet, eliminating the need to stock special parts.
World’s Most Inert Capillary GC Column Line Expanded
Agilent announced the addition of Agilent J&W DB-1ms and HP-1ms Ultra Inert columns to the industry’s most inert family of capillary GC columns, Agilent J&W Ultra Inert Capillary GC columns. The superior and consistent inertness of these columns allows for trace-level analysis of active compounds, such as acids and bases, with high confidence. This new chemistry is particularly well suited for applications such as fragrance fingerprinting, analysis of pesticides and drugs of abuse, and unknown sample screening.
“We’re raising the bar for GC column performance with reactive samples, and the excellent peak shapes these columns produce give our customers high confidence in the results,†said Helen Stimson, Agilent vice president and general manager, Consumables and Supplies Division.
Next-Generation HPLC-Chip for MS has Double the Life Expectancy
Agilent also unveiled the Agilent 1200 Series HPLC-Chip II, the second generation of its pioneering high-performance nano liquid chromatography/electrospray system for mass spectrometry. The new chip platform is designed to provide greater than two times the life of the original HPLC-Chip.
Agilent added proprietary Ion Implantation (II) technology to the new HPLC-Chips, extending life expectancy beyond 1,000 injections, depending on the application. The main benefits are lower cost-per-experiment and enhanced chip-to-chip and run-to-run reproducibility. The carbon ion implanted filter dramatically improves characteristics of polyimide surfaces as well as reduces friction between the rotary valve and the chip body for longer life.
Initially, the Agilent HPLC-Chip II is available in a phosphopeptide chip (for post-translational modifications), the large-capacity protein ID chip, and the ultra-high-capacity chip. HPLC-Chip II technology will be extended across the entire HPLC-Chip family in coming months. Agilent now offers 12 versions of HPLC-Chips, plus custom versions. All Agilent HPLC-Chips are compatible across the entire portfolio of Agilent mass spectrometers.
Agilent, U.S. EPA Collaborate to Study Perfluorinated Compounds
Agilent today announced it has entered into a Cooperative Research and Development Agreement (CRADA) with the National Exposure Research Laboratory of the U.S. EPA to use the Agilent time-of-flight mass spectrometer (TOF-MS) to detect and identify both known and unknown perfluorinated compounds (PFCs) in the environment.
The study of perfluorinated organic compounds in the environment has increased recently as a result of continued studies that indicate their distribution, persistence and toxicity in the environment and biological systems. The collaborative efforts between the National Exposure Research Laboratory (NERL) and Agilent will focus on identifying PFOS and PFOA (perfluorooctanesulfonic acid and perfluorooctanoic acid – both used in a variety of commercial products) isomers and related compounds while characterizing their environmental distributions and the potential pathways for human exposure.
The Agilent 6220 Accurate Mass TOF used in this CRADA will help EPA detect and identify compounds in part-per-trillion range. This capability, along with Agilent MassHunter software, is well suited for detecting and identifying very small amounts of unknown compounds.
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Flavor/Fragrance Ingredients in the Works
Last Updated on Tuesday, 10 March 2009 12:21 Written by Editor Tuesday, 10 March 2009 12:21
DORTMUND, Germany and MILAN—The joint research efforts of InterMed Discovery (IMD) and Axxam SpA have resulted in a technology platform that offers screening solutions and the discovery of natural bioactive compounds valuable to companies in the food, beverages, flavor and fragrance industries.
Based on that success, the companies signed a second joint research agreement that will focus on discovery and validation of flavor/fragrance functional ingredients, which will then be offered to food, beverages, flavor and fragrance companies. The proprietary compounds will have clearly defined activity profiles and naturally derived chemical properties.
“This cooperation is a direct response to what we see as growing market needs,†said Dr. Thomas Henkel, managing director of InterMed Discovery. “Our innovative approach to developing natural functional ingredients together with Axxam caters perfectly to the increasing market demand for turnkey solutions.â€
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Zenobia Therapeutics, Inc. Announces Sale of Commercial Fragment Library Ideal for Crystallographic, NMR and SPR Screening
Last Updated on Tuesday, 3 March 2009 03:53 Written by Editor Tuesday, 3 March 2009 03:53
LA JOLLA, Calif., March 2 /PRNewswire/ — Zenobia Therapeutics, Inc. (Zenobia) the leader in fragment-based lead discovery (FBLD) for CNS diseases, announced today that they are adding a 352 compound fragment library to their product offerings. The library is ready for screening by X-ray, NMR, and SPR methods, contains soluble, verified protein binders, is shape and functionally diverse, and has an average molecular weight of 155 Da. The compounds are pre-plated and will initially cost ~ $11/compound. The library was constructed by Zenobia’s team of seasoned FBLD professionals with over 25 years combined experience. Vicki Nienaber, Ph.D., President, CSO and founder of Zenobia, reported the first fragment-based crystallographic screening method in 2000.
“Over the past decade, FBLD has become a successful drug discovery method that has produced many NCEs and clinical candidates. We want FBLD to continue to positively impact drug discovery and are now providing a solid, simple starting point for fragment-based screening campaigns,” said Dr. Nienaber. “A great deal of the chemical space of drug-like molecules can be covered by a well chosen set of small fragment compounds. This efficient library design will provide researchers with a lot of information on target site binding within a small number of experiments,” said John Badger, Ph.D., Director of Structural Biology. The library has been examined by Dr. Ruo Steensma, Ph.D., Director of Chemistry for Zenobia Therapeutics. Dr. Steensma took forward two programs to IND using FBLD during her tenure as Director of Medicinal Chemistry at SGX Pharmaceuticals. “This is a perfect starting point for scientists interested in FBLD. The compounds are simple and ideally suited as starting points for further analoging. We look forward to working with fellow scientists who are interested in getting quality leads through this approach,” said Dr. Steensma. Co-founder of Zenobia, Robert Meadows, Ph.D., a co-inventor of the SAR by NMR method who has designed multiple fragment libraries for the NMR screening method says, “Zenobia’s library is a small, cherry picked selection of diverse chemotypes and shapes. And, since the compounds are all very soluble, screening with different methods is straightforward. Most importantly, once you find a hit with this library, developing the SAR is fast and economical.” Through consulting or collaborations, Zenobia offers its expertise in advancing SAR around fragment hits.
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