Bio Screening Industry News

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 Discovery™ 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.”

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.

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.

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

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,”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

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 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.”

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

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 years”.

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 leishmaniasis”.

The meeting was supported by the Bill & Melinda Gates Foundation.

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.

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

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.

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 Discovery™ 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.”

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.