Bio Screening Industry News

Archive for the 'Compound Screening' Category

March 27, 2009

GTCbio Announces 4th Annual Assay Development and Screening Conference taking place June 8-9, 2009.

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

Salk Forms Stem Cell Partnership With Sanofi-Aventis

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

March 26, 2009

Conference focuses on potential new drugs for malaria, leishmaniasis, and trypanosomiasis

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.

March 20, 2009

The French Institute I-Stem Realizes First Innovative Screens Using Stem Cells to Identify Drugs for Myotonic Dystrophy

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

Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs

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.

December 12, 2008

CytRx Unveils Clinical Development Plan for Pipeline Assets

Names World-Renowned Cancer Drug Expert Dr. Joseph Rubinfeld as Chief Scientific Advisor

LOS ANGELES–(BUSINESS WIRE)–CytRx Corporation (NASDAQ: CYTR) today unveiled its corporate strategy to focus its internal resources on the clinical development of oncology drug candidates tamibarotene and INNO-206, which the Company believes offer the greatest mix of near-term and medium-term revenue potential among its clinical assets. CytRx will pursue partnerships to advance the clinical development of INNO-406 (bafetinib) and its clinical molecular chaperone portfolio, where it continues to see significant future revenue potential. The Company further intends to use its proprietary high-throughput, high-content drug screening Master Chaperone Regulator Assay (MaCRA) platform to discover additional molecular chaperone drug candidates, including those that may inhibit cancer growth, which will support internal efforts to build an oncology drug franchise or future out-licensing possibilities.

CytRx also announced that Board of Directors’ member Dr. Joseph Rubinfeld has accepted the additional responsibility of Chief Scientific Advisor, and will consult on all aspects of the Company’s oncology development programs while serving as an important interface between the Company and investors, clinicians and industry thought leaders. Dr. Rubinfeld brings substantial expertise in oncology and drug development through his distinguished career. Dr. Rubinfeld was employed at Bristol-Myers Company International Division as Vice President and Director of Research and Development. While at Bristol-Myers, Dr. Rubinfeld was instrumental in licensing the original anticancer line of products, including Mitomycin and Bleomycin. Among other accomplishments, he was among the four co-founders of Amgen, Inc., and founded SuperGen, Inc., where he previously served as CEO, President and Chief Scientific Officer. In his career he has been instrumental in the development of several blockbuster cancer drugs including cisplatinum, etoposide, erythropoietin, decibitene and pentostatin, and the antibiotics amoxicillin and cefadroxil.

Steven A. Kriegsman, CytRx President and CEO said, “We feel that our stockholders are best served by a focus on potential therapeutics for cancer. We believe tamibarotene has strong potential as a revenue generator with a high likelihood for rapid U.S. approval as a third-line treatment for acute promyelocytic leukemia (APL). Our view is based on the substantial clinical history of tamibarotene as an approved treatment of relapsed APL, in Japan and the existing special protocol assessment (SPA) in place with the U.S. Food and Drug Administration (FDA) for our ongoing U.S. registration clinical trial. We are accelerating enrollment in this clinical trial, with the expectation of filing an NDA with the FDA as early as 2010. We are also taking steps to move into a Phase 2 clinical trial with INNO-206, our highly promising targetable pro-drug for the commonly prescribed chemotherapeutic doxorubicin. We believe that INNO-206 could be effective in a wide variety of cancers, including small cell lung cancer, sarcoma, breast and ovarian cancer and Non-Hodgkins Lymphoma.

“Importantly, we expect that we have ample financial resources with our current cash position and investment in RXi Pharmaceuticals Corporation to support this strategy,” according to Mr. Kriegsman. “We have strong oncology expertise within CytRx and are delighted that Dr. Joseph Rubinfeld, our long-time board member who has enjoyed an illustrious career developing cancer drugs, will be taking a leadership role in our oncology programs.”

Dr. Rubinfeld said, “Having reviewed the extensive data on tamibarotene and INNO-206, I am excited about the potential for these two cancer drug candidates and look forward to working closely with the CytRx management team to advance their clinical development to potential commercialization. I am also encouraged by the Phase 1 data we announced earlier this month with INNO-406, now known as bafetinib, which demonstrated positive, clinical responses in 35% of patients with refractory chronic myeloid leukemia. I believe these results will be instrumental in our search for a partnership for bafetinib.”

Mr. Kriegsman added, “We also stand behind our view that our orally administered molecular chaperone drug candidates, arimoclomol and iroxanadine, provide enormous potential in addressing large, underserved markets and are convinced that the prudent course to maximize stockholder value in this economic climate is to pursue pharmaceutical partners to share additional development costs for these longer-term programs. We intend to complete our ongoing arimoclomol animal toxicology studies and work aggressively toward lifting the current clinical hold in order to enable this drug candidate to move back into the clinic. At that point, we will seek partners for further development of arimoclomol as a therapeutic treatment for both ALS and stroke recovery. Additionally, iroxanadine has shown significant potential as a therapeutic treatment for diabetic foot ulcers and other diabetic complications, and based on Phase 2 data, we will pursue potential partnerships in cardiovascular conditions.”

CytRx’s drug portfolio includes the following:

Oncology Drug Candidates:

Tamibarotene: CytRx holds the North American and European rights to tamibarotene, a rationally designed, synthetic retinoid compound designed to potentially avoid toxic side effects of the current first-line APL treatment trans-retinoic acid (ATRA). CytRx is actively enrolling patients in a Phase 2 registration clinical trial, known as STAR-1, with tamibarotene to evaluate its efficacy and safety as a third-line treatment for APL. The registration study is being conducted under a Special Protocol Assessment. The FDA has granted Orphan Drug Designation and Fast Track Designation for the use of tamibarotene in patients with relapsed or refractory APL following treatment with ATRA and arsenic trioxide.

There are currently no approved third-line treatment options for refractory APL patients. CytRx estimates the U.S. market opportunity for tamibarotene in refractory APL at approximately $20 million annually. CytRx scientists are also evaluating clinical strategies for developing tamibarotene as a first-line or second-line APL therapy. The estimated annual market potential in the U.S. and Europe for an expanded label including refractory, maintenance and front-line therapy is $150 million. CytRx also retains an option to expand its licenses for the use of tamibarotene in other cancers including multiple myeloma, myelodysplastic syndrome and certain solid tumors in the U.S., and multiple myeloma, myelodysplastic syndrome and solid tumors, other than hepatocellular carcinoma, in Europe.

INNO-206: This pro-drug derivative of the commonly prescribed chemotherapeutic agent doxorubicin is designed to reduce adverse events by controlling drug release and preferentially targeting the tumor. In a Phase 1 study, INNO-206 was administered in doses at up to six times the standard dosing of doxorubicin without an increase in observed side effects over those historically seen with doxorubicin. Objective clinical responses were seen in patients with sarcoma, breast and lung cancers. The Company plans to evaluate further clinical development of INNO-206 in a wide variety of cancers, including sarcomas, breast and ovarian cancer, and Non-Hodgkins Lymphoma.

INNO-406 (bafetinib): INNO-406 (bafetinib), a potent, orally available, rationally designed, dual Bcr-Abl and Lyn-kinase inhibitor, is being evaluated for the treatment of patients with chronic myeloid leukemia (CML) and other leukemias that have a certain mutation called the Philadelphia Chromosome (Ph+) and are intolerant of or resistant to imatinib (Gleevec®) and second-line tyrosine kinase inhibitors (i.e. dasatinib (Sprycel®) and nilotinib (Tasigna®)). In November 2008, CytRx announced that bafetinib demonstrated positive, clinical responses in 35% of patients with CML in Phase 1 clinical testing. The Phase 1 clinical trial was used to determine the optimal dose prior to Phase 2 clinical efficacy testing.

CML is a type of cancer that starts in blood-forming cells of the bone marrow and invades the blood. In 2007, the American Cancer Society estimated that approximately 4,600 new cases of CML were diagnosed in the U.S. and that the number will increase as the population ages. Current estimates are that worldwide CML prevalence will increase by 10,000 patients a year, reaching a population of 110,000 in 2010. The global market will grow to an estimated $5.5 billion by 2012.

Molecular Chaperone Regulation

CytRx is a leader in molecular chaperone regulation technology. The Company currently has two orally administered, clinical-stage, drug candidates and recently discovered a series of additional compounds that may provide a pipeline for additional drug candidates. The Company’s drug candidates are believed to function by regulating a normal cellular protein repair pathway through the activation or inhibition of “molecular chaperones.” Because damaged proteins are thought to play a role in many diseases, activation of molecular chaperones that help to reduce the accumulation of misfolded proteins may have therapeutic efficacy in a broad range of disease states. Similarly, CytRx believes that the inhibition of molecular chaperones that normally help protect cancer cells from toxic misfolded proteins may result in the selective destruction of cancer cells.

  • Arimoclomol: This molecular chaperone regulator drug candidate is being considered as a treatment for amyotrophic lateral sclerosis (ALS or Lou Gehrig’s disease) and stroke recovery. Arimoclomol has been studied in seven Phase 1 and two Phase 2 clinical trials without any significant adverse events. CytRx’s Phase 2b clinical trial with arimoclomol as a treatment for ALS was placed on clinical hold by the FDA in January 2008, unrelated to any data generated by human studies, and additional preclinical toxicology studies are underway to resolve this issue.
  • Iroxanadine: CytRx believes that this orally available small molecule compound represents a potentially powerful breakthrough in the treatment of vascular diseases that are caused in part by damage to “vascular endothelium” that lines the inside of blood vessels. CytRx believes that endothelial dysfunction plays a key role in the development of various vascular diseases or their complications including diabetic ulcers, thrombosis, retinopathy, and peripheral artery disease. Preclinical and clinical studies with iroxanadine indicate that it has therapeutic potential for the treatment of cardiovascular atherosclerosis. According to the National Heart, Lung & Blood Institute, atherosclerosis is a leading cause of illness and death in the U.S. and affects approximately 4.6 million people annually.

CytRx San Diego Laboratory: The CytRx San Diego Laboratory is using the Company’s proprietary Master Chaperone Regulator Assay (MaCRA), a cell image-based screening tool that enables the rapid and quantifiable screening of large numbers of small molecule compounds. This technology is used to identify potential drug candidates that modify the activity of a protein known as heat shock transcription factor 1 (Hsf1) and consequently control entire groups of molecular chaperone proteins that repair or degrade toxic misfolded proteins present in diseased cells. Evaluation of the compounds identified in the screen has shown that they exhibit cytoprotective properties in cell culture models of disease. This platform has broad applicability to a range of therapeutic areas, through its ability to identify drug candidates that can either inhibit or amplify molecular chaperone activity. Information related to the development of MaCRA for compound screening was published in the November 2008 issue of the peer-reviewed Journal of Biomolecular Screening.

CytRx Oncology Expertise

Collectively, CytRx’s management and its Board of Directors have brought numerous cancer drugs to market. In addition to Dr. Rubinfeld, the senior managers and directors of CytRx who hold significant oncology experience include: Max Link, Ph.D., Chairman of the Company’s Board of Directors since 1996, who served for a number of years as Chairman and CEO of Sandoz Pharma as well as a director of Alexion Pharmaceuticals, Inc., Celsion Corporation and Discovery Laboratories, Inc.; Jack R. Barber, Ph.D., Chief Scientific Officer, who has significant R&D experience in oncology at Immusol and Viagene, where he most recently served as Head of Oncology; and Shi Chung Ng, Ph.D., Senior Vice President of Research and Development, who has substantial R&D experience at companies such as Abbott and ArQule, Inc., and most recently served as Vice President of Molecular Oncology at Ligand Pharmaceuticals.

About CytRx Corporation

CytRx Corporation is a biopharmaceutical research and development company engaged in the development of high-value human therapeutics. The CytRx drug development pipeline includes programs in clinical development for cancer indications, including tamibarotene in a registration study for the treatment of acute promyelocytic leukemia (APL). CytRx is developing two drug candidates based on its industry-leading molecular chaperone technology, which aims to repair or degrade misfolded proteins associated with disease. The Company owns and operates a research and development facility in San Diego. CytRx also maintains a 45% equity interest in publicly traded RXi Pharmaceuticals, Inc. (NASDAQ: RXII). For more information on the Company, visit www.cytrx.com.

Forward-Looking Statements

This press release contains forward-looking statements within the meaning of Section 21E of the Securities Exchange Act of 1934, as amended. Such statements involve risks and uncertainties that could cause actual events or results to differ materially from the events or results described in the forward-looking statements, including risks relating to the outcome or results of any pre-clinical or clinical testing of CytRx’s potential oncology or molecular chaperone drug candidates, including tamibarotene as a third-line treatment for APL, risks related to CytRx’s ability to enter into partnerships to advance the clinical development of INNO-406 and its clinical molecular chaperone portfolio, uncertainties related to the impact of the FDA’s clinical hold on the Company’s arimoclomol clinical trial for ALS on the timing and ability to resume clinical testing at the desired dosage of arimoclomol, the risk that any requirements imposed on the Company’s planned clinical trial designs for ALS or stroke recovery by the FDA as a result of the concerns expressed in their clinical hold of the Company’s ALS program might adversely affect the Company’s ability to demonstrate that arimoclomol is efficacious in treating ALS or stroke patients or cause the Company to cancel one or both of those trials, risks related to CytRx’s need for additional capital or strategic partnerships to fund its ongoing working capital needs and development efforts, risks related to the future market value of CytRx’s investment in RXi and the liquidity of that investment, and the risks and uncertainties described in the most recent annual and quarterly reports filed by CytRx with the Securities and Exchange Commission and current reports filed since the date of CytRx’s most recent annual report. All forward-looking statements are based upon information available to CytRx on the date the statements are first published. CytRx undertakes no obligation to publicly update or revise any forward-looking statements, whether as a result of new information, future events or otherwise.

November 26, 2008

IPR story 12- Patenting a mere idea


Jaidev had joined a leading Pharmaceutical Research Institute in India, for his Ph.D work. He reviewed his research plan thoroughly and also searched patents. Based on discussions with his guide, he formulated a very innovative research plan, pertaining to development of a new screening method for diabetic compounds. He started his work and after nearly 2 years of hard work, came up with very good data. He filed a patent in India and subsequently in the USA. He was confident of grant of patent, since nobody had done the work he had done.

The examination of his patent application started in the USA. He was shocked when his application in the USA was objected owing to a provisional patent filed by a researcher in USA. The provisional application filed by the USA researcher merely discussed theoritically an innovative research plan, very similar to the one proposed by Jaidev. However, there was no follow up after that and the researcher had abandoned the patent application. Mere theoritical discussion on the idea was there, without any data. However, it had been duly published and was in public domain. The US examiner objections were based on the observation, that Jaidev’s idea was not new- it had already been disclosed by someone else. Novelty was destroyed and Jaidev could not get a patent.

Discussion:

The case gives very important lessons for researchers:

1. Don’t wait for research work to be completed before filing a patent- even at initial stage or just when preliminary encouraging results give proof to an innovative concept, file a provisional patent application in India. It is quite cheap- govt. fee is just Rs.1000/- and in case you do it yourself, no further expense. But it protects your idea! After filing, within 12 months, you must file complete patent application, duly accompanied by data and including ‘claims’. In provisional, claims are not there.

2. Filing a provisional patent application can be done for a mere theoritical idea, with due discussion on the scientific and technical logic behind the concept. However, your filing date and hence PRIORITY gets protected from date of filing provisional.

Had Jaidev filed a provisionl application, well in time he might have been able to save his work. It was something very easy and simple, but because he was not aware, he waited to finish his work and lost the race to someone who was smart enough to file a provisional patent. However, the irony in this case is that even the US inventor did not get a patent, since he had not filed a complete patent application within one year. Maybe, he did not get success with experiments or some other problem. Jaidev did succeed in the Lab, but lost the patenting case, since his novelty had been destroyed by the US inventor.

Hence, do not underestimate the VALUE OF PATENTING YOUR IDEAS- THEY ARE PRECIOUS! FILE PROVISIONAL APPLICATIONS AT THE EARLIEST. DO NOT WAIT FOR YOUR RESEARCH TO FINISH.

Nanion Increases Throughput and Cuts Costs with a New Industrial 96-Channel Patch Clamp Screening Robot


Today, Nanion announces the late-stage development of a new automated patch clamp platform: the SyncroPatch 96. Developed to meet the throughput demands of industrial ion channel drug screening and safety profiling, and with a price-per-data-point compatible with screening standards, the SyncroPatch 96 will offer the highest throughput in the market for high quality HTS-oriented ion channel screening.

Munich, Germany, November 20, 2008 –(PR.com)– Following the successful market introduction of two automated patch clamp devices, the Port-a-Patch (2004) and the Patchliner (2006), Nanion now introduces the SyncroPatch 96. Nanion’s Patchliner and Port-a-Patch platforms enjoy great popularity in both academic and industrial settings and have received enthusiastic user feedback in customer surveys such as the HTStec report. Building on their success, the new SyncroPatch 96 vastly increases throughput while reducing the cost per data point to a level compatible with industrial ion channel screening requirements.

“There is a gap between the demands in ion channel drug screening and the capability of the high quality automated patch clamp platforms currently available on the market. Pharmaceutical companies want higher throughput and lower cost per data point, whilst maintaining data quality. The SyncroPatch96 will fill this gap, by providing high throughput, high quality patch clamp recordings, at a low enough cost to keep screeners happy.” says Dr. Niels Fertig, CEO of Nanion.

The SyncroPatch 96 acquires simultaneous recordings from 96 individual cells in a well-plate format and allows for screening of both ligand- and voltage-gated ion channels. The platform supports giga-seal recordings, continuous recording during compound application and addition of multiple compounds to each of the 96 cells. The SyncroPatch 96 will be launched in 2009.

About Nanion:

Nanion Technologies GmbH is a German Private Limited Company and was founded in 2002 as a spin-off from the Center for Nanoscience (CeNS) of the University of Munich. Nanion’s team has developed and globally established two highly successful automated patch clamp instruments as enabling tools for sophisticated and high throughput applications for ion channel research and drug discovery.

Nanion’s instruments use planar patch clamp chips which replace the traditional glass pipette used in the technique of patch clamping. Nanion was nominated in 2007 for Germany’s most prestigious innovation award the Deutscher Zukunftspreis (German Future Prize, Federal President’s Award for Technology and Innovation).

November 20, 2008

GEN Reports on the Trend Toward Predictive Toxicogenomics

NEW ROCHELLE, N.Y., Nov 19, 2008 /PRNewswire via COMTEX/ — Biotech scientists increasingly are applying genomics technologies to toxicology research to better understand the effects of novel drug candidates on a variety of organ systems, reports Genetic Engineering & Biotechnology News (GEN). They are especially interested in figuring out a new compound’s mechanism of action and eventually developing a predictive toxicology technique, according to the November 15 issue of GEN. ( http://www.genengnews.com/articles/chitem.aspx?aid=2675)

“Toxicogenomics, which is essentially gene-expression profiling, is the next step up from basic toxicology studies,” says John Sterling, Editor-in-Chief of GEN. “It is a more complex approach, and it will take some time before it becomes a regular tool in the technology armentarium of drug discovery and pharmaceutical scientists.”
So far most companies are focusing on toxicogenomics primarily as a method to explore mechanisms of action rather than to predict toxicity. Roche, for example, uses toxicogenomics to generate hypotheses when trying to unravel the cellular machinery underlying toxicity responses, which then are tested more thoroughly using other assays. Novartis is employing known toxic compounds to develop the techniques to understand the mechanistic actions of toxicity. Such screening led to the recent validation of biomarkers for kidney toxicity.
Groups such as The C-Path Predictive Safety Testing Consortium are examining published toxicogenomics multiple gene biomarkers or signatures and trying to validate those signatures across laboratories.
Also covered in the GEN article is work being carried out by Amgen, Entelos, Lilly Research Laboratories, Hamner Institutes for Health Sciences, and the Health and Environmental Sciences Institute.

SOURCE Genetic Engineering & Biotechnology News


	

November 19, 2008

Virtual Screening Gives Drug Design a Boost

San Diego, CA (OBBeC) – Researchers at the University of California, San Diego, developed a unique computational approach to identify key compounds that could lead to new drugs to combat African sleeping sickness — a disease spread by the biting tsetse fly and caused by the parasite Trypanosoma brucei.

Around 150,000 people per year get African sleeping sickness. Unless treated, the illness is invariably fatal and with limited treatment available. The commonly used medicines to treat the disease are either difficult to administer, expensive, or toxic. For example, the widely used drug melarsoprol is essentially arsenic dissolved in antifreeze. Only one new drug to treat African sleeping sickness has appeared in the past 50 years. “The biomedical significance of new drugs to treat trypanosomal diseases, which occur mainly in developing countries, would be huge,” says Peter Preusch, of the National Institute of General Medical Sciences (NIGMS).
The research team led by computational biologist J. Andrew McCammon, have identified five compounds that could provide the solution for this problem. The compounds block the activity of the trypanosomal REL1 enzyme, which the parasite needs in order to survive. According to the press report, REL1 has a unique role in the trypanosome’s mitochondria, the organelles that provide the parasite with energy. The enzyme joins mitochondrial messenger RNA fragments, making them whole and functional. These messages are the blueprints for making the proteins that power the mitochondria. Without REL1, some of these mitochondrial proteins are missing, which slows energy production and kills the parasite.
The results appeared online this week in the Proceedings of the National Academy of Sciences.
New Computational Approach
The approach developed by McCammon’s group uses a combination of several computational tools. It starts with a detailed model of the biological target –REL1 in this case — derived from X-ray crystallography. It then uses biophysical principles to find all the ways in which the protein can twist, turn, and wiggle.
“We know that proteins aren’t static,” said Dr. Rommie Amaro, the lead author of the study. “They’re dynamic moving machines. The unique thing about this approach is that it allows full protein flexibility.”
Though, predicting the countless shapes that a large, complex molecule like a protein can adopt requires enormous computer power. A REL1 analysis done on a regular desktop could take years while those on supercomputers take a few days. The computers used in this study, explains Amaro, are among the most powerful in the country.
Once they know the dynamics, the researchers carry out a virtual screen of hundreds of compounds, testing their ability to stick to a key part of REL1. Compounds that stick tightly have a good chance of inhibiting the enzyme’s activity and killing the parasite.
“It’s rather like a child’s puzzle where one must put the cow-shaped piece into the cow shaped hole in the barnyard scene,” explains Preusch, who oversees computational biology grants at NIGMS, which partially funded the work. But like real cows, he added, molecules are in constant motion. “McCammon has developed methods that take these motions into account, as well as the changes in a protein’s shape that can occur upon binding.”
The virtual screen predicted that about a dozen compounds would bind tightly to REL1’s hot spot. Knowing that a slightly different version of one of these might stick even more tightly, the researchers searched a large database of existing compounds for structurally similar molecules.
When they tested their best candidates experimentally, five inhibited REL1. These five molecules, which block the activity of a crucial trypanosomal enzyme, can now serve as the basis for future drug design and discovery efforts.
Future Outlook
McCammon’s computational method has already proven its utility for designing other important drugs. His group used it to develop a model for a new class of drugs to treat AIDS that led to raltegravir, which the Food and Drug Administration approved in 2007. McCammon’s team also used the method to identify promising drug candidates for treating H5N1 avian flu.
McCammon’s team is now focusing on designing even better inhibitors of trypanosomal REL1. The goal is to tweak the inhibitors’ structures, making them bind even more tightly to REL1 and less tightly to related human enzymes. Binding to human enzymes makes an inhibitor less attractive as a drug candidate because the interactions could cause undesired side effects.
This work, says McCammon, “tells a story that may be of wide interest.” The computational approach not only could lead to improved drugs for treating African sleeping sickness, but it could be used to develop compounds for use against other illnesses for which we need better medications.
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