Archive for the ‘R & D’ Category
TimTec Launches Division of Organic Synthesis and Medicinal Chemistry Contract Research Services
Last Updated on Saturday, 24 July 2010 04:31 Written by admin Thursday, 8 July 2010 11:39
Newark, DE, July 8, 2010 Press Release – TimTec, LLC is pleased to announce the launching of the new Division that manages Organic Synthesis and Medicinal Chemistry Contract Research Services. The emergence of the division is an evolutionarily progression for TimTecs business development. The company has been known for its expertise in organic chemistry design and supply for drug discovery for 15 years. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.
The Head of Contract Research Services, J. C. Pelletier, PhD., has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. The TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities. TimTec specialists are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges.
TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. Contract research services include, but are not limited to, flexible contracts, program management, structure-activity relationship evaluation, lead optimization, property optimization for ADME and PK, metabolite synthesis, enabling technologies (parallel synthesis, multistep synthesis, analytical chemistry), mg to kg synthesis capacity, compound distribution, and patent application preparation assistance. The Contract Research Division puts great emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of clients knowledge resources and interests. Dedication to service is matched by exceptionally competitive prices.
Contact Information:
TimTec LLC
Harmony Business Park A-301
Newark DE 19711
Tel 302 292 8500
Fax 302 292 8520
info@timtec.net
http://www.timtec.net/contract-research-services.html
About TimTec
TimTec LLC is a privately held company located in Newark Delaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds and collections, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.
Ranbaxy to transfer drug discovery unit to Daiichi Sankyo
Last Updated on Thursday, 8 July 2010 10:54 Written by admin Thursday, 8 July 2010 10:54
Jul 06, 2010 (Datamonitor via COMTEX) –
Daiichi Sankyo and Ranbaxy Laboratories, a research based pharmaceutical company, have announced that Ranbaxy’s new drug discovery research, or NDDR, has been transferred to Daiichi Sankyo India Pharma as part of the strategy to strengthen the global R&D structure of the Daiichi Sankyo Group.
The transaction has been reportedly approved by the Department of Scientific and Industrial Research, Ministry of Science and Technology, Government of India.
The new organization, Daiichi Sankyo Life Science Research Center (RCI) in India based in Gurgaon will play a key role in the group’s global drug discovery research – to create new drugs, especially in the area of low molecular weight infectious and inflammatory disease treatments. RCI will also reportedly continue to support the programs of dengue and tuberculosis that NDDR was working on in alliance with the department of biotechnology, Ministry of Science and Technology, Government of India.
Joji Nakayama, president and CEO of Daiichi Sankyo, said: “With the transfer of the NDDR into the Daiichi Sankyo Group’s pharmaceutical R&D organization, we will further strengthen our integrated global research capabilities through the addition of talented researchers who offer a new perspective and have a wealth
of imagination and experience. We look forward to achieving outstanding and innovative results based on the implementation of global research management throughout our highly diversified and global R&D structure.”
Posted under Asia, Drug Development, Press Releases, R & D | No Comments
TimTec’s Contract Research Services
Last Updated on Thursday, 8 July 2010 10:18 Written by Editor Thursday, 8 July 2010 03:22
High Quality Organic Synthesis and Medicinal Chemistry Contract Research Services at an Outstanding Value
TimTec brings 15 years of expertise in organic chemistry design and supply for drug discovery closer to your supplemental bench-top requirements by launching The Organic Synthesis and Medicinal Chemistry Contract Research Services Division. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.
TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. All Contract Research Services are delivered with an emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of our clients’ knowledge resources and interests. We are dedicated to providing these services at exceptionally competitive prices.
The Head of Contract Research Services has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. We are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges. Your TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities.
TimTec Contract Research Services Start with:
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Flexible Contracts
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Program Management
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State of the Art Facilities
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Structure-Activity Relationship Evaluation
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Lead Optimization
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Property Optimization for ADME and PK
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Metabolite Synthesis
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Enabling Technologies – Parallel synthesis, multistep synthesis, analytical chemistry
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Mg to Kg Capacity
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Compound Distribution – Solid or solution, vials or plates
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Patent Application Preparation Assistance
Supplemental Services and Products:
Custom Synthesis
Compound Acquisition
Weighting and Plating
HTS compounds and compound collections – ActiMol Line of products
Posted under ADMET Studies, Drug-Like Compounds, Medicinal Chemistry, New Products, North America, R & D, Research Projects | No Comments
Ion Channels Open Doors to New Drugs Increased R&D Efforts Are Overcoming Obstacles and Showing Potential
Last Updated on Thursday, 8 July 2010 03:20 Written by Editor Thursday, 8 July 2010 03:20
- Nina Flanagan
Researchers at the recent Society for Biomolecular Screening conference and CHI’s upcoming “Pharmacology Driven Assays for GPCRs and Ion Channels†shared information on a cornucopia of topics, including the latest enabling technologies, new screening paradigms, and novel approaches to generate GPCRs.
The IonFlux system from Fluxion Biosciences was recently beta tested by scientists at Novartis Institutes for Biomedical Research (NIBR). “Compounds, buffers, and waste are contained on a single 96-well plate, eliminating robotic handling. Air pressure drives experiments in microfluidic channels in a layer below the wells. This is a novel approach in automated electrophysiology,†explained Andrew Golden, Ph.D., post-doc fellow.
Robustness is enhanced via recordings taken from 20-cell ensembles (IonFlux HT), and pharmacology improved by recording a full range of concentrations from the same group of cells, according to the company. There are two available systems—the IonFlux 16, which uses 96-well plates, and the IonFlux HT, which uses 384-well plates.
Analysis of the prototype (alpha and beta testing) was initially focused on whether IonFlux could reproduce results demonstrated on other platforms. “The microfluidic approach could be helpful for ligand-gated ion channels—especially for subsets of those for fast desensitizing ligand-gated ion channels where you only add a short pulse of the ligand or neurotransmitter,†explained Mats Holmqvist, Ph.D., research investigator in the center for proteomic chemistry at NIBR.
In addition, Dr. Holmqvist said the hope for the new platform is that it should provide selectivity not only by target but also by function. “You can utilize ‘use dependency’—the accumulation of inhibition with repetitive depolarizations. If an ion channel is active, the drug may be much more potent.†With this new technology, one should be able to refine and understand how a compound affects an ion channel. However, it’s still too early to show whether this will be the case.
Since HT platforms for ion channels are fairly new, standardization across different instruments hasn’t been addressed. “There are different quality control parameters, including the way of recording a single cell per well or ensemble recording in parallel. Some machines use Oracle database versus file formats. We’ve been trying to address that in safety profiling. A quick answer is that we make a summary PDF file of every compound in each experiment that can be accessed any time,†noted Dr. Holmqvist.
Parallel Screening
The traditional screening paradigm involves one target for primary HTS. However, this process “wastes a considerable amount of time to get results, and also wastes efforts on compound management in order to get those compounds ready for testing,†said Peter Hodder, Ph.D., senior director of lead identification for the translation research institute at the Scripps Institute, Florida.
His group uses a parallel screening process that screens compounds against the target and antitarget simultaneously. “Antitarget is an all-encompassing name for any assay you would run that’s different from the target—usually to remove compounds from further consideration,†Dr. Hodder explained. “We found most of those compounds are junk compounds anyway.†The antitarget becomes important for the hit compounds, because it provides information on whether it is something specific to the target or whether it is something nonspecific to the assay format.
Time saved via parallel screening can be four to five weeks per target. In addition, and what is more important and what is harder to gauge, he noted, is saved efforts following false trails, which result in smaller, cleaner datasets. Relevant structure activity relationships emerge early in a campaign. For example, Dr. Hodder performed an SF1 (transcription factor) assay and ran the antitarget ROR against it and found potent compounds. “If we had relied on primary screening alone, those compounds would not have been selected.â€
The parallel-screening format is not specific to any target class. “What’s more important is how to apply it to different target classes or different assay formats.†His group was successful in screening ion channels, including TRPML3 with TRPN1 as the antitarget (TRP is transient-receptor potential). HTS probes confirmed that the target is not located on plasma membranes in native cells.
Dr. Hodder added that this approach can be used to help focus on the most important compounds for drug or probe discovery, but it’s key is in choosing the right antitarget. “If it’s too close in relationship to the target, you’re going to start throwing out compounds you don’t want to during the campaign.â€
His group is now performing more sophisticated screening using two or three antitargets and trying to find the overlap of hits that are specific in all three versus two or one of those targets and antitargets. “This challenges us to think about how we present and analyze our data.â€
Novel Assays
Some of the challenges of working with ion channels include controlling activity, whether with a small molecule ligand or voltage. Many ion channels inactivate within milliseconds, making HTS difficult.
David Weaver, Ph.D., director at Vanderbilt Institute of Chemical Biology HTS, has been focusing his research efforts on ion channels—especially 7TM (7-Transmembrane) receptors.
“We are interested in looking at some of the effector systems that are more physiologically relevant and one of these is the GIRK (G-protein regulated inwardly rectifying potassium (K+) channel).†His group developed this assay to measure the activity of GI-coupled 7TM receptors. “The idea was whether we could see any differences in the pharmacology and the fact that we may be using a more physiologically relevant end effector rather than using mutant G proteins to couple the change in intracellular calcium.â€
The success of the GIRK assay encouraged Dr. Weaver to examine ion channels as end effectors that could be used to generate new assays with physiological relevance. Preliminary data demonstrates the ability to detect changes in M-current (muscarinic-modulated potassium current, usually studied in the brain and peripheral nervous system) activity.
He developed an HTS-compatible assay that can measure and quantify the modulation of M-current downstream from the 7TM receptor using thallium-flux. This optical assay platform can use a commercially available kinetic imaging plate reader.
According to Dr. Weaver, the only nonstandard part of the assay is that he extracts a slope from the initial measurement, instead of fitting a peak amplitude. His hope is to use this assay to further understand the pharmacology of 7TM receptors. “It’s my intent that we can demonstrate that these are good, robust assays for use in HT screens to discover novel modulators of 7TM receptors or the ion channels we’re using as effectors.â€
Novel Targets
“Ion channels are terrific molecular targets, and many drugs have been targeted to them,†stated David Clapham, M.D., Ph.D., Aldo R. Castenada professor of cardiovascular research at Children’s Hospital Boston. Yet, one of the biggest challenges is the gold standard assay—the patch clamp.
This is a time-consuming technique—single cell membranes must be broken open and the current must be recorded while controlling voltage in the cell. Although HT assays exist, not all ion channels are suited to them. “The most promising are the very fast, voltage-dependent channels with large, rapid changes and ones less amenable are ones that are similar to each other in their properties, like TRP channels—these are more difficult.â€
Dr. Clapham also presented information on what he thought were good, fairly recent, ion-channel targets and included some recent data on some of his work with these targets.
Many TRP channels are involved in sensory functions, like smell, taste, and hearing. TRPV3 is an ion channel that is well expressed in skin. Dr. Clapham demonstrated that both skin barrier formation and some aspects of hair formation are altered by this ion-channel’s activation or block.
It is activated by subtle temperature changes—temperatures about 32ºC—indicating TRPV3 is sensing heat at the skin surface and relating that to the nerves. This indicates it may help regulate body temperature. Growth factors such as EPGR potentiates TRPV3 to bring calcium into karatinocytes, and, in turn, TRPV3 potentiates EPGR, so there’s a positive feedback loop.
“This is important for the proper formation of skin barriers, so that there is normally a cycle of karatinocytes maturing from deeper in the skin to the surface of the skin.†Dr. Clapham added that TRP channels are difficult to work with because they are fairly slow and their properties are often difficult to distinguish. In addition, they are often small in size, and there is a lack of known ways to activate them.
Additional ion channels that Dr. Clapham thought were worth pursuing were the NAV1.7 to NAV1.9 pain targets, which are voltage-gated sodium channels. A new chloride channel, TMAM16-A, and the ORAI channel, which is important in the immune system, were also on the list. An interesting new target for contraception, called CATSPER, is an ion channel only present in mature sperm and required for male fertility. “This may be a good method of contraception without hormones,†said Dr. Clapham.
“Our job is to find new targets and new molecules, and then other people can work with those molecules to target diseases.â€
New Approach
There are many challenges for the generation of new GPCRs, said Michel Bouvier, Ph.D., professor and chairman in the department of biochemistry at the University of Montreal. These include selectivity and ligand-biased signaling, where one receptor can couple to different signaling pathways in a cell.
“The problem with this is that you are trying to monitor the efficacy of a compound toward one signaling pathway, but since there are multiple ones, we don’t necessarily know which one to follow that will correlate with a disease or particular activity.†His approach is to develop one assay that could encapsulate in one reading all the signaling pathways and by dissecting the signatures, provide information about the pathways being engaged by a receptor.
Utilizing Roche’s label-free xCELLigence platform, his group is able to measure cell impedence. Each well of the plate has electrodes. As the cells grow, the impedance increases, and when the cells are treated with compounds that bind to receptors, many different pathways are triggered.
The readout reflects changes in impedance from the compound over time—providing a global assessment of the various pathways. Different compounds generate different curve shapes. “We can use this technology to differentiate classes of compounds that have different relative selectivity toward different pathways. It’s generating a simpler way to classify compounds in different efficacy profiles toward different signaling pathways.â€
Dr. Bouvier added that they can now, using selective inhibitors of different pathways such as the generation of cyclic AMP, show how the inhibition influences the shape of the impedance curve. “Not only can we start classifying the ligands in different categories or compounds, but we can start making predictions on which pathways these compounds will be actively inhibiting. His group is planning to develop algorithms to apply to the curve and thus, provide a response as to which pathway is being affected. “We first need to confirm which portion of the curve informs us about each pathway.â€
This approach can be used for almost any receptors, reported Dr. Bouvier. It provides a big time savings—one assay instead of four or five. However, he added, “we don’t know yet if all signaling pathways will respond to changes in impedance—from our data so far, we haven’t encountered such a pathway.â€
source: genengnews.com
Posted under Drug Development, New Drugs, Press Releases, R & D | No Comments
Potent Novel Tool For Combating Autoimmune Diseases And Leukemia
Last Updated on Thursday, 28 January 2010 06:10 Written by Editor Thursday, 28 January 2010 06:10
A study carried out by the scientists at the Scripps Research Institute illustrated a novel, highly practical strategy for identifying molecules that avert a particular form of immune cells from launching assaults on their host. These findings have added a potent new-fangled tool to the ongoing investigation for probable treatments for autoimmune diseases like MS or multiple sclerosis

, as well as for the treatment of types of leukemia like myeloid leukemia.
The study conducted by Thomas Kodadek, a professor in the Chemistry and Cancer Biology Departments, Scripps Florida, and associates was printed in the ‘Chemistry & Biology’ Journal.
In the novel study, Kodadek and his associates utilised samples taken from an animal model of MS for screening for T cells – a kind of white blood cell that dons fundamental role in the immune system – with an increasing presence in the ailment. The screen additionally recognized molecules that interfered with such T cells’ auto-reactive nature or their assault on the body itself instead of a foreign intruder like a virus or bacteria.
Kodadek stated that their method concurrently unearths and separates auto-reactive T cells along with inhibitors to them. A dual achievement at the core of which is a relative screening procedure of healthy T cells vs. Disease-causative T cells. Even as the process is technically complex and intricate, the thought behind it is not. The scientists intended to make the process of recognizing compounds simpler that could hinder auto-reactive T cells with outstanding specificity and the scientists were able to accomplish their objective.
The scientists employed a model of MS – an autoimmune inflammatory condition that affects the brain and the spinal cord for the study. MS is a condition wherein the immune system assaults the myelin sheath coating and defensive nerve cells that lead to a host of symptoms dependent on what component of the nervous system has been affected. Prevalent signs of the condition involve weariness, numbing sensation; difficulties experienced in walking balancing and co-ordination; dysfunctional bladder and bowel; ocular problems; giddiness and vertigo; sexual dysfunction problems; pain, mental problems; emotional variations and spastic behaviours.
Simplification of the Process
Kodadek and his associates set up the novel method for shedding light on these autoimmune diseases and other kinds of disorders and produced a vast assortment of peptoids –molecules linked to, though more constant as compared to the peptides which made up the proteins. By organizing thousands of the peptides microscopically, the prototype of binding antibodies (a form of autoimmune molecule) and peptoids could be pictured. By observing samples drawn from animal models of an identified disease such as MS, peptoids which exhibited binding to antibodies closely linked with that disease could be easily identified.
Even better, peptoids which showed binding to the autoreactive T cells could be spotted with no awareness of the particular antigen (molecules that elicit the immune assault), offering an impartial approach with which to explore potentially beneficial compounds.
Kodadek stated that they had made a breakthrough where they set up a system that identifies T cell receptors which are copious in an ailing animal and in sapped levels in a healthy animal.
Potential for Curative Breakthrough
The novel process created a novel potential for curative finding. Molecules that targeted auto-reactive T cells in a direct way, while overlooking those T cells that identify foreign antigens, could provide the basis for a new drug development program intended at elimination of autoreactive cells with no affect on the normal functioning of the immune system.
Kodadek stated that the novel study is not the ultimate solution as it employed a model of MS elicited by a sole antigen whereas in human beings there could be 2 to even more antigens that trigger an autoimmune disease like MS that needs further investigation. The method could be applicable with ease to blood cancers, although as the disease-causative T cells have been completely characterized and there being quite a few of them.
Source: simplehealthguide.com
Posted under Medicinal Chemistry, Press Releases, R & D | No Comments
JAX–West Helps Search for Compounds That Radically Extend Lifespan
Last Updated on Monday, 11 January 2010 05:30 Written by Editor Monday, 11 January 2010 05:30
In 2004, Avi Kremer, a 29-year old Harvard Business School student, was diagnosed with ALS. Avi’s doctors told him there was nothing that modern medicine could do for him. In response, he and fellow students founded Prize4Life, Inc. , a non-profit organization dedicated to accelerating research for treating and curing ALS by using the leverage of large inducement prizes. In 2006, Prize4Life opened the “ALS Biomarker Challenge,†offering a $1 million prize to a researcher who could find a biomarker that would reliably measure disease progress in ALS patients. A year ago, it established the “Avi Kremer ALS Treatment Prize,†a $1 million award for finding a treatment candidate that reliably and significantly increases the lifespan of ALS mouse models. Competing teams are actively pursuing several approaches, including therapies to replace damaged cells, protein-based therapeutics, and small molecule drugs that interfere with ALS-implicated pathways. Competition for both prizes is open to all interested researchers. Both prizes have attracted research teams from industry and academia from around the world.
The SOD1 Mouse
Three percent of ALS cases are associated with mutations in the antioxidant enzyme superoxide dismutase-1 (SOD1) gene, the first gene associated with ALS. With so little known about the genetics of ALS, research so far has concentrated on the pathogenesis of SOD1 mutations in laboratory mice. To provide researchers with the most widely used ALS mouse models available for preclinical drug testing, Prize4Life has partnered with The Jackson Laboratory (JAX). The models, popularly known as SOD1 mice, are distributed from dedicated supply colonies maintained by JAX® Breeding Services. JAX currently distributes 12 different SOD1 models – with different forms of the SOD1 mutation and on different genetic backgrounds. Among the most widely used of these models is JAX® Mice strain B6SJL-Tg(SOD1*G93A)1Gur/J (002726). Like several other SOD1 models, this one has a high copy number of the mutant human superoxide dismutase 1 (SOD1) transgene, which contains the Gly93–>Ala (G93A) substitution. The mutation underlies the most studied form of inherited ALS in humans. The mice lose motor neurons in the spinal cord, become paralyzed in one or more limbs, and die by four to five months. These phenotypes closely model those of human ALS (Gurney et al. 1994). As noted by Dr. Tom Maniatis, Chair of Columbia University’s Biochemistry & Molecular Biophysics Program, a prominent ALS researcher, and a member of Prize4Life’s Scientific Advisory Board, “An effective treatment for ALS is desperately needed, and the existing [SOD1] mouse model is the primary gateway to clinical trials†(CheckOrphan 2009).
SOD1 Mice Need Special Care
Many of the initial studies conducted with Tg(SOD1*G93A)1Gur/J mice have provided a wealth of information and insight on how to best use them in preclinical trials. However, like other highly expressed transgenes, the G93A transgene can spontaneously lose copy number, which can greatly confound experimental results. Therefore, the mice need to be handled carefully. When Prize4Life approached JAX to establish a dedicated supply for their researchers, Dr. Melanie Leitner (Chief Operating Officer and Chief Scientific Officer for Prize4Life), Dr. A. Sheila Menzies (Scientific Program Officer for Prize4Life), and Dr. Cathleen Lutz (Associate Director for Genetic Resource Science at JAX) produced a companion set of informational materials entitled “Working with ALS Miceâ€. The materials are available at www.jax.org/jaxmice/literature/factsheet/working_with_ALS_mice.pdf.
“Prize4Life spearheaded this effort,†say Lutz. “It’s really targeted to those investigators who are new to the field of ALS and who are working with the SOD1 mice and designing their preclinical trials. The scientific community has learned a great deal about how to work with these mice over the years. It’s important to make that information more widely known so that valuable time and resources aren’t wasted by repeating past mistakes.â€
If Prize4life succeeds in its goal of bridging the critical steps between academic discovery and therapy in the clinic, it could have major implications for ALS patients and for any group trying to solve a biomedical problem. Interested researchers can learn more at www.prize4life.org.
References
CheckOrphan. 2009. Prize4Life marks one-year anniversary of Avi Kremer ALS Treatment Prize. http://www.checkorphan.org/news/prize4life_marks_one_year_anniversary_avi_kremer_als_treatment_prize. October 13, 2009.
Gurney ME, Pu H, Chiu AY, Daly Canto MC, et al. 1994. Motor neuron degeneration in mice that express a human Cu,Zn superoxide dismutase mutation. Science 264:1772-5.
Source: animallab.com
Posted under Discoveries, Innovations and Patents, Drug Development, Press Releases, R & D | No Comments
Ore Pharmaceuticals Announces Upcoming Publication of Research Study on ORE1001
Last Updated on Thursday, 8 October 2009 12:19 Written by Editor Thursday, 8 October 2009 12:19
Ore Pharmaceuticals Inc. (Nasdaq:ORXE), announced today the publication of an article in the online version of the journal Inflammation Research titled, "Effects of the ACE2 inhibitor GL1001 on acute dextran sodium sulfate-induced colitis in mice." This article discussed the efficacy of Ore`s lead drug candidate, ORE1001 (formerly GL1001), in the dextran sodium sulfate animal screening model for inflammatory bowel disease drugs. The results show that treatment with ORE1001 displayed efficacy on par with that of the oral standard, sulphasalazine. ORE1001 improved common measures of the extent of damage, such as histopathology, in a dose-related and statistically significant manner. Moreover, ORE1001 markedly decreased tissue myeloperoxidase activity, a well-known marker of inflammation. The findings, when considered along with other studies of ORE1001, support further development of the compound in gastrointestinal inflammatory conditions. ORE1001 has progressed through multiple dose clinical phase I testing in the U.S. and is on track to commence a Phase Ib/IIa trial in ulcerative colitis, one of the two main disorders that comprise inflammatory bowel disease (IBD), in the second half of 2009. It is estimated that up to one million Americans are affected by IBD. With typical onset in childhood or early adulthood, these disorders cause many decades of pain and suffering and result in significant lost productivity, in addition to the direct costs of medical and surgical care. The burden on the U.S. healthcare system alone is significant; IBD is associated with health care costs estimated at more than $1.7 billion. Ore believes that ORE1001, if approved, could represent a significant enhancement to current therapies for treating this debilitating disease. The print article is expected to be published in an upcoming issue of Inflammation Research. The full text article is currently available online at: http://www.springer.com/birkhauser/biosciences/journal/11. Ore Pharmaceuticals Overview Ore Pharmaceuticals Inc. (the "Company") is a pharmaceutical asset management company. The Company acquires interests in pharmaceutical assets whose value, it believes, it can significantly enhance through targeted development, with the goal of then monetizing these assets through a sale or out-licensing. Initially, the Company will focus on developing and monetizing its current portfolio, which includes four clinical-stage compounds in-licensed from major pharmaceutical companies. The Company`s four compounds in its development portfolio are: ORE1001, its lead compound, ORE10002, ORE5002 (tiapamil) and ORE5007 (romazarit). Safe Harbor Statement This press release contains "forward-looking statements," as such term is used in the Securities Exchange Act of 1934, as amended. Such forward-looking statements include our ability to identify strategies for making its businesses successful and the impact of such strategies on our business and financial performance and on shareholder value. Forward-looking statements typically include the words "expect," "anticipate," "believe," "estimate," "intend," "may," "will," and similar expressions as they relate to Ore Pharmaceuticals or its management. Forward-looking statements are based on our current expectations and assumptions, which are subject to risks and uncertainties. They are not guarantees of our future performance or results. Our actual performance and results could differ materially from what we project in forward-looking statements for a variety of reasons and circumstances, including particularly risks and uncertainties that may affect the Company`s operations, financial condition and financial results and that are discussed in detail in the our Annual Report on Form 10-K and our other subsequent filings with the Securities and Exchange Commission. They include, but are not limited to: whether the compounds we develop will be commercially viable; whether we will be able to begin to generate sufficient new revenue from licensing or other transactions early enough to support our operations and continuing compound development; whether there will be valid claims for indemnification from the buyers of our Genomics Assets; whether there will be claims from the landlords of the leased properties we have assigned, the buyer of our Preclinical Division or the assignee of our Cambridge facility lease, that we would be required to pay as guarantors of such leases; whether we will be able to collect amounts due under the terms of promissory notes from the buyers of our Genomics Assets and molecular diagnostic business; whether we will be able to manage our existing cash adequately and whether we will have access to financing on sufficiently favorable terms to maintain our businesses and effect our strategies; whether we will be able to maintain our NASDAQ listing; whether we will be able to attract and retain qualified personnel for our business; and potential negative effects on our operations and financial results from workforce reductions and the transformation of our business. Ore Pharmaceuticals Inc. undertakes no obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Ore Pharmaceuticals Inc. Benjamin L. Palleiko SVP & CFO 617-649-2001 bpalleiko@orepharma.com
Source: Reuters
Evotec Announces Research Agreement With Biogen Idec
Last Updated on Thursday, 8 October 2009 12:14 Written by Editor Thursday, 8 October 2009 12:14
HAMBURG, Germany and OXFORD, UK, Sept. 9, 2009 (GLOBE NEWSWIRE) -- Evotec AG (Frankfurt:EVT) (Nasdaq:EVTC), a leading provider in the discovery and development of novel small molecule drugs, today announced that it has entered into a research agreement with Biogen Idec (Nasdaq:BIIB), a leading biopharmaceutical company headquartered in Cambridge, Mass., USA. Evotec will use its expertise and technologies in protein production, assay development and high throughput screening to identify hit molecules for Biogen Idec. Under the research agreement Evotec will screen a target selected by Biogen Idec with the option to add further targets as agreed. Evotec will provide Biogen Idec with access to its full range of screening technologies and diverse library of high quality compounds and will use its expertise in protein production and assay development to develop new assays for the target. Dr. Mark Ashton, Evotec's EVP, Business Development commented: "We believe that the quality of future drug candidates is very much dependent on the identification of high quality starting points. To this end we have established a platform of screening technologies that have been proven to identify high-class hit molecules. We are looking forward to working with Biogen Idec and identifying interesting hit compounds for them." Evotec has built a comprehensive platform of hit finding technologies that allow it to screen challenging targets and identify new classes of hit compounds that can be progressed towards new treatments for various diseases. These proven screening technologies coupled with Evotec's high quality screening library have been shown to unlock numerous biological targets and identify excellent start points for subsequent optimization. No financial details are disclosed. About Evotec AG Evotec is a leader in the discovery and development of novel small molecule drugs. The Company has built substantial drug discovery expertise and an industrialized platform that can drive new innovative small molecule compounds into the clinic. In addition, Evotec has built a deep internal knowledge base in the treatment of diseases related to neuroscience, pain, and inflammation. Leveraging these skills and expertise the Company intends to develop best-in-class differentiated therapeutics and deliver superior science-driven discovery alliances with pharmaceutical and biotechnology companies. Evotec has long-term discovery alliances with partners including Boehringer Ingelheim, CHDI, Novartis, Ono Pharmaceutical and Roche. The Company has a P2X7 antagonist for the treatment of inflammatory diseases in clinical development and a series of preclinical compounds and development partnerships, including a strategic alliance with Roche for EVT 101, a subtype selective NMDA receptor antagonist, for use in treatment-resistant depression. For additional information please go to www.evotec.com Forward-looking statements Information set forth in this press release contains forward-looking statements, which involve a number of risks and uncertainties. Such forward-looking statements include, but are not limited to, statements about our expectations and assumptions concerning regulatory, clinical and business strategies, the progress of our clinical development programs and timing of the results of our clinical trials, strategic collaborations and management's plans, objectives and strategies. These statements are neither promises nor guarantees, but are subject to a variety of risks and uncertainties, many of which are beyond our control, and which could cause actual results to differ materially from those contemplated in these forward-looking statements. In particular, the risks and uncertainties include, among other things: risks that the Company may be unable to reduce its cash burn through recent restructuring and cost containment measures and may not recognize the results of such measures within the expected timeframe; risks that product candidates may fail in the clinic or may not be successfully marketed or manufactured; the risk that we will not achieve the anticipated benefits of our collaborations, partnerships and acquisitions in the timeframes expected, or at all; risks relating to our ability to advance the development of product candidates currently in the pipeline or in clinical trials; our inability to further identify, develop and achieve commercial success for new products and technologies; the risk that competing products may be more successful; our inability to interest potential partners in our technologies and products; our inability to achieve commercial success for our products and technologies; our inability to protect our intellectual property and the cost of enforcing or defending our intellectual property rights; our failure to comply with regulations relating to our products and product candidates, including FDA requirements; the risk that the FDA may interpret the results of our studies differently than we have; the risk that clinical trials may not result in marketable products; the risk that we may be unable to successfully secure regulatory approval of and market our drug candidates; and risks of new, changing and competitive technologies and regulations in the U.S. and internationally. The list of risks above is not exhaustive. Our most recent Annual Report on Form 20-F, filed with the Securities and Exchange Commission, and other documents filed with, or furnished to the Securities and Exchange Commission, contain additional factors that could impact our businesses and financial performance. We expressly disclaim any obligation or undertaking to release publicly any updates or revisions to any such statements to reflect any change in our expectations or any change in events, conditions or circumstance on which any such statement is based.
Source: Reuters
KINAXO launches KinAffinity® services for efficient profiling of kinase inhibitors in cells or tissue
Last Updated on Thursday, 8 October 2009 10:53 Written by Editor Thursday, 8 October 2009 10:53
Martinsried, Germany, October 01, 2009 / b3c newswire / - KINAXO Biotechnologies GmbH announced today that it added KinAffinity® to its service portfolio. KinAffinity® provides invaluable information about a kinase inhibitor’s selectivity in a cell or tissue of interest. It simultaneously determines affinities for native kinases expressed within a cellular proteome and thus overcomes the limitations of traditional biochemical assays that only use recombinant proteins.
Kinase inhibitors with favorable pharmaceutical properties are extensively pursued as therapeutics in numerous oncological, neurological and inflammatory indications. However, their development faces significant challenges such as target specificity for the disease-relevant target proteins. Here, KinAffinity® provides critical information to select the right lead compound for clinical development.
KinAffinity® combines proprietary chemical proteomics methods with state-of-the-art quantitative mass spectrometry (see Sharma et al., Nature Methods 2009). Endogenously expressed, post-translationally modified kinases are enriched by a ready-to-use affinity matrix in the presence of native binding partners and competed with the kinase inhibitor of interest. Subsequently, bioinformatic methods are used to reveal the inhibitor’s quantitative cellular target profile. The inhibitor’s targets are ranked by their affinities and reported to the customer.
KinAffinity® is applicable for type I and type II kinase inhibitors. It facilitates selectivity analysis on an organism level that accounts for differences in protein expression between different cells, as well as their mutational and modification status that might affect drug binding.
Link to the news release
About KINAXO – www.kinaxo.com
KINAXO Biotechnologies GmbH is a privately-held biotechnology company based in Munich/Martinsried, Germany. As a spin-off of the Max Planck Institute of Biochemistry in Martinsried, we closely cooperate with several of the Institute’s most outstanding scientists in the field of chemical proteomics and quantitative mass spectrometry, namely Dr. Henrik Daub, Prof. Jesper Olsen and Dr. Jürgen Cox. KINAXO’s technology portfolio delivers direct insights into a compound’s cellular interactions and its mode of action and is routinely applied to decrease drug development times and improve therapeutic strategies. To expand its KinAffinity® platform, KINAXO recently received financial funding from the Bavarian Ministry of Economics. The underlying technology was licensed from the Max Planck Society and co-developed by scientists of the Max Planck Institute of Biochemistry and KINAXO’s scientists.
KINAXO has several ongoing collaborations with major pharmaceutical and biotechnology companies such as Boehringer Ingelheim, Johnson & Johnson and Bayer, and is financed by European investors BioM, High-Tech Gründerfonds, KfW, the Max Planck Society, and Mountain Partners.
Source:Â B3C Newswire
Posted under Drug Development, Drug-Like Compounds, Industry News, Press Releases, R & D | No Comments
Researchers develop screening test for cells that activate immune system
Last Updated on Wednesday, 26 August 2009 11:31 Written by Editor Wednesday, 26 August 2009 11:31
UT Southwestern Medical Center researchers are the first to design a large-scale, cell-based screening method that identifies which compounds activate immune-return cells that hold compact for prospective cancer-fighting vaccines.
The new screening technique can scan thousands and even millions of compounds to identify those that activate dendritic cells, which are on constant recon patrol throughout the body to scout out cancerous or infected cells and alert the immune system.
“Our assay is unique from other conventional ones in its sensitivity and cost- and time-efficiency,†said Dr. Akira Takashima, professor of dermatology and vice chairman for research and head of the project.
Dendritic cells (DCs) are considered key to developing future vaccines that can either mimic the body’s natural immune response or turn on immune responses that failed – due, for example, to cancer or an immune deficiency.
The team, which also included Dr. Norikatsu Mitzumoto, assistant professor of dermatology and the study’s lead author, and Drs. Hironori Matsushima and Hiroaki Tanaka, postdoctoral researchers in dermatology, created the cell-based biosensor system.
“We basically engineered DCs to express a fluorescent signal only when sensing activation signals so that you can identify immuno-stimulatory agents very easily,†said Dr. Takashima. Immuno-stimulatory agents launch the immune system.
The research appears on Blood magazine’s online Web site and will appear in a future issue.
“We have optimized the high-throughput screening capability – an experienced scientist can now test one thousand chemicals a day almost single-handedly,†added Dr. Mizumoto. Previously, scientists would have to test each compound individually, a time-consuming process.
Their research already has led to the discovery of several compounds that turn on dendritic cells, which are found throughout the body from skin to blood. They continuously scan the body at the cellular level looking for antigens – foreign cells and materials invading the body – and for molecular signatures of tissue damage or infection.
“Their primary job is to present antigens to the immune system so that you develop protective immunity for infection and cancer,†said Dr. Takashima.
The DC biosensor system should help pharmaceutical and biotech companies sift through large numbers of chemicals for ones that tell the dendritic cells to launch the immune response. It may also prove useful in identifying biothreat agents because it detects infectious pathogens with high sensitivity.
Dr. Takashima said he hopes to garner additional funding to discover potent immuno-stimulatory drugs by screening high-quality libraries of compounds.
Doing so may be the first step toward developing a new class of vaccines that force or trick the natural immune system to kick on, or initiate an immune response that can be copied and initiated artificially.
Other UT Southwestern researchers from dermatology involved in the study were Dr. Yasushi Ogawa, postdoctoral researcher, and Dr. Jimin Gao, former instructor.
The research was funded by the National Institutes of Health, the Dermatology Foundation Career Development Award and the American Cancer Society Junior Investigator Award.
http://www.utsouthwestern.edu/
Research and Markets: Accelerating Lead Generation: Emerging Technologies and Strategies
Last Updated on Monday, 24 August 2009 11:30 Written by Editor Monday, 24 August 2009 11:30
(live-PR.com) – DUBLIN, Ireland (Research and Markets) – Research and Markets (www.researchandmarkets.com/research/fb1566/accel ..) has announced the addition of the “Accelerating Lead Generation: Emerging Technologies and Strategies” report to their offering.
The number of approvals for new drugs and biologics has fallen steadily in recent years, despite increasing R&D expenditure. Cost effective and innovative approaches to drug discovery and development have therefore become particularly important
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to ensure shareholder value. Improvements to the lead generation process are a key initiative for company's aiming to avoid expensive compound failures in the latter stages of the drug discovery process.
Accelerating Lead Generation: Emerging technologies and strategies' is a report that provides an in-depth examination of state-of-the-art technologies for lead generation. This report assesses the potential of new and emerging technologies for improving the quality of drug candidates entering clinical research, and reviews the benefits associated with different approaches to lead generation, including high throughput screening, fragment based drug discovery and virtual screening. The lead generation strategies adopted by leading pharma companies are evaluated to provide strategic recommendations for success, and the trends that are shaping the future acceleration of lead generation are identified.
Key Findings:
- Truly novel molecules are far more likely to be identified during the optimization process through the manipulation of structures than through screening. Methods include forming a new ring structure within a compound (or opening one out), the replacement of functional groups with bioisosteres and scaffold-hopping. Emerging methods for scaffold hopping based on force fields are growing in popularity.
- Virtual screening and fragment-based drug discovery will complement HTS-generated data rather than replacing it. The low cost of virtual screening and its potential for improving library design means that large screens can be carried out in the earliest stages of drug discovery. Conversely, it is best to apply fragment-based drug discovery to targets for which quality structural information is readily available.
- New technologies that replace fluorescence-based or radioligand displacement assays are growing in throughput and are being rapidly introduced across the industry. Innovations that improve the throughput and sensitivity of label-free technologies are either introducing them to drug discovery as secondary assays, or promoting secondary assay technologies to primary versions.
- Improved methods for handling data, multiplexing assays, and using primary cells, 3D cell culture or stem cell derived populations will increase the physiological relevance of data collected. Novel in vivo models, such as zebrafish and whole animal imaging may also provide additional data.
Use this report to...
- Analyse the potential of emerging technologies for improving the quality of drug candidates and understand how such innovations can improve the ability of fragment based drug discovery and virtual screening to identify new lead compounds.
- Explore recent developments in high throughput screening with this report's analysis of innovations in biological assay development, including improvements in vitro assays, cell-based assay technology and in-vivo methods for lead generation.
- Examine the role of ADME and toxicology in accelerating lead generation with this report's analysis of innovations in the assessment of ADME characteristics and toxicology at the lead generation stage.
- Evaluate the lead generation strategies of major companies with this report's case study analysis of Bayer, Boehringer Ingelheim, Millennium Pharmaceuticals (Takeda), and understand the importance of R&D models, academia collaborations and technological innovations to lead generation success.
Key Topics Covered:
Chapter 1 Introduction
Chapter 2 Identifying hits: library design, virtual screening and fragment based drug discovery
Chapter 3 Innovations in biological assay development
Chapter 4 ADME and toxicology in lead generation
Chapter 5 Lead generation strategies in the pharma industry
Chapter 6 R&D models, innovation & future success of lead generation
Chapter 7 Appendix
Companies Mentioned:
- Bayer
- Boehringer Ingelheim
- Millennium Pharmaceuticals (Takeda)
For more information visit www.researchandmarkets.com/research/fb1566/accel ..
Source: Business Insights
Posted under Compound Screening, Press Releases, R & D | No Comments
Nuevolution Announces Worldwide Technology Cross-Licensing Agreement With GSK
Last Updated on Monday, 24 August 2009 11:11 Written by Editor Monday, 24 August 2009 11:11
COPENHAGEN, Denmark, July 28 /PRNewswire/ — Nuevolution today announced the execution of a worldwide technology cross-licensing agreement with GlaxoSmithKline.
The agreement relates to a number of patented technologies for rapid synthesis and DNA-tagging of hundreds of millions of chemically diverse drug-like small molecule compounds and the efficient screening of these, facilitating the identification of potent drug leads. These technologies were developed by Nuevolution and Praecis Pharmaceuticals, a wholly owned subsidiary of GlaxoSmithKline.
Under the terms of the cross-licensing agreement, GlaxoSmithKline will obtain a non-exclusive license under technology patents of Nuevolution, and Nuevolution will obtain a one time license fee and a non-exclusive license under technology patents of GlaxoSmithKline.
Further details of the agreement are not disclosed.
“By entering into this agreement, both companies are offered an optimal basis for continued development and application of the technologies” said Allen Oliff, SVP Molecular Discovery Research of GSK and Alex Gouliaev, CEO of Nuevolution A/S continued “our innovative technologies allow small molecule hit and lead discovery at an unprecedented scale. This agreement secures both companies the rights to operate these powerful technologies to their fullest extent”.
About Nuevolution
Nuevolution is a leading lead discovery company founded in 2001 and based in Copenhagen, Denmark. The company has developed Chemetics(R), a unique, patent protected hybrid of proven wet chemistry and molecular biology which represents the ultimate fragment based lead discovery technology. Chemetics(R) enables rapid synthesis and DNA-tagging of hundreds of millions of chemically diverse drug-like small molecule compounds and the efficient screening of these, facilitating the identification of potent drug leads at unprecedented quantity, quality and speed compared to existing lead discovery technologies.
Nuevolution partners its technology with pharmaceutical and biotechnology companies, and is also developing an internal pipeline by applying Chemetics(R) to validated cancer and cardiovascular targets. Nuevolution has demonstrated the power of Chemetics(R) by identifying highly potent and drug like novel ligands with the potential to address major unmet medical needs across a range of therapeutic areas and target classes.
Nuevolution is a privately owned company and has raised EUR 37 million in financing from key Scandinavian investors, including SEB Venture, Sunstone Capital, SLS Invest and Novo A/S. For more information about Nuevolution A/S, please visit the company’s website http://www.nuevolution.com
Posted under Business and Investment, Collaborations, Drug Development, Europe, Press Releases, R & D | No Comments
Drug Approvals, Natural And Unnatural
Last Updated on Friday, 21 August 2009 01:16 Written by Editor Friday, 21 August 2009 01:16
I seem to have been putting a lot of graphics up this week, so here’s another one. This is borrowed from a recent Science paper on the future of natural-products based drug discovery. It’s interesting both from that viewpoint, and because of the general approval numbers:

And there you have it. Outside of anomalies like 2005, we can say, I think, that the 1980s were a comparative Golden Age of Drug Approvals, that the 1990s held their own but did not reach the earlier heights, and that since 2000 the trend has been dire. If you want some numbers to confirm your intuitions, you can just refer back to this.
As far as natural products go, from what I can see, the percentage of drugs derived from them has remained roughly constant: about half. Looking at the current clinical trial environment, though, the authors see this as likely to decline, and wonder if this is justified or not. They blame two broad factors, one of them being the prevailing drug discovery culture:
The double-digit yearly sales growth that drug companies typically enjoyed until about 10 years ago has led to unrealistically high expectations by their shareholders and great pressure to produce “blockbuster drugs” with more than $1 billion in annual sales (3). In the blockbuster model, a few drugs make the bulk of the profit. For example, eight products accounted for 58% of Pfizer’s annual worldwide sales of $44 billion in 2007.
As an aside, I understand the problems with swinging for the fences all the time, but I don’t see the Pfizer situation above as anything anomalous. That’s a power-law distribution, and sales figures are exactly where you’d expect to see such a thing. A large drug company with its revenues evenly divided out among a group of compounds would be the exception, wouldn’t it?
The other factor that they say has been holding things back is the difficulty of screening and working with many natural products, especially now that we’ve found many of the obvious candidates. A lot of hits from cultures and extracts are due to compounds that you already know about. The authors suggest that new screening approaches could get around this problem, as well as extending the hunt to organisms that don’t respond well to traditional culture techniques.
None of these sound like they’re going to fix things in the near term, but I don’t think that the industry as a whole has any near-term fixes. But since the same techniques used to isolate and work with tricky natural product structures will be able to help out in other areas, too, I wish the people working on them luck.
Posted under Business and Investment, Drug Development, R & D, Reports | No Comments
CytRx Unveils Clinical Development Plan for Pipeline Assets
Last Updated on Friday, 12 December 2008 02:47 Written by Editor Friday, 12 December 2008 02:47
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.â€
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.â€
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.â€
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.
Green protein inhibits Alheimer’s, CSIRO scientists find
Last Updated on Thursday, 20 November 2008 03:42 Written by Editor Thursday, 20 November 2008 03:42
BY NYSSA SKILTON
MEDICAL REPORTER
18/11/2008
CSIRO scientists have developed a way to screen for compounds that can inhibit the progression of Alzheimer’s disease.
The system involves using live yeast and a protein called Abeta fused to a fluorescent green protein, which comes from jellyfish.
The scientists, working within CSIRO’s Preventive Health Flagship, published their findings in the latest edition of the Journal of Alzheimer’s Disease.
Alzheimer’s disease is the fourth leading cause of death in people older than 65 and there is no cure known to science.
It is thought to be the result of a loss of neurons in the brain, caused by a process in which toxic forms, known as multimers, of the small Abeta protein are created.
Lead author Ian Macreadie said the scientists had discovered a ”rapid screening system” to identify inhibitors of this process.
”Compounds that inhibit the formation of the toxic multimers may lead to the prevention or delay of the disease,” Dr Macreadie said.
”The yeast trial we developed could lead to the discovery of new agents which may prove useful in preventing or delaying the onset of Alzheimer’s disease.”
The researchers tested their screening system using folate, a nutrient known to protect against Alzheimer’s disease. They found that the folate made the yeast with the jellyfish protein greener.
The green colour signifies that the additive, in this case the folate, has stopped the Abeta protein from changing into its toxic forms.
”The greener the better,” Dr Macreadie said. ”We’re interested in finding not just folate, but many existing compounds and novel compounds that may be helpful in [combating] Alzheimer’s.”
The researchers have already screened hundreds of compounds in the search for Alzheimer’s inhibitors. They plan to screen foods to identify nutrients they may use to enrich foods to protect consumers.
InhibOx and the National Foundation for Cancer Research Announce Launch of DrugFinder
Last Updated on Wednesday, 1 October 2008 03:52 Written by Fred Wednesday, 1 October 2008 03:52
Posted under Business and Investment, Europe, Press Releases, R & D | No Comments
Pfizer, Lilly, and Merck & Co. Seed Firm with $39M to Challenge High Attrition Rates in R&D
Last Updated on Tuesday, 15 July 2008 03:04 Written by Fred Tuesday, 15 July 2008 03:04
Pfizer, Eli Lilly, Merck & Co. are investing $39 million to form a company to address the issue of high attrition rates in drug development. The new entity, Enlight Biosciences, has been cofounded by PureTech Ventures and academic researchers.
Enlight will develop technologies in a precompetitive model according to what its founding members require. All three firms will have access to any technology or tests developed.
Enlight Biosciences has reportedly already begun studies in molecular imaging, biologics, and drug delivery. The company will work on technologies that: increase the likelihood of success for drugs that pass early development milestones, help with early prediction of human response, provide accurate readouts of animal and human response to intervention, such as molecular imaging and biomarkers, and make promising chemical and biological compounds better suited to human treatment in terms of formulation and drug delivery.
Technologies that can better predict the right candidates for development and thus make Phase III evaluations more predictable often lose out on investment dollars, PureTech points out. In spite of strides made in this area of technology development for drug R&D, such as PCR, RNAi, and high-throughput screening, the industry still struggles with compounds failing in late-stage trials after billions of dollars have been invested.
“At a time when there is concern over productivity in R&D, Enlight Biosciences is providing a safe haven where leaders in the pharmaceutical industry can develop tools that will accelerate innovation and delivery of novel drugs to patients,†states Frank Douglas, M.D., Ph.D., PureTech Ventures Partner.
Posted under Business and Investment, Collaborations, North America, Press Releases, R & D | No Comments
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