News

Company News: biocrea and Pfizer Jointly Presented Details on Novel PDE10 Inhibitors at the 241st ACS National Meeting & Exposition

– Novel treatment opportunities for CNS diseases –

biocrea, a biopharmaceutical company focusing on novel treatments for disorders of the central nervous system (CNS), today reported details on the design and synthesis of novel, brain-penetrating phosphodiesterase-10 (PDE10) inhibitors developed in collaboration with Pfizer Inc. (NYSE: PFE). The data were featured in joint presentations[1] with Pfizer at the recent 241st ACS National Meeting & Exposition, an event organized by the American Chemical Society (ACS).

The data demonstrated that the scientists at Pfizer and biocrea were able to eliminate undesired activity on adenosine receptors and to considerably improve the compounds´ physicochemical properties and potency. The team had started with initial high-throughput hits characterized by low potency and selectivity. Further lead optimization led to a number of compounds with very robust activity in a range of preclinical models of anti-psychotic efficacy. Moreover, these PDE10 inhibitors produced low levels of catalepsy, suggesting a minimal risk for the induction of side-effects involving the extrapyramidal system (EPS), the most common adverse reaction observed with anti-psychotic drugs.

Phosphodiesterases (PDEs) have been identified as key regulators of intracellular cyclic nucleotide levels in the brain. Mechanistically, PDE10 inhibition has two major benefits, mimicking, (1) the effects of antagonists of the dopamine-2 receptor, the current standard treatment for psychosis, and (2) the effects of agonists of dopamine-1 receptors, which may decrease the side-effect liabilities while contributing to a pro-cognitive profile.

 

[1] Malamas M et al., 241st ACS National Meeting & Exposition Abstract 65 – Imidazo[1,5-a]quinoxalines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/Qr3C; Malamas, M. et al., 241st ACS National Meeting & Exposition Abstract 66 – Benzo[e]imidazo[5,1-c][1,2,4]triazines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/pl1Q


Food for Thought: Weekly Wrap-Up

In Frankfurter Allgemeine Zeitung (FAZ) Martina Lenzen-Schulte this week reports about an oncology symposion in Wiesbaden/Germany that dealt with oncology patients increasingly turning towards alternative medicines – 40 to 70% according to recent estimates. Oncologists now start to notice they cannot ignore patents’ needs and hopes, and therefore a number of clinicians have turned to looking at available studies on complementary medicine to separate the wheat from the chaff. However, it turns out that many of these studies – on mistletoe therapy as well as on dietary recommendations – are insufficient to provide sound evidence.

Werner Bartens in Sueddeutsche Zeitung features a 3,700 patients study published in the Journal of the American Medical Association demonstrating that contrary to common wisdom low salt diets increase the risk of heart attacks and stroke.

In Wirtschaftswoche, Susanne Kutter introduces the Diapat diagnostic test developed by German biotech company Mosaiques DiaPat GmbH that analyses more than 6,000 different peptide and protein molecules in human urine in one run. The test can be used to diagnose and even predict the onset of diseases. It has just been approved by FDA for the diagnosis of renal diseases. Already, the company markets a prostate cancer urine test in Germany. Mosaique’s test, Kutter claims, is but one of the many achievements to come from proteomics. She adds that the tests will have the potential to save the healthcare system billions of Euros.

Haydn Shaughnessy in Forbes states the record of cancer treatment still looks poor, with cancer mortality not improving a lot – as for example compared to heart diseases. Likewise, many preventive measures such as exercise and low fat diets don’t work. Shaughnessy therefore makes the case to support crowdsourcing approaches to develop a cancer cure like Pink Army and Cancer Commons (see akampioneer’s earlier entry on Open Source Principles – a Concept for the Life Sciences?). Also in Forbes, Matthew Herper forecasts that Pfizer will break itself up and spin out companies soon.

Eric Pfanner in New York Times looks at new European ventures to fill a void in world news after so many news organizations are laying off journalists or closing shop. As examples, he introduces Worldcrunch, a web-based start-up translating newspaper articles from around the world into English and Presseurop which translates into other languages, too.

In the New Scientist Jessica Hamzelou writes that people easily distracted might have more grey matter in their brains than focused people. In a separate article, she also features a pacemaker-like, implantable device that can deliver timed doses of medications for a year. Boonsri Dickinson, also in New Scientist, interviews nobelist Eizabeth Blackburn, the co-discoverer of the telomerase enzyme and its role in aging. Blackburn co-founded biotech company Telome Health, which is now starting to sell a test for telomere length. While at present it is sold for research purposes, e.g. to know more about telomer length as markers of aging, the test will be offered to the public through physicians for $200 later this year. Ferris Jabr in New Scientist introduces an approach fastening nanocapsules filled with interleukins to T cells as a way to cure cancer. So far, it seems to work in mice.

And here our favorite quote from Matthew Herper’s blog, who recently mused about whether entrepreneurs share some genetic characteristics, and if so, whether one could invent an antibody to turn someone into an entrepreneur: “‘Entrepreneur Antibody:’ Serious Side Effects Might Include Visual Hallucinations of Venture Capital.”

And finally, Norbert Lossau in Die Welt features a study by LinkedIn into the most common given names of CEOs, finding that in Germany they are Wolfgang, Christoph and Michael. In France, Gilles is number one, while it is Charles in the UK, Ray in Canada, Guido in Italy and Howard in the US. Marketing people often have short names like Chip, Todd or Trey, while engineers seem to have much longer give names. So think twice before naming your next newborn!

Company News: bubbles & beyond Expands Into I&I Sector, Signs Agreement with JNC Corporation

bubbles & beyond, a technology company focusing on customized intelligent fluids™, and the Japanese chemicals company JNC Corporation (formerly CHISSO) today announced an exclusive development collaboration on novel cleaning and stripping solutions for microelectronic devices.

Under the agreement, bubbles & beyond and JNC Corporation will jointly develop new solutions to facilitate and accelerate the complex cleaning processes for microelectronics. Within the next 18 months, both companies will identify and develop next-generation, sustainable cleaning and stripping agents suitable for the production of various microelectronics components, e.g. LCDs, OLEDs, plasma screens, motherboards, semiconductors, etc..

JNC Corporation receives an option to obtain the exclusive manufacturing and commercialization rights in Asia to any products resulting from the collaboration, while bubbles & beyond retains all product rights outside Asia. Moreover, bubbles & beyond receives alloted R&D payments during the collaboration.

Food for Thought: Moving Into the Clinic Without Animal Toxicity Tests

This month, MedNous provides an in-depth case study on an immune therapy developed by Immunocore Ltd. that won approval from the British and US regulators MHRA and FDA to start clinical trials on the basis of in-vitro safety studies only – without conducting any toxicity tests in animals.

The product in question, IMCgp100, is a monoclonal T cell receptor fused to an anti-CD3 single chain antibody fragment. The molecule is tricky in that both binding sites bind to human proteins and cells only. As a result, animal studies would have been without any predictive value. The company therefore had to design a reliable preclinical test for predicting the behavior of the drug in humans.

This has been a particular challenge as regulators still were digesting the shock from the TeGenero disaster in 2006, when six healthy volunteers almost died from cytokine storm in a Phase I clinical study of an immune therapy. Back then, the drug had been tested in animals and the volunteers received only a fraction of the dose that had been safely administered to monkeys.

After intense consultations with the regulators, Immunocore conducted a battery of tests on human cells to find out about potential cytokine release, cross-reactivity, etc. The company, too, tested whether hormones were able to shut done activity of the drug in case something would go wrong during the trials.

Trials are on the way already at three UK and two US sites in patients with metastatic melanoma and Immunocore hopes to have preliminary data, including some efficacy results, by 2012.

1 … 177 178 179 … 201