Radebeul, Germany, February 14, 2011 – biocrea, a biopharmaceutical company focusing on novel treatments for disorders of the central nervous system (CNS), today announced it has filed a patent application covering its brain-penetrating inhibitors of phosphodiesterases. These compounds constitute a new generation of promising drug candidates to address several CNS disorders that are currently lacking effective treatment options.
“Phosphodiesterases, or PDEs, are key regulators of brain signaling. Recently, PDEs have also been associated with a number of CNS diseases, and inhibiting certain PDEs in the brain bears great therapeutic potential for indications such as schizophrenia, depression, anxiety or movement disorders,” said Dr. Martin Gunthorpe, CSO of biocrea. “However, a lot of opportunities are still unexplored so far. Most attempts have failed to develop small molecule PDE inhibitors that easily penetrate the brain and act with sufficient specificity and efficacy. biocrea has pioneered the development of PDE2 and PDE10 inhibitors that overcome these limitations. Therefore, our compounds open an exciting avenue for novel treatment options for severe diseases of the central nervous system.”
This week, biocrea has submitted a patent application to the U.S. Patent Office (USPTO) covering compounds and uses of its proprietary PDE2 and PDE10 inhibitors.
While the inhibitors of PDE10 show excellent potential for the treatment of schizophrenia, Huntington’s disease and Tourette’s syndrome, the PDE2 inhibitors cover a whole spectrum of new biological activities and treatment opportunities. “As an example,” Gunthorpe said, “we have demonstrated in animal models that these compounds are able to significantly improve cognitive deficits and have therapeutic potential to treat depression and anxiety.”
Moreover, biocrea’s brain-penetrating PDE2 inhibitors show promise for the treatment of drug-induced movement disorders. “This constitutes a completely novel therapeutic approach for this indication, a common side effect of anti-psychotic medications,” Gunthorpe added.
biocrea’s patent application also comprises dual inhibitors of PDE2 and PDE10 as the combination of both modes of action in one molecule results in synergistic biological effects.
The most advanced compound of biocrea’s novel family of PDE inhibitors, a brain-penetrating, selective PDE2 inhibitor, has been selected to enter pre-clinical development.
biocrea focuses on the discovery and development of novel drugs for the treatment of debilitating CNS diseases such as schizophrenia, depression, and anxiety. biocrea’s key expertise lies in the discovery and optimization of selective ion channel and enzyme modulators, such as phosphodiesterases (PDEs).
The company has been established by seasoned experts with an exceptional track record in the biopharmaceutical industry (e.g. Asta Medica, Degussa, GlaxoSmithKline, Biotie Therapies). Among others, the team was involved in the discovery and development of the potassium channel opener retigabine and the development of a PDE10 inhibitor portfolio for the treatment of schizophrenia in collaboration with GlaxoSmithKline and Wyeth Pharmaceuticals, now Pfizer.
Following its incorporation in November 2010, biocrea is currently implementing a comprehensive partnering and licensing strategy.
Phosphodiesterases (PDEs) are key regulators of signal transduction. As such, they are fundamental in the performance and maintenance of our daily life and health. Phosphodiesterase inhibition can thus be exploited to treat a wide variety of diseases, e.g. chronic obstructive pulmonary disease (through inhibition of PDE4) or erectile dysfunction (through inhibition of PDE5). Recent studies have revealed a striking distribution pattern of PDEs in the brain, which implies a high therapeutic potential of certain PDEs (e.g. PDE2, PDE10) to treat diseases like schizophrenia, cognition impairment, Parkinson’s disease and more. Brain penetrating PDE inhibitors therefore offer a novel approach for the treatment of these debilitating diseases.
So far, validating the benefit of brain PDE inhibitors in CNS diseases has been difficult because access to brain PDEs is limited by the so-called "blood brain barrier" (BBB). The team of biocrea has overcome these limitations and developed brain-penetrating, highly specific PDE inhibitors that constitute a new generation of promising drug candidates for the treatment of CNS disorders.
Dr. Tom Kronbach CEO, biocrea Tel.: +49 351 / 4043 3332 Fax: +49 351 / 4043 3216