biocrea?s first-in-class PDE2 inhibitor demonstrates strong potential for the treatment of cognitive disorders
Data on novel PDE2 inhibitor BCA909 presented at 24th ECNP Congress in Paris
Radebeul, Germany, September 7, 2011 – biocrea, a biopharmaceutical company focusing on novel treatments for disorders of the central nervous system (CNS), today announced data on its innovative CNS-penetrating PDE2 inhibitor. The compound, which is code-named BCA909, was selected as a preclinical candidate earlier this year. It demonstrates strong potential for the treatment of diseases in which normal learning and memory is impaired, e.g. mild cognitive impairment, Alzheimer’s disease and schizophrenia. Details on the compound were presented at the 24th ECNP Congress of the European College of Neuropharmacology in Paris, France (Sept. 3-7, 2011).
To date, few PDE2 inhibitors have been pharmacologically characterized. While initial findings have been encouraging, suggesting pro-cognitive and anxiolytic efficacy, the compounds did not enter the brain in sufficient quantities. With BCA909, biocrea has developed a novel, potent and selective PDE2 inhibitor with excellent CNS penetration and an efficacy and safety profile suitable for further development for multiple disease indications.
During the ECNP congress, biocrea presented data from extensive preclinical studies in vitro and in animal models of learning and memory. The key findings demonstrate that BCA909 delivers significant pro-cognitive activity in models of cognitive impairment resulting from either disruption of cholinergic or glutamatergic neurotransmission. Furthermore, BCA909 does not induce tolerance, indicating that maintained pro-cognitive efficacy, achieved through modulation of multiple neurotransmitter systems, can be delivered by the novel PDE2 mechanism of action.
“Phosphodiesterases catalyze the degradation of intracellular cyclic nucleotides, such as cAMP and/or cGMP, which regulate, among others, ion channels crucial for the proper functioning of the central nervous system,” said Martin Gunthorpe, CSO of biocrea. “Our data support the hypothesis that the positive effect of our PDE2 inhibitor on cognition is due to the elevation of intracellular cyclic nucleotide levels, which results in strengthened synaptic plasticity, a hallmark of learning and memory at the cellular level.”
Tom Kronbach, CEO of biocrea, added: “These data, combined with the demonstrated efficacy of BCA909 in models of anxiety and depression, highlight that biocrea’s PDE2 inhibitors have the potential to become first-in-class compounds with a superior profile compared to currently available treatment options for a range of debilitating diseases, in which patients suffer marked cognitive impairment.”
Preclinical development of BCA909 is ongoing.
biocrea focuses on the discovery and development of novel drugs for the treatment of debilitating CNS diseases such as schizophrenia, memory impairment and Chorea Huntington. biocrea’s key expertise lies in the discovery and optimization of selective ion channel and enzyme modulators.
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. Previous collaborators of the biocrea team include GlaxoSmithKline, Wyeth and 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 human life and health. Therefore, they can also play a role in the onset and progress of various diseases. 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 and Huntington´s disease. Brain penetrating PDE inhibitors therefore offer a novel approach for the treatment of these debilitating diseases.
So far, it has been difficult to apply PDE inhibitors in CNS diseases because access to brain PDEs is limited by the so-called blood brain barrier. 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
Tel.: +49 351 / 4043 3332
Fax: +49 351 / 4043 3216
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Posted: September 2011