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 clinical 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.
About biocrea
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.
Visit biocra at http://www.biocrea.com/