Shire gets exclusive option for Heptares A2A program for CNS diseases

10 May 2011

Closely-held UK-based drug discovery firm Heptares Therapeutics says it has signed an exclusive option agreement with Ireland-headquartered Shire (LSE: SHP) for a novel adenosine A2A antagonist discovered by Heptares and currently in preclinical development.

Adenosine A2A is a G-protein coupled receptor (GPCR) involved in the regulation of dopaminergic pathways in the brain. Recently, inhibition of the A2A receptor has been proved to be clinically effective in treating symptoms of Parkinson’s disease and may offer benefits in additional CNS diseases.

The Heptares A2A program reflects a new approach to this GPCR target. Heptares stabilized the A2A receptor using its proprietary StaR technology, determined the receptor’s binding characteristics through Biophysical Mapping, and resolved its 3D crystal structure using x-ray crystallography. This advanced knowledge of the target enabled Heptares scientists to discover entirely new types of chemical structures for inhibiting the A2A receptor.

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