Heptares will receive up-front payments and up to $190 million in milestones.

Shire is paying Heptares up-front fees and potentially $190 million in milestones to exercise its option for an exclusive worldwide license to the latter’s preclinical-stage adenosine A2A receptor antagonist candidate, which is in development for the potential treatment of CNS disorders.

Heptares is focused on the development of drugs targeting G-protein-coupled receptors (GPCRs). The firm is exploiting an integrated discovery platform that includes technologies for engineering stabilized GPCRs (known as StaRs®) in their native conformations, and the identification of new ligand-interaction sites and screening for drug candidates. In January the firm reported publication of research papers describing how its technologies were used to stabilize the A2A receptor, enabling the application of structure-based drug discovery techniques including its Biophysical Mapping™ technique, fragment screening, and x-ray crystallography to the receptor. The surface plasmon resonance-based BioPhysical Mapping technique allows for the 3-D determination of compound-binding to facilitate the design of drug candidates.

“We are impressed with the novelty and quality of the A2A antagonist leads generated by Heptares, resulting from what we believe to be the first time a structure-based drug discovery approach has been applied from the beginning to a GPCR drug target,” comments Jeff Jonas, svp for R&D, specialty pharmaceuticals and regenerative medicine at Shire. “This agreement with Heptares is a reflection of our growth strategy of investing and focusing on highly targeted drug discovery platforms.”

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