Heptares exercises exclusive option to license new A2A antagonist for CNS disorders

Heptares Therapeutics, the leading GPCR drug discovery company, announces that an operating company of Shire PLC (LSE: SHP, NASDAQ: SHPGY), the global specialty biopharmaceutical company, has exercised its exclusive option to license a novel adenosine A_2A antagonist discovered by Heptares that is currently in preclinical development. Adenosine A_2A is a G-protein coupled receptor (GPCR) involved in the regulation of dopaminergic pathways in the brain. Inhibition of the A_2A receptor is a validated mechanism in the treatment of CNS disorders.

Under the terms of the agreement Heptares grants Shire an exclusive licence to worldwide development and commercial rights to A_2Aantagonists discovered by Heptares. Heptares receives upfront option grant and exercise payments and is also eligible to receive future development and commercial milestone payments up to US$190 million plus royalties on product sales. Further terms of the agreement are not being disclosed.

Jeff Jonas, Senior Vice President, Research & Development, Specialty Pharmaceuticals and Regenerative Medicine, Shire, said:  "Shire is continuously in search of innovations that have the potential to help us develop well differentiated medicines that will bring value to patients. This agreement with Heptares is a reflection of our growth strategy of investing and focusing on highly targeted drug discovery platforms. We are impressed with the novelty and quality of the A_2A 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.  We look forward to a fruitful partnership with Heptares and to advancing the programme for the benefit of patients suffering from CNS disorders."

"The exercise of this option and initiation of the worldwide licensing agreement with Shire, one of the world's leading CNS specialty pharmaceutical companies, is an outstanding achievement for Heptares," said Malcolm Weir, CEO of Heptares. "The A_2A programme is the most advanced example of the Heptares drug discovery platform, and highlights our ability to deliver fundamentally novel chemotypes as a basis for first-in-class and best-in-class medicines addressing a broad range of diseases."

The Heptares A_2A programme reflects a new approach to this GPCR target. Recently published papers (refs 1-3) describe how Heptares technology was used to stabilise the A_2A receptor, enabling the application for the first time of structure-based drug discovery (SBDD) techniques including Biophysical Mapping™, fragment screening and x-ray crystallography to the receptor. The advanced knowledge of the target generated by this approach enabled Heptares scientists to discover entirely new types of chemical structures for inhibiting the A_2A receptor, potentially possessing best-in-class drug-like characteristics, a radical advance after decades of largely unsuccessful medicinal chemistry.