Heptares Therapeutics Grants Shire an Exclusive Option to License Novel Adenosine A2A Antagonist

Monday, May 9, 2011 Drug News
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WELWYN GARDEN CITY, England, May 9, 2011 /PRNewswire/ --

- Best-in-Class Candidate With Potential in Treatment

of CNS Diseases

Heptares Therapeutics today announced it has signed an exclusive option agreement with Shire Pharmaceuticals 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 programme reflects a new approach to this GPCR target. Heptares stabilised the A2A receptor using its proprietary StaR(R) technology, determined the receptor's binding characteristics through Biophysical Mapping(TM), 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.

Under the terms of the agreement, Heptares has granted Shire an exclusive option, upon completion of certain preclinical studies, to license worldwide development and commercial rights to the Heptares A2A programme. Heptares has received an upfront payment and is eligible, upon exercise of the option by Shire, to an option exercise payment, future milestone payments, plus royalties on product sales. Further terms of the agreement are not being disclosed.

"We are excited to sign this option agreement with Shire for the development of our novel A2A antagonist, a potentially best-in-class new agent for treating patients suffering from debilitating CNS diseases," said Malcolm Weir, CEO of Heptares. "A2A is an important and clinically validated GPCR drug target, yet it has never been adequately addressed by the available older chemistries. Heptares has discovered fundamentally novel chemotypes as the basis for a new and, we believe, superior approach to A2A receptor pharmacology."

About Heptares Therapeutics

Heptares is a drug discovery company creating new medicines targeting G-protein-coupled receptors (GPCRs). The Company is currently leveraging its GPCR expertise and proprietary StaR(R) technology to build a pipeline of best-in-class and first-in-class GPCR-targeted medicines for the treatment of CNS, metabolic and other diseases.

GPCRs represent the single most important family of drug targets in the human body, yet, due to their inherent instability when removed from cell membranes, little or no structural information about these valuable targets has been available to drive structure-based drug discovery programmes. Heptares' StaR(R) (Stabilised Receptor) technology enables the first-ever thermo-stabilisation of GPCRs. This breakthrough allows Heptares scientists to resolve GPCR structures and deploy structure-based drug discovery techniques to identify potent and selective drug candidates to previously undruggable targets.

Heptares has raised more than $40 million from leading venture investors, Clarus Ventures, MVM Life Science Partners, Novartis Option Fund and Takeda Ventures, and has formed partnerships with Shire, Takeda and Novartis.

For additional information, please visit: http://www.heptares.com

For information on Shire, please visit the Company's website: http://www.shire.com

    Contact Information

    Heptares Therapeutics Ltd         +44-(0)1707-358-629
    Dr Malcolm Weir, CEO              malcolm.weir@heptares.com
    Dr Barry Kenny, CBO               barry.kenny@heptares.com

    Citigate Dewe Rogerson            +44(0)20-7282-2948
    Dr Mark Swallow, Dr Chris Gardner mark.swallow@citigatedr.co.uk

SOURCE Heptares Therapeutics


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