Last updated on April 17, 2014 at 1:21 EDT

Heptares Grants Shire an Exclusive Worldwide Licence to Develop and Commercialise Novel Drug Candidate for CNS Disorders

March 19, 2012

WELWYN GARDEN CITY, England and BOSTON, Massachusetts, March 20, 2012 /PRNewswire/ –

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
A2A antagonist discovered by Heptares that is currently in preclinical development.
Adenosine A2A is a G-protein coupled receptor (GPCR) involved in the regulation of
dopaminergic pathways in the brain. Inhibition of the A2A 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 A2Aantagonists 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 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. 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 A2A
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 A2A programme reflects a new approach to this GPCR target. Recently
published papers (refs 1-3) describe how Heptares technology was used to stabilise the A2A
receptor, enabling the application for the first time of structure-based drug discovery
(SBDD) techniques including Biophysical Mapping(TM), 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 A2A receptor, potentially possessing best-in-class drug-like
characteristics, a radical advance after decades of largely unsuccessful medicinal

About Heptares Therapeutics

Heptares discovers and develops new medicines targeting GPCRs (G-protein-coupled
receptors), a super-family of drug targets linked to a wide range of human diseases. We
have established R&D collaborations with Shire, Takeda, AstraZeneca, MedImmune and
Novartis Option Fund, and have raised $40M in venture financing from MVM Life Science
Partners, Clarus Ventures, Novartis Venture Fund and Takeda Ventures. Heptares is an
industry pioneer in GPCR structure-based drug design and has built a unique capability for
discovering novel molecules that modulate historically undruggable or challenging GPCRs.
Our integrated discovery platform includes proprietary technologies for engineering
stabilised GPCRs in their natural pharmacological conformations, identifying previously
unknown chemistries for GPCR protein-drug interactions, and deploying advanced
fragment-based approaches to GPCR target space for the first time. Using this approach, we
are generating a broad pipeline of drug candidates for serious CNS and metabolic
disorders, including Alzheimer’s disease, Parkinson’s disease, schizophrenia, autism,
anxiety & depression, chronic insomnia, addiction and diabetes. For more information,
please visit http://www.heptares.com.


        1) Langmead, C. et al. (2012) J. Med. Chem. DOI: 10.1021/jm201455y.
          Published online: January 17, 2012
        2) Congreve, M. et al. (2012) J. Med. Chem. DOI: 10.1021/jm201376w. Published
          online: January 5, 2012
        3) Zhukov, A. et al. (2012) J. Med. Chem., 2011, 54 (13), pp 4312-4323

        Contact Information

        Citigate DeweRogerson (for Heptares)
        Mark Swallow, Chris Gardner
        +1 857-222-4586

        +44 (0)20-7282-2948

        Heptares Therapeutics Ltd

        Malcolm Weir, Chief Executive Officer (UK)
        +44 (0)1707-358-629

        Dan Grau, President (USA)

SOURCE Heptares Therapeutics

Source: PR Newswire