Heptares Provides GPCR Expertise to New European Drug Discovery Consortium

WELWYN GARDEN CITY, England and BOSTON, November 29, 2012 /PRNewswire/ --

Consortium supported with over €20 million funding from EU Innovative Medicines Initiative and big pharma

Heptares Therapeutics, the leading GPCR drug discovery company, is joining a group of leading European academic and industry researchers known as the 'K4DD' ('Kinetics for Drug Discovery') Consortium to investigate binding kinetics or 'kinotypic' properties of drug-receptor complexes. The five-year program will focus on important drug target classes, such as protein kinases, proteases and GPCRs - with the goal of demonstrating the value of kinotypic information to early drug discovery and to establish kinotype analysis as a routine part of the lead compound optimisation process.

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Heptares will provide stabilised GPCRs (StaRs®) to the consortium, as well as access to expertise and to its broader GPCR discovery platform, which makes the study of GPCR binding kinetics possible. In particular, Heptares' Biophysical Mapping™ technology has been designed and developed specifically to screen and study the binding kinetics of small molecules and antibody fragments in complex with StaRs®, making it a powerful tool for GPCR lead discovery and optimisation. In return, Heptares will receive grant funding from the EU, which will enable the Company to develop further its expertise and capabilities in this area.

The K4DD Consortium has been established based on the theory that, to date, drug discovery has focused on drug-receptor binding affinity and selectivity. However, finding new molecules that have high binding affinity and selectivity has not radically increased the chances of those molecules getting to market. New evidence suggests that 'target residence time' or the time a drug remains bound to its target may be as important as affinity or selectivity for its clinical effects.

The Consortium has been set up as part of the European Union's Innovative Medicines Initiative, and is funded with over €20 million from the EU and contributions from members of EFPIA (European Federation of Pharmaceutical Industries and Associations). The Consortium, which will be coordinated by Bayer Healthcare and Leiden University, will include 20 partners with expertise in structure elucidation, bioanalytical technologies, computational drug design and pharmacology from leading academic institutions, biotech companies and pharmaceutical companies across Europe.

"In its commitment to the K4DD programme, the EU and the pharmaceutical industry in Europe have recognised the importance of kinotypic information to lead optimisation and ultimately successful drug development," commented Fiona Marshall, Heptares Chief Scientific Officer. "Heptares' unique and powerful drug discovery capability makes it ideally placed to contribute to this exciting research programme, particularly as we have successfully used the optimisation of receptor kinetics in our GPCR-focused drug discovery programmes. We look forward to working with the other consortium partners to advance our collective understanding in this area and to develop the tools needed to improve the success rate of drug discovery and development."

About the Innovative Medicines Initiative (IMI)

IMI is the world's largest public-private partnership in health. IMI is improving the environment for pharmaceutical innovation in Europe by engaging and supporting networks of industrial and academic experts in collaborative research projects. The European Union contributes €1 billion to the IMI research programme, which is matched by in kind contributions worth at least another €1 billion from the member companies of the European Federation of Pharmaceutical Industries and Associations (EFPIA).

The Innovative Medicines Initiative is currently funding 37 projects, many of which are already producing impressive results. The projects all address major bottlenecks which will accelerate the development of safer and more effective treatments for patients.

The research leading to these results has received support from the Innovative Medicines Initiative Joint Undertaking under grant agreement no. 115366, resources of which are composed of financial contribution from the European Union's Seventh Framework Programme (FP7/2007-2013) and EFPIA companies' in kind contribution. More info: http://www.imi.europa.eu

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.  Our pharmaceutical partners include Shire, AstraZeneca, MedImmune and Takeda, and we are backed by MVM Life Science Partners, Clarus Ventures, Novartis Venture Fund and Takeda Ventures.

Heptares is pioneering the application of structure-based drug design to the GPCR superfamily of targets and is focused on creating molecules that modulate high-value, yet historically undruggable or challenging, GPCRs.  Our platform incorporates 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 have generated a broad pipeline of drug candidates for the treatment of serious disorders, including Alzheimer's disease, Parkinson's disease, schizophrenia, depression, chronic insomnia, addiction disorders, migraine and diabetes.  For more information about Heptares, please visit http://www.heptares.com.

SOURCE Heptares Therapeutics




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