Heptares Scientists to Receive the Malcolm Campbell Memorial Prize for 2015 in Recognition of Their Outstanding Contribution to GPCR Drug Discovery

LONDON and BOSTON, January 23, 2015 /PRNewswire/ --

Heptares Therapeutics, the clinical-stage GPCR structure-guided drug discovery and development company, is delighted to announce that the Malcolm Campbell Memorial Prize for 2015 has been awarded to Miles Congreve (Vice President of Chemistry), Fiona Marshall (Chief Scientific Officer and co-founder) and Malcolm Weir (Chief Executive Officer and co-founder) for the seminal contributions to GPCR drug discovery made by Heptares Therapeutics since the company was founded in 2007.

GPCRs (G protein-coupled receptors) form the most important family of drug targets in the pharmaceutical industry and are linked to a wide range of disease areas; they are the targets for approximately 40% of all existing drugs.

The Prize, awarded by the UK Royal Society of Chemistry's Biological and Medicinal Chemistry Sector, is in recognition of work that has included building the world-renowned StaR® technology platform, which enables precision drug design based on structural information for validated and challenging GPCRs, and the invention of a number of clinical candidates with potential to transform the treatment of a wide range of human diseases. Such candidates include the world's first selective M₁ agonist, which is in clinical studies for improving learning and memory in patients with Alzheimer's disease, schizophrenia and other related diseases. Heptares is also advancing a non-stimulant medicine targeting the adenosine A_2A receptor for treating attention deficit hyperactivity disorder (ADHD).

The winners are particularly commended on their outstanding publication record, and on their willingness to release data into the public domain.

Fiona Marshall, Heptares CSO, said: "Our progress at Heptares since 2007 has been extraordinary and has involved valuable scientific contributions from a very talented team beyond the three of us. We are very proud therefore to receive this prestigious award in recognition of these achievements. We strongly believe in the potential of our integrated technology, discovery and development operation to improve the treatment of severe and debilitating conditions that affect many millions of people around the world."

The Malcolm Campbell Memorial prize commemorates Professor Campbell's outstanding contributions in a broad range of chemistry and their applications to the understanding of bioactivity. The prize is awarded biennially and previous winners include teams at AstraZeneca for the discovery and development of the anti-clotting medicine Brilinta™/Brilique™, at Pfizer for the anti-HIV treatment Sezentry®/Censentri® (maraviroc), and at Organon for the selective relaxant binding agent Bridion® (sugammadex). More information about the Prize can be found here.

The 2015 prize will be presented formally to the winning team during the 18^th RSC/SCI Medicinal Chemistry Symposium to be held at Churchill College in Cambridge on 13-16 September 2015.

About Heptares Therapeutics 

Heptares is a clinical-stage company creating transformative medicines targeting G protein-coupled receptors (GPCRs), a superfamily of receptors linked to a wide range of human diseases. Our proprietary structure-based drug design technology enables us to engineer drugs for highly validated, yet historically undruggable or challenging, GPCRs. Using this approach, we have built an exciting pipeline of new medicines with the potential to transform the treatment of Alzheimer's disease, ADHD, diabetes, schizophrenia, migraine, and other diseases. Our pharmaceutical partners include Cubist, MorphoSys, Takeda, AstraZeneca and MedImmune, and we are backed by Clarus Ventures, MVM Life Science Partners, Novartis Venture Fund, the Stanley Family Foundation and Takeda Ventures. To learn more about Heptares, please visit http://www.heptares.com 

About the Heptares StaR® Platform 

At the heart of Heptares' integrated structure-based design platform for GPCR-focused drug discovery and development is its proprietary StaR® technology. A StaR protein is a stabilised GPCR with a small number of point mutations that greatly improve its thermostability without disrupting its pharmacology. StaR technology allows the generation of stable, functionally relevant, purified GPCRs in their natural pharmacological conformations (agonist or antagonist), including orphan receptors, that retain their expected drug-binding characteristics. Whereas unstable wild-type proteins are intractable to structural studies, StaR proteins allow structure determination and provide the launch pad for an SBDD approach to GPCR drug targets that for the first time enables:

• Determination of 3D structures of GPCRs and complexes with bound ligands by X-ray crystallography and Biophysical Mapping™
• Deployment of compound screening and advanced fragment-based drug discovery approaches to GPCRs
• Full integration of GPCR pharmacology and medicinal chemistry
• Discovery of novel agents directed towards high-value yet historically challenging or undruggable GPCR drug targets

Heptares' StaR platform also offers a breakthrough solution to the main challenge associated with making antibodies against GPCRs: producing purified, properly folded and functional protein when removed from the cell membrane for use as an antigen. Furthermore, StaR proteins preserve biologically relevant epitopes, thereby enabling generation of diverse panels of functional antibodies.

HEPTARES is a registered trademark in the EU, Switzerland, US and Japan;  

StaR is a registered trademark in the EU and Japan.