AstraZeneca and Heptares Therapeutics announced they have entered a four-year collaboration focused on the potential discovery and development of new medicines targeting G-Protein Coupled Receptors (GPCRs).

GPCRs are among the largest and most important family of proteins found in the human body, yet they become highly unstable when removed from their natural membrane-bound environments. This instability has prevented pharmaceutical researchers from understanding GPCR structures and hampered efforts to design medicines that work on GPCR targets.

This collaboration brings together Heptares’ GPCR discovery expertise and proprietary technologies, including its StaR technology, which engineers stabilized receptors allowing GPCRs to be investigated, with AstraZeneca’s biopharmaceutical discovery, development and commercial capabilities.  Research conducted under the collaboration will focus on a number of specific GPCR targets linked to central nervous system/pain, cardiovascular/metabolic and inflammatory disorders from projects in AstraZeneca’s small and large molecule portfolio, including projects from AstraZeneca’s biologics unit, MedImmune. This research will act as the starting point for drug discovery by producing the first-ever stabilized forms of GPCRs in their natural pharmacological conformation.

As part of a joint discovery effort, Heptares and AstraZeneca will engage their respective discovery teams, compound libraries, and other discovery technologies for the purposes of initial screening and lead identification.  Results will be combined into a common pool and the best leads will be further optimised collaboratively. AstraZeneca will then select pre-clinical, small and large molecule candidates and will be solely responsible for preclinical and clinical development.

Under the terms of the agreement, AstraZeneca has worldwide commercial rights to product candidates emerging from the collaboration. Heptares will receive an upfront $6.25 million cash payment fee plus committed research funding and also qualifies for significant future payments depending on  delivery of agreed milestones. Heptares will also receive royalties on sales of all products discovered through the joint research.

“This exciting collaboration gives us access to cutting-edge technology that will enable us to apply our biophysical and antibody generation capabilities to this important, yet extremely challenging, area of research. Our work will focus on a range of different diseases across our small and large molecule portfolio with the goal of discovering innovative treatments for patients in areas of medical need,” said Martin Mackay, president, Research and Development, AstraZeneca.

“This alliance with AstraZeneca illustrates the broad power and scalability of the Heptares technology to generate novel drug candidates in regions of GPCR space that were previously regarded as closed to pharmaceutical discovery,” said Malcolm Weir, CEO of Heptares. “We look forward to working closely with our AstraZeneca colleagues to extend the range of targets and therapeutic areas to which we apply our GPCR capabilities, and are excited by the significant R&D commitment of AstraZeneca to this pioneering GPCR alliance.”

AstraZeneca is a global, innovation-driven biopharmaceutical business with a primary focus on the discovery, development and commercialisation of prescription medicines for gastrointestinal, cardiovascular, neuroscience, respiratory and inflammation, oncology and infectious disease.

Heptares is a drug discovery company creating new medicines targeting G-Protein-Coupled Receptors (GPCRs).

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 (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.