AZ, Heptares in GPCR Pact

AstraZeneca and Heptares Therapeutics 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 AZ’s discovery, development and commercial capabilities. Research conducted under the collaboration will focus on a number of specific GPCR targets linked to CNS/pain, CV/metabolic and inflammatory disorders from projects in AZ’s small and large molecule portfolio, including projects from its 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 preclinical, small and large molecule candidates and will be solely responsible for preclinical and clinical development.

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