AstraZeneca and Heptares Therapeutics today 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.”
