Heptares Successfully Completes Research Phase of Antibody Discovery Collaboration with MedImmune

January 23, 2014

LONDON and BOSTON, January 23, 2014 /PRNewswire/ –

Stabilised GPCR (StaR(R)) Proteins Delivered For All Nominated Targets

Heptares Therapeutics, the leading GPCR structure-guided drug discovery and
development company, has successfully completed the research phase of its antibody drug
discovery collaboration with MedImmune, the global biologics research and development arm
of AstraZeneca. In achieving this milestone, Heptares has delivered StaR(R) proteins
(thermostabilised G protein-coupled receptors, GPCRs) for its targets nominated by
MedImmune for antibody discovery as part of the research collaboration initiated in May
2011. For each project, nomination of the target and delivery of the StaR protein resulted
in milestone payments to Heptares from MedImmune.

Malcolm Weir, Heptares CEO, said: “The delivery of a StaR for each nominated target is
an important achievement in the successful research phase of our collaboration with
MedImmune. The StaR proteins will now be used by MedImmune as antigens to which novel
therapeutic antibodies can be generated. The ability of our StaR platform to generate
antigen for antibody drug discovery, as exemplified by the success of our collaboration
with MedImmune, highlights the potential of this technology to transform GPCR-targeted
drug design and development.”

The Heptares StaR technology provides a solution to the central challenge associated
with obtaining antigens for raising antibodies against GPCR targets: generating purified,
properly folded and functional protein which has been removed from the cell membrane. StaR
proteins also preserve epitopes from the desired pharmacological state (active or
inactive) of the GPCR, thereby enabling generation of panels of functional antibodies
targeting the disease-relevant form of the receptor.

By the end of 2012, 37 therapeutic antibodies had been approved and are being marketed
in countries around the world, generating sales of $64.5 billion in 2012. Of the ten
best-selling drugs in 2012, six were monoclonal antibody drugs, each with annual sales
exceeding $5 billion. However, only one GPCR-targeting antibody has been approved
(Poteligeomogamulizumab, an anti-CCR4 antibody approved in Japan), which reflects the
central technical challenge of accessing reliable high-quality GPCR antigen.

Heptares has determined that approximately 100 GPCR targets across a range of diseases
(cancer, fibrosis, inflammation, respiratory, pain) are suitable and commercially
compelling as antibody targets. Heptares is now leveraging its StaR platform to generate
antigens for GPCR antibody drug discovery via partnerships with MedImmune and other
companies. To date, Heptares has achieved all scientific milestones in its drug discovery
collaborations on or ahead of schedule.

About Heptares Therapeutics

Heptares creates new medicines targeting clinically important, yet historically
challenging, GPCRs (G protein-coupled receptors), a superfamily of drug receptors linked
to a wide range of human diseases. Leveraging our proprietary structure-based drug design
technology platform, we have built an exciting pipeline of novel drug candidates with the
potential to transform the treatment of serious diseases, including Alzheimer’s disease,
ADHD, diabetes, schizophrenia, and migraine. 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

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

SOURCE Heptares Therapeutics

Source: PR Newswire

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