Heptares Achieves All Research Milestones and Receives Milestone Payment From GPCR Drug Discovery Agreement With Takeda

Heptares Achieves All Research Milestones and Receives Milestone Payment From
                  GPCR Drug Discovery Agreement With Takeda

  PR Newswire

  WELWYN GARDEN CITY, England and BOSTON, April 29, 2013

WELWYN GARDEN CITY, England and BOSTON, April 29, 2013 /PRNewswire/ --

Heptares Therapeutics, the leading GPCR drug discovery and development
company, announces it has achieved all milestones in its collaboration with
Takeda Pharmaceutical Company. By achieving these milestones, Heptares will
receive a significant payment from Takeda, under the terms of the agreement
signed by the two companies in 2011.

The agreement is focused on a single GPCR target nominated by Takeda that,
until now, has proved intractable to rational drug discovery efforts due to
its instability when removed from the cell membranes and the resulting lack of
insight into its structure. Over the course of the collaboration Heptares has
leveraged its structure-based drug design (SBDD) approach to GPCRs and
proprietary technologies to generate the first-ever stabilised form of the
target in a clinically relevant conformation enabling a series of novel lead
candidates against the target to be designed.

Tetsuyuki Maruyama, General Manager Pharmaceutical Research Division, Takeda
said: "We are impressed with the efficiency and results from this partnership
with Heptares. In achieving these milestones, the Heptares team has
demonstrated its ability to design new, high-quality small molecules to a
previously challenging GPCR target. We look forward to continuing our
partnership and taking these leads forward into pre-clinical development."

"Our partnership with Takeda provides an excellent validation of our
GPCR-focused structure-based drug design approach and capabilities," said
Malcolm Weir, CEO of Heptares. "We see similar good progress in our other
partnerships where to date we have hit every milestone. This success, in turn,
provides us with an important source of capital, which has enabled us to build
an impressive proprietary pipeline and provided funds to advance our
first-ever selective M1 agonist into first clinical studies later this year."

Under the terms of the agreement, Takeda receives worldwide commercial rights
to new drugs emerging from the collaboration. Upon signing, Heptares received
an upfront payment of £1.7 million and an investment in an equity stake of
approximately £2.8 million purchased by Takeda Ventures Inc., a wholly-owned
subsidiary of Takeda. Heptares has also now received £1 million in
research-stage milestones and is eligible to receive $96 million in additional
later-stage milestones plus royalties on product sales. Further terms of the
agreement are not disclosed.

About G protein-coupled receptors (GPCRs)

The GPCR superfamily is the largest and single most important family of drug
targets in the human body. It plays a central role in many biological
processes and is linked to a wide range of disease areas. GPCRs are expressed
in every type of cell in the body where their function is to transmit signals
from outside the cell across the membrane to signaling pathways within the
cell, between cells and between organ systems. There are over 375 GPCRs
encoded in the human genome, of which 225 have known ligands and 150 are
orphan targets. GPCRs are the site of action of 25-30% of current drugs. Six
of the top ten and 60 of the top 200 best-selling drugs in the US in 2010
target GPCRs.

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
advanced structure-based drug design technology platform, we have built an
exciting discovery and development pipeline of novel drug candidates, which
have the potential to transform the treatment of serious diseases, including
Alzheimer's disease, Parkinson's disease, schizophrenia, migraine and
diabetes. Our pharmaceutical partners include Shire, AstraZeneca, MedImmune,
Morphosys, Takeda and Cubist, and we are backed by MVM Life Science Partners,
Clarus Ventures, Novartis Venture Fund and Takeda Ventures. To learn more
about Heptares, please visit http://www.heptares.com .

Contact: Contact Information: Citigate Dewe Rogerson (for Heptares), Mark
Swallow, Chris Gardner, +44(0)20-7282-2948, mark.swallow@citigatedr.co.uk;
Heptares Therapeutics Ltd, Malcolm Weir, Chief Executive Officer (UK),
+44(0)1707-358-629, malcolm.weir@heptares.com; Dan Grau, President (USA),
+1-857-222-4586, dan.grau@heptares.com
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