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Last updated on April 16, 2014 at 1:21 EDT

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

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 GBP1.7 million and an investment in an equity stake of approximately GBP2.8 million
purchased by Takeda Ventures Inc., a wholly-owned subsidiary of Takeda. Heptares has also
now received GBP1 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.

SOURCE Heptares Therapeutics


Source: PR Newswire