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Heptares and Takeda Initiate Drug Discovery Collaboration Focused on GPCR Linked to CNS Disorders

April 11, 2011

CAMBRIDGE, England, April 11, 2011 /PRNewswire/ –

– Deal Includes GBP4.5 Million Upfront Cash and Equity, Up to GBP60.5
Million
in Future Milestone Payments, and Royalties on Product Sales

Heptares Therapeutics and Takeda Pharmaceutical Company today announced
the formation of a two-year drug discovery collaboration focused on a single
G-protein coupled receptor (GPCR) that plays an important role in the
pathology of central nervous system disorders. This GPCR has proved
intractable using historical drug discovery efforts, due to its instability
when removed from cell membranes and the resulting lack of insight into its
structure. A new medicine targeting this GPCR would be first-in-class.

During the collaboration, Heptares will leverage its proprietary StaR(R)
(stabilised receptor) technology to engineer the first-ever thermally
stabilised forms of the GPCR as the basis for the drug discovery programme.
Heptares will also apply advanced structural biology[*1] and rational drug
design approaches[*2] – including Biophysical Mapping(TM), X-ray
crystallography and fragment screening – to characterise the GPCR’s structure
and to generate early leads. Takeda will participate in lead generation and
then assume responsibility for preclinical development and clinical
development of new drugs candidates.

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 is also eligible to receive
future milestone payments of up to GBP60.5 million[*3] plus royalties on
product sales. Further terms of the agreement are not being disclosed.

“We are excited to be collaborating with Takeda to unlock a key GPCR
target for treating CNS disorders, an area of significant unmet medical need
where Takeda has established a leading scientific and commercial position,”
said Malcolm Weir, CEO of Heptares Therapeutics. “As we advance Heptares’
internal pipeline of GPCR-targeted medicines, we also plan to pursue
attractive external opportunities, such as this partnership with Takeda, to
extend our technology broadly across the GPCR universe.”

“The Heptares StaR(R) technology is a powerful new capability for
discovering GPCR-targeted drugs and we look forward to applying it to a
specific GPCR target of interest to Takeda in the area of neuroscience,” said

Shigenori Ohkawa, Chief Scientific Officer at Takeda Pharmaceutical Company.
“The Heptares platform applies broadly to the GPCR target family and delivers
stabilised forms that most precisely capture the pharmacological
conformations of GPCRs as they exist in their natural cellular environments.”

[*1] Structural biology is the combined use of molecular biology and
biophysical technologies, in particular X-ray crystallography, for the
elucidation of three-dimensional structures of biological macromolecules,
especially proteins.

[*2] Rational drug design approaches apply structural biology to
understand in atomic detail how compounds interact with their target
receptors, so they can be systematically turned into viable drug candidates
by iterative medicinal chemistry.

[*3] For future milestone payments, Heptares is eligible to receive GBP1M
(GBP) in research-stage milestones and $96M (USD) in additional later-stage
milestones. To report the total future milestone payments in the single
currency of GBP, the figure reported above of GBP60.5M reflects the
conversion of $96M at a current exchange rate of 0.62, which equals GBP59.5M
(GBP), plus GBP1M (GBP), which equals GBP60.5M (GBP).

About Heptares Therapeutics

Heptares is a drug discovery company creating new medicines targeting
G-protein-coupled receptors (GPCRs). The Company is currently leveraging its
GPCR expertise and proprietary StaR(R) technology to build a pipeline of
best-in-class and first-in-class GPCR-targeted medicines for the treatment of
CNS, metabolic and other diseases.

GPCRs represent the single most important family of drug targets in the
human body, yet, due to their inherent instability when removed from cell
membranes, little or no structural information about these valuable targets
has been available to drive structure-based drug discovery programmes.
Heptares’ StaR(R) (Stabilised Receptor) technology enables the first-ever
thermo-stabilisation of GPCRs. This breakthrough allows Heptares scientists
to resolve GPCR structures and deploy structure-based drug discovery
techniques to identify potent and selective drug candidates to previously
undruggable targets.

Heptares has raised more than $35 million from leading venture investors,
Clarus Ventures, MVM Life Science Partners and Novartis Option Fund.

http://www.heptares.com

About Takeda Pharmaceutical Company

Located in Osaka, Japan, Takeda is a research-based global company with
its main focus on pharmaceuticals. As the largest pharmaceutical company in
Japan and one of the global leaders of the industry, Takeda is committed to
strive towards better health for patients worldwide through leading
innovation in medicine. Additional information about Takeda is available
through its corporate website, http://www.takeda.com.

    Contact Information:

    Heptares Therapeutics Ltd              +44(0)1707-358-629
    Dr Malcolm Weir, CEO                   malcolm.weir@heptares.com
    Dr Barry Kenny, CBO                    barry.kenny@heptares.com

    Citigate Dewe Rogerson (For Heptares)  +44(0)20-7282-2948
    Dr Mark Swallow, Dr Chris Gardner      mark.swallow@citigatedr.co.uk

    Takeda Pharmaceutical Company
    Mihoko Shinomiya                       +81-3-3278-2037

SOURCE Heptares and Takeda


Source: newswire



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