Heptares Secures GBP21 Million in Series A Fund Raising to Accelerate Development of Pipeline of Small Molecules Against High-Value GPCR Drug Targets

February 24, 2009

LONDON, February 24 /PRNewswire/ –

– Syndicate Comprises Leading Sector Investors Clarus Ventures, MVM Life
Science Partners and Novartis Option Fund

Heptares Therapeutics Ltd, the drug discovery company focused on drugs
targeting G-protein-coupled receptors (GPCRs), announces today it has raised
GBP21 million (US$30 million) of equity finance in a successful Series A
private round from three blue-chip international venture capital firms.
Clarus Ventures led the syndicate, which includes the founding investor, MVM
Life Science Partners, and the Novartis Option Fund. All three investors
contributed equally.

Michael Steinmetz for Clarus Ventures and Anja Koenig for the Novartis
Option Fund have joined the Heptares Board of Directors as non-executive

Over the next three years, Heptares intends to use the new funds to
develop its own pipeline of small-molecule drug candidates using its
proprietary StaR(TM) technology platform. These novel drug candidates will be
developed against currently intractable GPCRs that are highly validated
targets for the treatment of disease. Further progress in the application of
StaR technology over this period is also expected to yield commercial
partnering opportunities outside Heptares’ core focus, for example, improved
therapeutic antibodies against GPCRs.

GPCRs play a crucial role in many diseases and are the site of action of
25-30% of current drugs; as such they represent a major area of interest for
pharmaceutical companies. However, these membrane proteins are notoriously
difficult to isolate from cells in an intact and active form and this has
severely restricted efforts to study GPCRs using modern drug discovery

Heptares’ StaR (Stabilised Receptor) technology platform enables the
Company to overcome this technology hurdle by engineering and purifying GPCRs
in stable and functional conformations that retain their drug-binding
characteristics. The Company can then apply contemporary drug discovery
approaches, such as crystallisation and structure-based design, biophysical
analysis of ligand interactions, and fragment screening to stabilised GPCRs.
This unique approach is expected to radically improve the chances of finding
drugs to previously intractable targets and enable the development of safer
and more selective therapeutic agents.

Heptares was founded in 2007 as a spin-out from the prestigious MRC
Laboratory of Molecular Biology (Cambridge, UK) based on world-class
pioneering research and expertise in GPCRs. In 2008, the StaR technology was
used successfully to elucidate the three-dimensional atomic resolution
structure of the beta-1 adrenergic receptor, which is the site of action of
beta blockers.

Heptares’ CEO, Dr Malcolm Weir, said: “We are very pleased to have
completed this significant fundraising in the current economic environment.
We are delighted to have attracted such a truly international group of
blue-chip investors and see this as a real endorsement of the quality and
commercial potential of our StaR technology. We now have a very good
opportunity to implement our strategy for generating new drug candidates to
highly validated but previously challenging GPCRs.”

Dr Michael Steinmetz, Managing Partner at Clarus Ventures, said:
“Heptares has made impressive progress in developing its unique StaR
technology since its inception in 2007. Its platform has the potential to
make important GPCR drug targets accessible to drug discovery techniques
previously not applicable to this class of proteins. The commercial
opportunity arising from developing new first/best-in-class drugs to GPCRs is
clear, particularly with pharmaceutical company pipelines under pressure. We
are pleased and excited to participate in this funding round with MVM and
Novartis Option Fund, and are committed to supporting the experienced
management team in fulfilling the potential of Heptares’ innovative approach.”

Dr David Tapolczay, CEO of Medical Research Council Technology, said:
“Heptares is a prime example of the importance of MRC’s long-term support for
basic biomedical research and the potential for discoveries to translate into
a commercial enterprise that is dedicated to producing better medicines. The
fact that Heptares has attracted such a strong investor syndicate and funding
round so early in its development also shows how quickly this translation of
basic research into significant health benefits can be made to occur.”

Notes to Editors

About Heptares Therapeutics Ltd

Heptares is a drug discovery company focused on the discovery of novel
small-molecule drugs targeting G-protein-coupled receptors (GPCRs). The
Company is deploying its proprietary StaR(TM) technology principally against
highly validated but currently difficult or intractable GPCR targets in
several disease areas.

GPCRs are the single most important family of drug targets in the human
body, but because of their inherent instability they are refractory to
structural studies and in vitro screening. StaR technology enables the
engineering of stabilised GPCRs, making them amenable to these vital drug
discovery approaches. There are many clinically relevant GPCR targets across
a wide range of therapeutic areas where discovery is advancing slowly and for
which structural information, novel screening approaches and potential
antibody therapeutics would greatly enhance progress.

Heptares was founded in 2007 and its StaR technology arose out of the
pioneering work of Heptares’ founding scientists, Richard Henderson and Chris
at the MRC Laboratory of Molecular Biology (Cambridge, UK) and of a
wider group of MRC scientists, including Gebhard Schertler, and Ed Hulme of
the National Institute for Medical Research, London. Malcolm Weir (CEO) and

Fiona Marshall (CSO) are its founding management.

For more information, see http://www.heptares.com

About Clarus Ventures

Clarus Ventures is a life sciences venture capital firm founded by a team
of accomplished investment professionals with extensive and complementary
industry backgrounds, which have enabled them to establish a long history of
success in creating value. Their deep relationships with world thought
leaders and decision makers allow this team to identify unique investment
opportunities and shepherd them to maturity. Clarus augments its core
expertise of investing in biopharmaceuticals and medical technology companies
with the deep and diverse expertise of the team in research and development,
commercialization, business development and operations management at the
global level. Clarus is based in Cambridge, MA and San Francisco, CA and
presently manages over US$1.2 billion across two lifesciences dedicated funds.

For additional information on Clarus Ventures, please visit

About MVM Life Science Partners LLP

MVM Life Science Partners LLP, founded in 1997, is one of the UK’s
leading Venture Capital firms and manages three funds totalling over US$500
. MVM invests across the Life Sciences market including
biopharmaceuticals, diagnostics, drug delivery, gene therapy, medical
devices, OTC medicines, research tools and vaccines. MVM invests
predominantly in start up and early stage companies based across Europe and
in the US. The MVM team has broad experience across the Life Science and
Venture Capital markets and maintains offices in London and Boston.

For more information: http://www.mvmlifescience.com

About Novartis Option Fund

The Novartis Option Fund is part of the Novartis Venture Funds.
Established in 1996, the Novartis Venture Funds currently manage over US$650
in committed capital and are invested globally in more than 50
private life sciences companies across therapeutics, vaccines, devices and
diagnostics. As a financially driven corporate life science investor, the
Novartis Venture Fund invests in those companies which have the potential to
lead the next innovation wave in new areas that will be critical to patient
care. The Novartis Venture Funds team of eight investment professionals
located in Basel, Switzerland and Cambridge, Massachusetts, brings together
extensive expertise in the biotech and pharmaceutical industry and venture

    For more information: http://www.venturefund.novartis.com

    Contact Information:

    Heptares Therapeutics Ltd
    Dr Malcolm Weir
    Phone: +44(0)20-8906-7182
    Mobile: +44(0)7968-947268
    E-mail: malcolm.weir@heptares.com

    Clarus Ventures
    Dr Michael Steinmetz
    Phone: +1-617-949-2200
    E-mail: msteinmetz@clarusventures.com

    MVM Life Science Partners
    Dr Martin Murphy
    Phone: +44(0)20-7557-7500
    E-mail: martinmurphy@mvmlifescience.com

    Novartis Option Fund
    Dr Anja Koenig
    Phone: +41-61-3241287
    E-mail: anja.koenig@novartis.com

    Citigate Dewe Rogerson (for Heptares)
    Dr Mark Swallow
    Phone: +44(0)20-7282-2948
    E-mail: mark.swallow@citigatedr.co.uk

SOURCE Heptares Therapeutics Ltd

Source: newswire

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