Galapagos reveals key drug target for Alzheimers disease by fionan


									Press release                                                                         13 February 2009

          Galapagos reveals key drug target for Alzheimer’s disease

           •     Starting point for potential breakthrough treatment
           •     Published in Science
           •     U.S. patent granted

Mechelen, Belgium; 13 February 2009 – Galapagos NV (Euronext: GLPG) announces
the discovery of a human drug target that plays a key role in Alzheimer’s disease.
This breakthrough was published today in Science, one of the world’s most
prestigious scientific journals. The data presented in Science are a result of the
collaboration between Galapagos and the academic group of Professor Bart De
Strooper at the Flanders Institute for Biotechnology VIB and the KU Leuven in
Belgium. The U.S. patent office has granted Galapagos a patent on this discovery.

“GPR3 is a promising drug target for developing a treatment for Alzheimer’s. There is a lack of
drug targets in this field, and it is gratifying that Galapagos discovered GPR3,” commented Onno
van de Stolpe, CEO of Galapagos. “Through this collaboration with Professor Bart De Strooper,
one of the leading experts in the Alzheimer’s field, we have been able to prove the key role of
GPR3 in Alzheimer’s and are excited that we can now share these data with the scientific
community. Galapagos is now starting drug discovery with the aim to deliver a candidate drug to
treat Alzheimer’s disease.”

Crucial role of drug target
The Science article describes how GPR3 was identified in human cells using Galapagos’ platform.
The article further describes the role of GPR3 in Alzheimer’s disease. Inhibition of GPR3
prevented the accumulation of beta-amyloid, a protein in the brains of Alzheimer’s patients that is
believed to cause the disease. The article also shows that GPR3 levels are higher in the areas of
the brain that are affected in Alzheimer’s patients. The activity of GPR3 can likely be inhibited
with a small molecule drug. Taken together, GPR3 is a promising drug target for development of
a treatment for Alzheimer’s disease.

Galapagos has recently been awarded U.S. patent 7,429,459 for the use of GPR3 in screening for
Alzheimer’s drugs. Similar patent applications are pending in Europe and other major territories.
Galapagos made its Alzheimer's discovery in the same way as its novel, patent-protected targets
in bone & joint disease were identified.

The article entitled “The orphan G protein–coupled receptor 3 modulates amyloid-beta peptide
generation in neurons” is available today through the Science website at
and is published in the 13 February1 printed edition of the journal.

About Alzheimer’s disease
Alzheimer’s disease is a terminal, degenerative illness that causes problems with memory,
thinking and behavior. In 2006 there were an estimated 27 million patients worldwide with
Alzheimer; this is expected to quadruple by 2050. There is no cure available for Alzheimer;
current therapies address only symptoms of the disease.

   Full reference: Thathiah, A., Spittaels, K., Hoffmann, M., Staes, M., Cohen, A., Horré, K., Vanbrabant,
  M., Coun, F., Baekelandt, V., Delecourte, A., Fischer, D.F., Pollet, D., De Strooper, B., and Merchiers, P.
  The orphan G protein–coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science
  323 (2009), 946-951.
About Galapagos’ Alzheimer’s disease program
Galapagos identified novel targets in Alzheimer’s disease using its proprietary adenoviral based
discovery platform. This work was supported by a €1.4 million grant from the Flemish IWT. A
number of novel targets were identified, including GPR3, and patent applications were filed on
the role of these targets in Alzheimer’s disease. In January 2006, Galapagos made the strategic
decision to focus its internal drug discovery on the bone and joint diseases, but continued
working on the Alzheimer’s disease program through a collaboration with Professor Bart De
Strooper of the VIB and KU Leuven (Belgium). Galapagos plans to enter into discussions with
potential pharmaceutical partners while progressing GPR3 into drug discovery.

About Galapagos
Galapagos (Euronext: GLPG; OTC: GLPYY) is a drug discovery and development company with
small molecule programs in bone and joint diseases, bone metastasis, cachexia, anti-infectives
and metabolic diseases.      It has established risk sharing alliances with GSK, Janssen
Pharmaceutica, Eli Lilly and Merck. Through an alliance with MorphoSys, Galapagos is also
developing new antibody therapies in bone and joint diseases. Its division BioFocus DPI offers a
full suite of target-to-drug discovery products and services to pharmaceutical and biotech
companies and to patient foundations, encompassing target discovery and validation, screening
and drug discovery through to delivery of pre-clinical candidates. Galapagos currently employs
470 people and operates facilities in six countries, with global headquarters in Mechelen,
Belgium. More info at:

VIB, the Flanders Institute for Biotechnology, is a non-profit research institute in the life sciences.
Some 1,100 scientists and technicians conduct strategic basic research on the molecular
mechanisms that control the functioning of the human body, plants, and micro-organisms.
Through a close partnership with four Flemish universities − Ghent University, the Katholieke
Universiteit Leuven, the University of Antwerp, and the Vrije Universiteit Brussel − and a solid
investment program, VIB unites the forces of 65 research groups in a single institute. Their
research aims at fundamentally extending the frontiers of our knowledge. Through its
technology transfer activities, VIB strives to convert the research results into products for the
benefit of consumers and patients. VIB also develops and distributes a broad range of
scientifically substantiated information about all aspects of biotechnology. More info at:

K.U. Leuven
The University of Leuven is Belgium’s largest university and one of the oldest universities in
Europe, founded in 1425. It is a comprehensive university with 14 faculties, with a long tradition
of high-quality interdisciplinary research and teaching. The University of Leuven has over 33,000
students (12 percent international) and over 17,000 staff members (8,600 in the various
university departments and 8,700 at UZ Leuven, the university hospital). More info at:

Center for Human Genetics
The Center for Human Genetics provides research, education and services in the fields of
genetics, cell biology and developmental biology. With the aid of genetics, the Center strives to
increase our understanding of human diseases. It conducts leading research in molecular
genetics and provides a platform for genetic technologies to support clinical and fundamental
research in Belgium and abroad. The Center places its clinical and scientific expertise at the
service of society in the form of advice, diagnosis and treatment. Attention is also directed to the
social, ethical and psychological implications of new insights and clinical practices in human
genetics on the individual and on society. More info at:

Galapagos NV
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028

This release may contain forward-looking statements, including, without limitation, statements containing
the words “believes,” “anticipates,” “expects,” “intends,” “plans,” “seeks,” “estimates,” “may,” “will,” “could,”
“stands to,” and “continues,” as well as similar expressions. Such forward-looking statements may involve
known and unknown risks, uncertainties and other factors which might cause the actual results, financial
condition, performance or achievements of Galapagos, or industry results, to be materially different from
any historic or future results, financial conditions, performance or achievements expressed or implied by
such forward-looking statements. Given these uncertainties, the reader is advised not to place any undue
reliance on such forward-looking statements. These forward-looking statements speak only as of the date
of publication of this document. Galapagos expressly disclaims any obligation to update any such forward-
looking statements in this document to reflect any change in its expectations with regard thereto or any
change in events, conditions or circumstances on which any such statement is based, unless required by law
or regulation.

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