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 February[1] 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.
    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.

    [1] 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.