Galapagos enters the clinic with rheumatoid arthritis candidate drug

Click here to access the live audio webcast presentation at 11.00 CET, call number +32 2290 1608
  • First-in-human trial with breakthrough candidate drug
  • Based on novel Galapagos target MAPKAPK5
  • Broad US patents granted
    Mechelen, Belgium; 27 March 2009 – Galapagos NV (Euronext: GLPG) announces that today it initiated Phase I clinical development of its novel mechanism of action, first-in-class candidate drug GLPG0259 for rheumatoid arthritis (RA).  GLPG0259 is the first small molecule from Galapagos’ target discovery platform to enter the clinic.  GLPG0259 targets protein kinase MAPKAPK5, which represents a new approach for the treatment of RA.  The US Patent Office has granted Galapagos patents on the use of this target for the discovery of RA drugs and on the chemical space around this candidate drug.
    Target MAPKAPK5 (formerly encoded by Galapagos as GT418) is a new starting point for the treatment of RA.  Galapagos discovered and validated the key role of this target in the RA disease process, using its proprietary target discovery technology.  MAPKAPK5 had not been previously associated with RA; however, Galapagos’ internal research indicated that it is involved in a signaling pathway that is central to inflammation.  The candidate drug GLPG0259 inhibits MAPKAPK5, and demonstrates excellent bone protection and reduced inflammation in a standard RA animal model.  GLPG0259 has successfully completed preclinical development.  Galapagos received US patents for the use of target MAPKAPK5 for the discovery of RA drugs and on the lead series of compounds directed against this target.  Similar patents are pending in Europe and other major regions. 
    GLPG0259 is a compound in Galapagos’ internal RA program, which is part of an alliance with Janssen Pharmaceutica.  Upon successful completion of a Phase IIa clinical trial for GLPG0259, Janssen has the exclusive option to license the program for €60 million, with further potential milestones to Galapagos of €776 million and double-digit royalties on global sales.
    “Today’s entry into the clinic is a true landmark for Galapagos,” said Onno van de Stolpe, CEO of Galapagos.  “This is the first candidate medicine based on our target platform to enter the clinic and I am extremely proud of our team who made this achievement possible.  We moved this RA program from concept to clinic in less than five years.  Furthermore, we possess a broad portfolio of programs that further solidifies our activity in this therapeutic area.”
    Details of the Phase I clinical trial
    The primary endpoints of this first-in-human trial will be to determine the safety, tolerability, and pharmacokinetics of the candidate drug GLPG0259.  The double blind, single ascending and multiple dose studies will be conducted in 34 healthy human volunteers in Belgium over the coming months.
    About Galapagos’ target discovery approach and MAPKAPK5
    Galapagos applies its target discovery platform to identify completely new starting points, known as targets, for the development of breakthrough medicines.  In its RA program, Galapagos tested cells from the joints of rheumatoid arthritis patients and identified 19 new targets.  MAPKAPK5 (mitogen-activated protein kinase-activated protein kinase 5) was shown to play a key role in inflammation and in the breakdown of collagen in human cartilage and formed the basis of the discovery and development of the candidate drug entering Phase I development.  GLPG0259 is the first clinical candidate with this novel mechanism of action.  Galapagos has patents for the use of target MAPKAPK5 for the discovery of RA drugs (US patent 7,306,923), and on the lead series of compounds directed toward MAPKAPK5 (US patent 7,501,411).
    R&D update webcast
    Galapagos will give further details on research data and development plans during a live audio webcast presentation starting at 11.00 CET today.  Click here to access the live audio webcast.  To participate in the meeting remotely by telephone, dial +32 2290 1608 ten minutes prior to commencement.  A question and answer session will follow the presentation.  The archived webcast also will be available for replay shortly after the close of the call.
    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 GlaxoSmithKline, Janssen Pharmaceutica, Eli Lilly and Merck & Co.  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 480 people and operates facilities in six countries, with global headquarters in Mechelen, Belgium.  More info at:
    Galapagos NV
    Onno van de Stolpe, CEO
    Tel: +31 6 2909 8028
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