Galapagos is developing its novel mechanism of action, first-in-class candidate drug GLPG0259 for rheumatoid arthritis (RA). This 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. Results from the first Phase I study for this candidate drug demonstrated good safety in healthy volunteers and a profile that supports once-daily oral dosing. Galapagos is on-track to complete Phase I trials by the end of 2009 and plans to initiate a Phase IIa efficacy study in 2010.

In October 2007, Galapagos entered into a worldwide multi-target alliance with Janssen Pharmaceutica NV, a Johnson & Johnson company, to discover and develop novel small-molecule therapeutics for the treatment of RA.


Related presentations and publications

Small molecule inhibitors of a novel target MAPKAPK5 show bone protection and anti-inflammatory activity in in vivo models of rheumatoid arthritis
Andrews M , et al.
EULAR
10-13 June 2009

The alpha7 nicotinic acetylcholine receptor on fibroblast-like synoviocytes and in synovial tissue from rheumatoid arthritis patients: a possible role for a key neurotransmitter in synovial inflammation
van Maanen MA, Stoof SP, van der Zanden EP, de Jonge WJ, Janssen RA, Fischer DF, Vandeghinste N, Brys R, Vervoordeldonk MJ, Tak PP
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Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents
Lin HS, Hu CY, Chan HY, Liew YY, Huang HP, Lepescheux L, Bastianelli E, Baron R, Rawadi G, Clément-Lacroix P
Br J Pharmacol. 2007 Apr;150(7):862-72

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