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
Arthritis Rheum. 2009 May;60(5):1272-81
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