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. Phase
I studies for GLPG0259 have shown a good safety
profile in healthy volunteers and confirm a once-daily oral
dosing regimen. Furthermore, the studies have confirmed
the feasibility of combining GLPG0259 with methotrexate
(the current standard treatment for RA) in future trials.
A similar safety and PK profile was observed for the capsule
formulation of GLPG0259, which will be used in the Phase
II dose-finding efficacy trial in RA patients scheduled
to begin in the third quarter of 2010. An interim readout
of this trial is expected in Q2 2011 and the full Phase
II results are planned for Q4 2011.
GLPG0259
is in Galapagos’ internal RA program, which is part
of an option agreement with Janssen Pharmaceutica. Upon
the completion of a dose finding Phase II 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 up to double-digit
royalties on global sales.
Galapagos
is developing a second orally-available, small molecule
for rheumatoid arthritis – GLPG0634. This novel candidate
drug is selective against Janus kinase (JAK) 1 and 2 targets,
a target class whose inhibition has already proven clinical
efficacy in treating rheumatoid arthritis, and is fully
owned by Galapagos. In August 2010, Galapagos initiated
first-in-human studies
for GLPG0634, with the aim to out-license the
program at a later stage.
For
more information, contact Galapagos
business development.
Related presentations and publications
GLPG0259,
a small molecule kinase inhibitor being developed for rheumatoid
arthritis, shows good safety, tolerability and pharmacokinetics
in healthy volunteers
Vanhoutte, F. et al.
WorldPharma2010
19 July 2010
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