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: www.glpg.com.
CONTACT
Galapagos
NV
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028
ir@glpg.com
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.
|