Mechelen, Belgium;
28 February 2008 – Galapagos NV (Euronext & LSE:
GLPG) announced today that it has selected pre-clinical
candidates in its rheumatoid arthritis and bone metastasis
programs. It is the Company's intention to submit IND (Investigational
New Drug) applications for these programs later this year,
with initiation of clinical trials for bone metastasis by
yearend and for rheumatoid arthritis early 2009. The Company
also intends to select a pre-clinical candidate in osteoarthritis
in 2008. Progress on these and other drug discovery programs
will be discussed during the webcast this afternoon.
“By moving the first
drug from our rheumatoid arthritis program into the pre-clinical
development phase, Galapagos is taking an important step
toward discovering first-in-class, disease modifying small
molecule drugs for bone and joint diseases,” said
Onno van de Stolpe, Chief Executive Officer of Galapagos.
“In addition, we are excited that the bone metastasis
program has accelerated to the stage where we can dose first
patients in a clinical trial before year end. This program,
with a potential secondary indication in osteoporosis, provides
a relatively fast path toward a marketed drug with significant
revenue potential for Galapagos and its shareholders.”
Pre-clinical candidate
in rheumatoid arthritis
The Company announced that its rheumatoid arthritis (RA)
candidate against kinase target GT418 demonstrates significant
bone protection and reduced inflammation in the industry
standard mouse model. The effect of this oral compound was
at least equivalent to Enbrel® (etanercept), the injectable
anti-TNF treatment for rheumatoid arthritis. The compound
also demonstrates good bioavailability in three animal species.
Based on these encouraging results, pre-clinical development
has started, with the aim to file an IND by the end of 2008
and initiate a clinical Phase I trial shortly thereafter.
The Phase I trial will be designed to provide safety and
dosage data as endpoints, with preliminary data on pharmacodynamic
properties.
Galapagos’ rheumatoid
arthritis target GT418 was discovered and validated in cells
from rheumatoid arthritis patients, using the Company’s
proprietary target discovery platform. The Company’s
pre-clinical program in rheumatoid arthritis marks the first
ever in this undisclosed mode of action. Galapagos has filed
patent protection on both the role of the target in rheumatoid
arthritis as well as on the candidate drug. Galapagos’
rheumatoid arthritis programs are partnered with Janssen
Pharmaceutica, a Johnson & Johnson company. Galapagos’
candidate drug is a compound in Galapagos’ internal
program within the alliance with Janssen. Upon successful
completion of a Phase IIa trial in Galapagos’ internal
RA programs, Janssen has the exclusive option to license
a program for €60 million, with further potential milestones
to Galapagos in excess of €776 million and tiered double-digit
royalties on global sales.
Pre-clinical candidate
in bone metastasis
Galapagos’ program in bone metastasis is based on
the integrin receptor antagonist (IRA) compound series in
the portfolio of research programs acquired with ProSkelia
in late 2006. The IRA program is based on a known target
characterized in scientific literature. The Company’s
aim in bone metastasis is to deliver an oral drug which
reduces progression of bone metastases and bone degeneration.
Galapagos’ candidate drug has shown reduction of bone
metastasis and bone degeneration comparable to Zometa®
(zolendronate), the industry gold standard treatment for
metastatic bone cancer, and superior prevention of metastases
to other organs. The drug has also demonstrated a reduction
in tumor growth and prevention of blood vessel formation
in pre-clinical animal studies, clearly differentiating
the compound from Zometa. Galapagos’ candidate drug
in bone metastasis has a potential second indication in
osteoporosis and has already demonstrated anti-osteoporotic
activity in pre-clinical animal studies. Based on these
encouraging results, Galapagos announced the initiation
of pre-clinical development of the compound, with the planned
initiation of dosing in man in a Phase I clinical trial
before the end of 2008. The Phase I trial is designed to
deliver safety and tolerability at various dose levels with
preliminary pharmacokinetic data for use in designing later
trials.
“The speed with which
our research teams were able to deliver these candidate
compounds in pre-clinical development testifies to the quality
of our science and approach in drug discovery,” added
Dr Graham Dixon, Senior Vice President Drug Discovery. “Once
we have initiated clinical studies with both known and novel
targets, our remaining discovery programs will also benefit
from the processes and infrastructures put into place.”
Advancement to pre-clinical
development in osteoarthritis in 2008
Galapagos announced achievement of a Proof of Principle
(reduction of a disease marker) and Proof of Concept (reduction
of targeted symptoms) in pre-clinical models in its osteoarthritis
(OA) program. Galapagos compounds block cartilage degradation
in diseased cartilage explants, while diseased mouse joints
treated with this compound also showed reduced cartilage
destruction. Galapagos’ osteoarthritis program has
progressed from validated targets to a Proof of Concept
in 18 months, in this challenging area where there are currently
no marketed disease-modifying drugs. The data generated
thus far encourage the Company to aim for delivery of a
pre-clinical candidate in OA by end 2008. Galapagos’
osteoarthritis program was partnered in an alliance with
GlaxoSmithKline (GSK) in June 2006, which was expanded in
June 2007. Galapagos has received €15.1 million in
payments on this alliance to date and may receive up to
€171 million in further milestones as well as up to
double-digit royalties on commercial products.
Progress in Alzheimer’s
Disease program
Galapagos announced progress in its Alzheimer’s Disease
program in collaboration with Professor Bart De Strooper
of the VIB and KU Leuven (Belgium). Galapagos’ target
GT177 was confirmed in in vivo animal models, including
knock-outs, to be a key regulator in the production of the
amyloid ß peptides that are central to the pathogenesis
of Alzheimer’s Disease. Galapagos is now actively
looking for a licensee with the capability to develop a
drug based on Galapagos’ intellectual property covering
target GT177.
Discontinuation
of SARM program and return of E2G program to ProStrakan
The Company further announced that it will discontinue drug
discovery activity on the lead series from its SARM program
in osteoporosis and cachexia due to the limited bioavailability
of the compounds and the strong success of the Company’s
other R&D programs. Galapagos is seeking partners to
out-license this program. In addition, Galapagos will return
the Estrogen Glucoside (E2G) program to ProStrakan. Galapagos
had an option to license this program for the treatment
of ‘hot flashes’ in menopausal women. On 8 August
2007, Galapagos announced that it would only pursue this
program if a commercial partner were found. As the right
partner was not identified, it was decided to return the
program to ProStrakan.
R&D Update Webcast
Galapagos will give further details on research data and
plans during a live audio webcast presentation starting
at 14.00 CET/8 AM US Eastern time. To participate in the
meeting remotely by telephone, dial +32 2290 1608 prior
to 13.55 CET (7:55 AM US EST). The live audio webcast of
the press conference can be accessed on the Galapagos website
at www.glpg.com.
About bone metastasis
In a process known as metastasis, cancer cells break away
from a primary tumor and form new tumors elsewhere in the
body. When a new tumor forms in bone, it is referred to
as bone metastasis or metastatic bone cancer. The forms
of cancer that lead most commonly to metastatic bone cancer
are breast, prostrate, and lung cancer. Approximately 500,000
new cases of bone metastasis are diagnosed annually in the
US and Europe. As there is no cure for bone metastasis,
current therapies focus on slowing cancer growth. Sales
of these therapies amounted to €1.5 billion in 2007,
with growth to over €3.5 billion expected by 2023.1
About Galapagos
Galapagos (Euronext Brussels, GLPG; Euronext Amsterdam,
GLPGA; London AiM: GLPG) is a drug discovery company with
pre-clinical programs in bone and joint diseases and bone
metastasis. Its division BioFocus DPI offers a full suite
of target-to-drug discovery products and services to pharmaceutical
and biotech companies, encompassing target discovery and
validation, screening and drug discovery through to delivery
of pre-clinical candidates. BioFocus DPI also provides adenoviral
reagents for rapid identification and validation of novel
drug targets, compound libraries for drug screening as well
as chemogenomics and ADMET database products to select targets
and compounds. Galapagos currently employs 460 people and
operates facilities in seven countries, with global headquarters
in Mechelen, Belgium. More information about Galapagos and
BioFocus DPI can be found at www.glpg.com
and www.biofocusdpi.com.
CONTACT
Galapagos NV
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028
ir@glpg.com
