Galapagos to present favorable pre-clinical data on GLPG1790, a selective ephrin receptor kinase inhibitor, at AACR in San Di...
March 18 2014 - 1:37AM
- First selective small molecule ephrin receptor kinase
inhibitor to enter development
- GLPG1790 has high efficacy against triple-negative
breast cancer
- Potentially suitable for other ephrin-driven
cancers
- GLPG1790 is fully proprietary to
Galapagos
MECHELEN, Belgium, March 18, 2014 (GLOBE
NEWSWIRE) -- Galapagos NV (Euronext: GLPG) will
present favorable pre-clinical data on GLPG1790 in triple-negative
breast cancer at the American Association for Cancer Research
(AACR) Annual Meeting in San Diego on 7 April 2014. In the
abstract, Galapagos disclosed that GLPG1790 is the first selective
small molecule inhibitor of the ephrin receptor kinase family,
which could play a key role in melanoma, pancreatic, ovarian,
prostatic, and colorectal cancers, in addition to triple-negative
breast cancer.
"With GLPG1790, Galapagos shows once again that
it excels in identification of relevant novel modes of action, and
is successful in discovering selective compounds directed toward
these," says Dr Piet Wigerinck, Galapagos CSO. "We are
pleased to present the ephrin receptor kinase targeted approach of
GLPG1790 towards triple-negative breast and potentially other
ephrin-driven cancers at AACR this year. Targeted approaches
in oncology typically show good efficacy and less toxicity than
chemotherapy."
AACR poster details Abstract number: 1753
Poster session: 7 April 2014, 8 AM - 12 PM, Hall A-E, Poster
Section 31, Poster #26 "GLPG1790: the first Ephrin (EPH) receptor
tyrosine kinase inhibitor for the treatment of triple negative
breast cancer"
Candidate drug GLPG1790 shows remarkable in vivo
efficacy in a triple negative breast cancer xenograft pre-clinical
model. Full tumor blockage was observed after 30 mg/kg/d oral
dosing, correlated with target inhibition in the tumor.
Extensive molecular mode of action studies, using GLPG1790
and knock-down tools, prove EPHA2 target engagement and impact on
the MAPK pathway and cell cycle, important elements of the biology
of many cancer types.
GLPG1790 has good drug-like properties, and
safety/tolerability studies with the candidate drug look
favorable. Galapagos is completing preclinical studies with
GLPG1790, and is carefully considering a number of options before
entering the first clinical trials in humans. This novel
program is fully proprietary to Galapagos.
About triple-negative breast
cancer
GLPG1790 has shown high activity against breast
tumors that are triple-negative, for which the absence of estrogen
(ER), progesterone (PR) or HER2 receptors affects the prognosis for
recovery, and no targeted therapeutic options are currently
available. Breast cancer is a disease in which tumor cells
form in the breast tissue; it is one of the most common types of
cancer in women. There are many different types of breast
cancer, and as a result, there are many options for
treatment. Targeted drug treatments such as Herceptin® and
Avastin®1attack specific types of breast cancer cells.
Decisions about the best possible treatment with targeted drugs are
based on tests for the presence of ER, PR and HER22.
Triple-negative breast cancer (tumor cells that have no ER, PR and
HER2) accounts for one-fifth of breast cancers, and it usually
affects young women. There are no targeted drugs available
yet for patients with triple-negative breast cancer.
About Galapagos
Galapagos (Euronext: GLPG; OTC: GLPYY) is
specialized in novel modes-of-action, with a large pipeline
comprising five Phase 2 studies (two led by GSK), one Phase 1
study, six pre-clinical, and 20 discovery small-molecule and
antibody programs in cystic fibrosis, inflammation, antibiotics,
metabolic disease, and other indications. In the field of
inflammation, AbbVie and Galapagos signed a worldwide license
agreement whereby AbbVie will be responsible for further
development and commercialization of GLPG0634 after Phase 2B.
GLPG0634 is an orally-available, selective inhibitor of JAK1
for the treatment of rheumatoid arthritis and potentially other
inflammatory diseases, currently in Phase 2B studies in RA and in
Phase 2 in Crohn's disease. Galapagos has another selective
JAK1 inhibitor in Phase 2 in ulcerative colitis and psoriasis,
GSK2586184 (formerly GLPG0778, in-licensed by GlaxoSmithKline in
2012). GLPG0974 is the first inhibitor of FFA2 to be
evaluated clinically for the treatment of IBD; this program is
currently in a Proof-of-Concept Phase 2 study. GLPG1205 is a
first-in-class molecule that targets inflammatory disorders and has
completed Phase 1. AbbVie and Galapagos signed an agreement
in CF whereby they work collaboratively to develop and
commercialize oral drugs that address two mutations in the CFTR
gene, the G551D and F508del mutation. Potentiator GLPG1837 is
at the pre-clinical candidate stage. Galapagos has 400 employees,
operating from its Mechelen, Belgium headquarters and facilities in
The Netherlands, France, and Croatia. Further information at:
www.glpg.com
CONTACT
For media and investor inquiries: Elizabeth
Goodwin, Head of Corporate Communications & Investor Relations
Tel: +31 6 2291 6240 ir@glpg.com
For business development inquiries: Andre
Hoekema, Senior VP Corporate Development Tel: +31 71 7506 700
bd@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. 1 Herceptin®
and Avastin® are registered trademarks of Roche for trastuzumab and
bevacizumab, respectively
2 Human epidermal growth factor type 2
receptor
HUG#1768621
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