MECHELEN, BELGIUM--(Marketwire - December 21, 2011) -
* Galapagos initiates Phase I First-in-Human trial with GLPG0974
* GLPG0974 is a potent inhibitor of GPR43, a novel Galapagos target
* Galapagos has been returned full rights to GLPG0974 by GSK
Mechelen, Belgium; 21 December 2011 - Galapagos NV (Euronext: GLPG)
today that it has initiated clinical Phase I development of the first
of GPR43, a novel target for inflammatory diseases. This target was
through Galapagos' proprietary target discovery platform.
GLPG0974 is an orally available small molecule that reduces migration
neutrophils, one of the critical cell types in inflammatory processes by
inhibition of GPR43 (also known as FFAR2). Overactivity of neutrophils is
cause of tissue damage in illnesses such as inflammatory bowel disease, and
anti-inflammatory mechanism may provide for a novel treatment approach.
will be the first inhibitor of GPR43 to be evaluated clinically.
The First-in-Human study with GLPG0974 will focus on providing more
on its pharmacokinetics and pharmacodynamics, using an innovative design
clinical testing specifically intended for early clinical exploration of
"GSK has decided to return the GPR43 program to Galapagos, and consequently
will not receive a milestone for initiation of this study," said Onno van
Stolpe, CEO of Galapagos. "We are encouraged by the results of this
thus far and have made the decision to continue moving forward with GLPG0974
Details of GLPG0974 First-in-Human trial
The primary endpoints of the first-in-human trial for GLPG0974 will be
determine the pharmacokinetics and to evaluate biomarker effects of
candidate drug. In addition, the safety and tolerability of a wide dose
will be evaluated. The placebo-controlled, double-blind, single ascending
study is being conducted in 36 healthy human volunteers in Belgium over
coming months. It follows the design for exploratory single dose trials,
supported by guidelines that EMEA and the FDA designed to boost innovation
drug discovery and development.
GLPG0974 is an orally available small molecule, nanomolar inhibitor of GPR43
(G-protein coupled receptor), also known as FFAR2 (free fatty acid receptor
which was identified by Galapagos as playing a key role in
GLPG0974 has shown potent inhibition of neutrophil migration (HOW)
successfully passed single dose animal safety evaluation. No other
of GPR43 are currently known to have been evaluated clinically.
Galapagos (Euronext: GLPG) (PINKSHEETS: GLPYY) is a mid-size
specialized in the discovery and development of small molecule and
therapies with novel modes-of-action. The Company is progressing GLPG0634,
well as one of the largest pipelines in biotech, with seven programs
development and over 50 discovery programs. The Galapagos Group has over
employees and operates facilities in six countries, with global headquarters
Mechelen, Belgium. More info at: www.glpg.com
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