MECHELEN, BELGIUM--(Marketwire - December 02, 2010) -
· Successful completion of first-in-human trial for GLPG0492
· Plans to initiate extended dose and Proof of
studies in 2011
Mechelen, Belgium; 2 December 2010 - Galapagos NV (Euronext: GLPG)
today that it has successfully completed the first-in-human trial for
its candidate drug for cachexia (loss of weight and muscle mass) and
other indications, such as Duchenne muscular dystrophy. The candidate
showed good safety in healthy volunteers and a pharmacokinetic (PK)
which supports once-daily oral dosing.
In this first-in-human trial, healthy volunteers were given increasing
candidate drug GLPG0492 by oral administration. Safety data were favorable
no severe adverse events or changes in vital signs and laboratory
reported. Changes in biomarker levels lasting more than 24 hours
consistent with once-daily oral dosing. Similar positive safety and
results were seen for elderly volunteers. Galapagos plans to conduct a
Phase I trial in healthy volunteers in the course of 2011 to assess the
and tolerability of GLPG0492 over at least 14 consecutive days. Based on
trial, a Proof of Concept study is scheduled for late 2011.
"We are encouraged by the promising results of this first clinical
GLPG0492," said Piet Wigerinck, Galapagos' SVP Development. "Comparable
and PK profiles were seen for younger and elderly volunteers, the latter
particularly relevant for a therapeutic aimed at improving muscle
Details of the first-in-human clinical trial
The primary endpoints of the first-in-human trial were to determine the
tolerability and pharmacokinetics of the candidate drug GLPG0492. The
blind, single ascending dose study was conducted in 16 young healthy
volunteers, with 12 receiving ascending doses of GLPG0492 (ranging 0.5 to
mg) and four receiving placebo. Another group of 12 elderly subjects (> 60
years) received three single 100 mg doses once weekly over a three week
to compare the PK profile of the oral solution and capsule formulation.
About GLPG0492 and cachexia
GLPG0492 is an orally available small molecule that Galapagos has
its selective androgen receptor modulator (SARM) program. In pre-
studies, GLPG0492 has shown efficacy in the treatment of cachexia,
involuntary loss of weight and muscle mass which can affect patients
diseases such as cancer, chronic obstructive pulmonary disease (COPD) and
It is estimated that worldwide more than two million people die annually
the consequences of cancer-related cachexia.
Candidate drug GLPG0492 has been shown to improve muscle mass in animal
with minimal cardiovascular, prostate, or virility side effects
seen in androgen therapies. Galapagos aims for once-a-day oral dosing
improves muscle mass and function, with minimal effects on hormonal
patients. With the support of two foundations - Charley's Fund and the
Avery Foundation - Galapagos is currently evaluating the potential
of GLPG0492 in pre-clinical models of Duchenne muscular dystrophy.
Galapagos aims to complete the Proof of Concept study for GLPG0492 in the
of 2011 before out-licensing the program.
Galapagos (Euronext: GLPG; OTC: GLPYY) is a mid-size biotechnology
specialized in the discovery and development of small molecule and
therapies with novel modes-of-action. The Company is progressing one
largest pipelines in biotech, with six clinical and over 50 small
discovery/pre-clinical programs. Through risk/reward-sharing alliances
GlaxoSmithKline, Lilly, Janssen Pharmaceutica, Merck & Co., Roche and
Galapagos is eligible to receive up to EUR3.3 billion in downstream
plus royalties. The Galapagos Group has over 800 employees and
facilities in seven countries, with global headquarters in Mechelen,
More info at: www.glpg.com
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 Muscaritoli et al, Asia Pac J Clin Nutr 2008;17 (S1):387-390
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