Galapagos presents GLPG0634 at EULAR poster session

Posters now available online at www.glpg.com
Q&A session with Galapagos CSO today at 15.00 CET/9 AM EDT/6 AM PT, call numbers for the teleconference call: US +1-480-629-9645, Toll-free +1-877-941-60; Belgium +32-2290-1608, Toll-free 0800-50747; Netherlands +31 20 794 8504, Toll-free 0800-265-8528

Mechelen, Belgium; 13 June 2013 - Galapagos NV (Euronext: GLPG) is presenting three posters on its selective JAK1 inhibitor GLPG0634 at the European League Against Rheumatism (EULAR) Annual Congress taking place this week in Madrid, Spain.  The posters are available online at www.glpg.com.

Chief Scientific Officer Dr Piet Wigerinck will answer questions about the posters in a teleconference call at 15.00 CET/9 am EDT/6 am PT, call numbers US +1-480-629-9645, Toll-free +1-877-941-60; Belgium +32-2290-1608, Toll-free 0800-50747; Netherlands +31 20 794 8504, Toll-free 0800-265-8528.  A recording of the teleconference call will be archived on Galapagos' website.

Following is an overview of the posters, with key conclusions:

Safety and efficacy of GLPG0634, a selective JAK1 inhibitor, in patients with rheumatoid arthritis: results of a 4-week Phase IIA dose ranging, multi-center trial

Selective inhibition of JAK1 by once-daily dosing of GLPG0634 from 75 - 300 mg was well tolerated and efficacious in this 4-week study.  A favourable safety profile was observed, with an absence of the typical findings reported for other JAK inhibitors.  GLPG0634 caused no anemia, no overall change to LDL or ALT, and no neutropenia.  Regarding efficacy, a dose trend for improvement in RA disease parameters was found: 30 mg QD was sub-optimal, while doses of 75, 150 and 300 mg showed promising efficacy, with similar response rates in CRP, TJC, SJC and DAS28.

An imbalance in baseline characteristics of two patient groups may have influenced the study outcome:
·     the placebo group showed a relatively high response rate correlating with a short history of RA
·     the 150 mg group was most severely diseased.  The 150 mg group showed a robust response in CRP, TJC, and SJC.  However, the 4-week duration of the trial was too short to reach the full potential on patient-reported scores (pain assessment, global assessment, HAQ-DI).

The encouraging short term efficacy and favourable safety profile in this study supports the potential of selective inhibition of JAK1 as a future RA treatment option, and confirms data from a previous Proof of Concept study at a 200 mg daily dose.

Once-daily dosing of GLPG0634, a selective JAK1 inhibitor, is supported by its active metabolite

An active and JAK1-selective metabolite supports the activity of GLPG0634.  The lower potency of the metabolite is compensated by its high exposure in humans.  The long half-life of the metabolite and the resulting high plasma levels when parent GLPG0634 is at trough, provides a lasting effect.  Because of the 7-hour half-life of GLPG0634, both BID and QD regimens were studied.  However, the metabolite contribution to JAK1 inhibition now provides a potential explanation for the sustained efficacy results observed with once daily dosing of GLPG0634, adding to convenience for patients.

Biological effects of the JAK1 selective inhibitor GLPG0634 on inflammation markers in arthritic mice

Oral administration of the selective JAK1 inhibitor GLPG0634 in arthritic mice demonstrates a selective engagement of the JAK1 target by GLPG0634 in vivo.  Progression of established arthritis in the CIA model is blocked by selective inhibition of JAK1.  GLPG0634 administration inhibits inflammation and confers structural protection at the level of bone and cartilage in a therapeutic CIA model.  A single administration of GLPG0634 is sufficient to block CIA-induced inflammatory signalling.

About candidate drug GLPG0634
GLPG0634 is an orally-available, novel Janus kinase (JAK) inhibitor with selectivity for JAK1 developed by Galapagos.  JAKs are critical components of signalling mechanisms utilized by a number of cytokines and growth factors, including those that are elevated in rheumatoid arthritis patients.  JAK inhibitors have shown long-term efficacy in rheumatoid arthritis studies with an early onset of action.  GLPG0634 differentiates from other JAK inhibitors in development by specifically targeting JAK1, a strategy which could result in a better efficacy and safety profile.  GLPG0634 is a fully proprietary program.  Upon successful completion of the Phase 2b studies in RA, AbbVie will license the program and will assume sole responsibility for Phase 3 clinical development and global manufacturing.  Furthermore, AbbVie and Galapagos recently announced the initiation of a Phase 2 study with GLPG0634 in Crohn's Disease.

About EULAR
The annual EULAR congresses are a major event in the calendar of world rheumatology.  The aim is to provide a forum of the highest standard for scientific (both clinical and basic), educational and social exchange between professionals involved in rheumatology, liaising with patient organisations, in order to achieve progress in the clinical care of patients with rheumatic diseases.  More info at: www.eular.org

About Galapagos
Galapagos (Euronext: GLPG; OTC: GLPYY) is specialized in novel modes-of-action, with a large pipeline of four clinical, seven pre-clinical, and 30 discovery small-molecule and antibody programs in cystic fibrosis, inflammation, antibiotics, metabolic disease, and other indications.
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 about to enter Phase 2 studies in Crohn's disease.  AbbVie and Galapagos signed a worldwide license agreement whereby AbbVie will be responsible for further development and commercialization after Phase 2b.  Galapagos has another selective JAK1 inhibitor in Phase 2 in lupus and psoriasis, GSK2586184 (formerly GLPG0778, in-licensed by GlaxoSmithKline in 2012).  GLPG0187 is a novel integrin receptor antagonist currently in a Phase 1b patient study in metastasis.  GLPG0974 is the first inhibitor of GPR43 to be evaluated clinically for the treatment of IBD; this program is currently in a Proof of Concept Phase 2 study.
The Galapagos Group, including fee-for-service companies BioFocus, Argenta and Fidelta, has 800 employees and operates facilities in five countries, with global headquarters in Mechelen, Belgium.  Further information at: www.glpg.com

CONTACT

Galapagos NV
Piet Wigerinck, CSO
Tel: +32 477 62 7103

Elizabeth Goodwin, Director Investor Relations
Tel: +31 6 2291 6240
ir@glpg.com

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