Galapagos’ Rheumatoid Arthritis Drug Catches Investors Interest

Phase II study data on Galapagos’ rheumatoid arthritis drug has caused curiosity within the industry.

Last week, the Belgian drug maker revealed statistics from a Phase II study of GLPG0634, which showed that the Janus kinase (JAK)-1 inhibitor reached the primary endpoint of significant improvement in the signs and symptoms of rheumatoid arthritis (RA). The 36-patient trial lasted for four weeks, with 83% of patients showing an improvement in ACR20 levels at just four weeks.

Within the study, GLPG0634 was administered in two dosages of 200 mg: one group taking a once-daily dose (QD), and the other taking twice-daily doses of 100 mg (BID).

GLPG0634 was well-tolerated, with all patients finishing the trial, and no anaemia or increases in lipids were observed. No severe adverse events were reported.  GLPG0634 is the first JAK1 selective compound to show clinical efficacy, and as the Proof-of-Concept data indicate, this strategy could result in a cleaner safety profile.

GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) currently in development by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases.  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 effectiveness in rheumatoid arthritis trials with an early onset of action.

“We noticed a rapid and remarkable response for the RA patients participating in this trial, with no treatment-emergent safety signals arising,” commented Minodora Mazur, MD, PhD, Professor Internal Medicine & Rheumatology, State Medical and Pharmaceutical University “Nicolae Testemitanu” and Principal Investigator for the trial. “Patients did very well while on therapy – in fact, many reported significant improvements after one week of treatment,” Mazur added.

Piet Wigerinck, head of development of Galapagos, commented that “despite the short duration of the trial, GLPG0634 shows one of the highest initial response rates ever reported for RA treatments”. If this efficacy and safety profile is maintained in longer studies, the drug “has the potential to become a blockbuster treatment for RA and other inflammatory diseases”, he added.

Galapagos plans to initiate an extended dose-range study for the drug in the first half of 2012. This will further outline the optimal doses for efficacy and safety to be evaluated in longer term studies of patients.

Galapagos expects group revenues of 146 million euros for 2011 and positive operational and net earnings. However it notes that “this guidance will only be achievable in the event the GLPG0634 programme is successfully partnered before year-end.” The Mechelen-based firm is in discussions with a number of drugmakers but “has not yet decided whether or not to partner, and on which conditions”.

Galapagos’ stocks jumped roughly 22% on the news, and analysts at Edison Investment Research issued a comment saying that “this has pitched this hitherto almost unknown compound squarely into the high-profile oral disease-modifying anti-rheumatic drugs (DMARD) space behind the two potential blockbusters of Pfizer’s tofacitinib and AstraZeneca’s fostamatinib”.

In terms of partnering, Edison says it appears that Galapagos “may have had an option-based offer on the table, but it probably makes more sense to retain rights and conduct further studies”.


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