Galapagos is applying its functional screening program to discover novel drugable targets in rheumatoid arthritis (RA).

We have developed assays in human primary rheumatoid arthritis synovial fibroblasts (RASFs) that measure activation of RASF mediated collagen degradation pathways. SilenceSelect and FLeXSelect are screened in these assays to identify drugable targets that inhibit RASF mediated collagen degradation. These hits are then validated through a small selection of secondary validation assays, in order to select a final set of high value, novel, drugable RA targets for compound screening.

Galapagos has achieved a reduction in disease-causing cytokines and reduced paw swelling in a therapeutic mouse RA model. Recently, the Company reported that these lead compounds also show substantial protection against bone loss in the industry standard RA animal model. Furthermore, the program has achieved relevant potencies and pharmacokinetic profiles for compounds in lead optimization. These compounds target a proprietary kinase protein that was identified using the Galapagos’ SilenceSelect discovery platform. Based on these important results, Galapagos anticipates initiation of preclinical studies in 2007, with a candidate drug expected to enter clinical phase I in 2008.

In October 2007, Galapagos entered into a worldwide multi-target alliance with Janssen Pharmaceutica NV, a Johnson & Johnson company, to discover and develop novel small-molecule therapeutics for the treatment of RA. Under the alliance agreement, Janssen may select up to 12 programs from Galapagos’ internally identified RA targets into the alliance. Janssen receives future option rights to exclusively license these programs. In addition, Janssen obtained an option to the future development and commercialization of product candidates from Galapagos’ other internal RA programs, including its most advanced program based on the kinase target GT418. For more information, please visit the RA alliance page.