Galapagos NV has initiated phase-I clinical development of its novel mechanism of action, first-in-class candidate drug GLPG0259 for rheumatoid arthritis (RA). GLPG0259 is the first small molecule from Galapagos' target discovery platform to enter the clinic. GLPG0259 targets protein kinase Mapkapk5, which represents a new approach for the treatment of RA. The US Patent Office has granted Galapagos patents on the use of this target for the discovery of RA drugs and on the chemical space around this candidate drug.

Target Mapkapk5 (formerly encoded by Galapagos as GT418) is a new starting point for the treatment of RA. Galapagos discovered and validated the key role of this target in the RA disease process, using its proprietary target discovery technology. Mapkapk5 had not been previously associated with RA; however, Galapagos' internal research indicated that it is involved in a signalling pathway that is central to inflammation. The candidate drug GLPG0259 inhibits Mapkapk5, and demonstrates excellent bone protection and reduced inflammation in a standard RA animal model. GLPG0259 has successfully completed preclinical development. Galapagos received US patents for the use of target Mapkapk5 for the discovery of RA drugs and on the lead series of compounds directed against this target. Similar patents are pending in Europe and other major regions.

GLPG0259 is a compound in Galapagos' internal RA programme, which is part of an alliance with Janssen Pharmaceutica. Upon successful completion of a phase-IIa clinical trial for GLPG0259, Janssen has the exclusive option to license the program for €60 million, with further potential milestones to Galapagos of €776 million and double-digit royalties on global sales.

"Today's entry into the clinic is a true landmark for Galapagos," said Onno van de Stolpe, CEO of Galapagos. "This is the first candidate medicine based on our target platform to enter the clinic and I am extremely proud of our team who made this achievement possible. We moved this RA programme from concept to clinic in less than five years. Furthermore, we possess a broad portfolio of programmes that further solidifies our activity in this therapeutic area."

Galapagos is a drug discovery and development company with small molecule programmes in bone and joint diseases, bone metastasis, cachexia, anti-infectives and metabolic diseases.