Phase II Trial for RA Drug Begins

A phase II clinical study began for Galapagos NV’s drug candidate GLPG0259, a novel drug being developed for rheumatoid arthritis (RA).

The safety and efficacy of the drug candidate will be tested in RA patients during the clinical trial. Galapagos plans to announce interim results by the middle of next year and complete the trial by the end of 2011.

“This trial marks the first time a Galapagos novel target candidate drug is tested in patients,” said Onno van de Stolpe, CEO of Galapagos, in a press release. “We are very proud of the high level of innovation that went into this programme— from the cutting-edge science that led to this new target all the way to the innovative trial design, which will allow us to receive initial efficacy information for this candidate drug by the middle of next year.”

The clinical Proof-of-Concept phase II trial for GLPG0259 will involve 180 RA patients with insufficient response to the standard-of-care treatment, methotrexate (MTX). The aim of the trial is to evaluate the efficacy and safety of GLPG0259 in treating RA.

Patients with moderate to severe RA will be divided into four groups, all continuing to receive a stable background of MTX. Three groups will receive a different once-daily dose of GLPG0259 and the fourth group will receive a placebo, for a period of 12 weeks.

The primary endpoint will be the ACR20 response rate, which is the standard primary endpoint for RA clinical trials.

Galapagos received regulatory approvals to start the pan-European trial, with patient recruitment beginning next month. The trial has been designed to obtain initial efficacy data using the highest dose for the first 30 patients. Twenty of these patients will receive GLPG0259 and 10 will receive placebo in the first half of 2011. Based on this initial readout, Galapagos plans to complete the dose-finding component of the trial by the end of 2011.

The drug candidate GLPG0259 inhibits MAPKAPK5 in human cells, and demonstrates bone protection and reduced inflammation in a standard RA animal model. Protein target MAPKAPK5 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 has shown that it plays a key role in inflammation and in the breakdown of collagen in human cartilage.

Phase I clinical studies for GLPG0259 in healthy volunteers demonstrated good safety. The feasibility of combining GLPG0259 with MTX was also confirmed in the phase I trial.

GLPG0259 is a compound in Galapagos’ internal RA programme, which is part of an option agreement with Janssen Pharmaceutica. Upon the completion of a dose-finding phase II clinical trial for GLPG0259 scheduled to be completed by year end 2011, Janssen has the exclusive option to license the program for €60 million, with further potential milestones to Galapagos of €776 million and up to double-digit royalties on global sales.

Galapagos is a mid-size biotechnology company specialized in the discovery and development of small molecule and antibody therapies with novel modes-of-action.