Mechelen, Belgium; 6 August 2009 – Galapagos NV (Euronext: GLPG) announces the successful completion its first-in-human trial of the novel candidate drug GLPG0259 for rheumatoid arthritis (RA). The candidate drug showed good safety in healthy volunteers and an excellent pharmacokinetic (PK) profile thus far, which supports once-daily oral dosing. GLPG0259 is a novel mechanism-of-action inhibitor of the protein kinase MAPKAPK5, which was discovered through Galapagos’ target discovery platform and represents a new approach for the treatment of RA.
The goal of the first-in-human trial was to determine the safety, tolerability, and pharmacokinetics of the candidate drug GLPG0259. The double blind, single ascending and multiple dose study was conducted in 34 healthy volunteers in Belgium from March to May 2009. The compound was administered up to five consecutive days and showed good safety, with no cardiovascular side effects. The desired PK profile obtained thus far supports once-daily oral dosing.
“We are encouraged by the positive outcome of the first human trial for a candidate drug derived from Galapagos’ target discovery platform,” said Onno van de Stolpe, CEO of Galapagos. “We are on track to complete the Phase I trials for GLPG0259 by the end of 2009. Furthermore, preparations are underway to start a Phase IIa study in 2010, where we will assess the efficacy of this novel mechanism of action candidate drug in treating RA patients.”
About MAPKAPK5 and candidate drug GLPG0259
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 showed that it plays a key role in inflammation and in the breakdown of collagen in human cartilage. The candidate drug GLPG0259 inhibits MAPKAPK5 in the human cell, and demonstrated excellent bone protection and reduced inflammation in a standard RA animal model.
GLPG0259 is a compound in Galapagos’ internal RA program, which is part of an option agreement with Janssen Pharmaceutica. Upon the completion of a dose finding Phase II 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.
About Galapagos
Galapagos (Euronext: GLPG; OTC: GLPYY) is a drug discovery and development company with small molecule programs in bone and joint diseases, bone metastasis, cachexia, anti-infectives and metabolic diseases. It has established risk sharing alliances with GSK, Janssen Pharmaceutica, Eli Lilly and Merck. Through an alliance with MorphoSys, Galapagos is also developing new antibody therapies in bone and joint diseases. Its division BioFocus DPI offers a full suite of target-to-drug discovery products and services to pharmaceutical and biotech companies and to patient foundations, encompassing target discovery and validation, screening and drug discovery through to delivery of pre-clinical candidates. Galapagos currently employs 495 people and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More info at: www.glpg.com.
CONTACT
Galapagos NV
Onno van de Stolpe, CEO
Tel: +31 6 2909 8028
This release may contain forward-looking statements, including, without limitation, statements containing the words “believes,” “anticipates,” “expects,” “intends,” “plans,” “seeks,” “estimates,” “may,” “will,” “could,” “stands to,” and “continues,” as well as similar expressions. Such forward-looking statements may involve known and unknown risks, uncertainties and other factors which might cause the actual results, financial condition, performance or achievements of Galapagos, or industry results, to be materially different from any historic or future results, financial conditions, performance or achievements expressed or implied by such forward-looking statements. Given these uncertainties, the reader is advised not to place any undue reliance on such forward-looking statements. These forward-looking statements speak only as of the date of publication of this document. Galapagos expressly disclaims any obligation to update any such forward-looking statements in this document to reflect any change in its expectations with regard thereto or any change in events, conditions or circumstances on which any such statement is based, unless required by law or regulation.