Galapagos Presents Promising Pre-clinical and Phase 1 Results

Galapagos NV presents pre-clinical and Phase 1 results for autotaxin inhibitor GLPG1690 at the European Respiratory Society Annual Meeting in Amsterdam, Netherlands. Galapagos expects to file an exploratory Phase 2 study in idiopathic pulmonary fibrosis before year end.

GLPG1690 has potential application in other pulmonary diseases such as chronic obstructive pulmonary disease (COPD), as supported by the presentation on pre-clinical findings at ERS this year:

"Pharmacological profile and efficacy of GLPG1690, a novel ATX inhibitor for COPD treatment," poster PA2129 in Poster Discussion Session: "New targets and modalities for the treatment of asthma and COPD" (September 28, 2015; Room D201-202, 10:45 AM - 12:45 PM)

Galapagos is the first to show efficacy of an autotaxin inhibitor in pre-clinical models for COPD and IPF, pointing to novel therapeutic areas for autotaxin inhibition. The poster shows how GLPG1690 acts as a potent inhibitor of mouse and human autotaxin (IC50: 100 -500 nM range). Furthermore, GLPG1690 reduces inflammation in a mouse steroid-resistant tobacco smoke model to a similar extent as a standard therapy for COPD.

Galapagos also presents the topline results with GLPG1690 in Phase 1 in healthy human volunteers: "Favorable human safety, pharmacokinetics and pharmacodynamics of the autotaxin inhibitor GLPG1690, a potential new treatment in COPD," oral presentation OA484 in session "Advances in the future treatment of COPD" (September 27, 2015; Room 2.1, 10:45 AM - 12:45 PM)

GLPG1690 was safe and well tolerated up to a single oral dose of 1500 mg and up to 1000 mg twice daily for 14 days, with no significant adverse effects on ECGs, vital signs or laboratory parameters. The compound also showed good oral bioavailability with a half-life of 5 hours and a dose-proportional increase in exposure.

GLPG1690 showed concentration-dependent reduction of a relevant biomarker (plasma LPA18:2 levels) with a maximum of approximately 90%. At steady state, continuous reduction of this biomarker levels of >60% was observed from 0 to 24 hours. The presentation will also include relevant pre-clinical model data for COPD and IPF with GLPG1690.