GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

When GLPG1205 is administered at a concentration of 1 μM for a duration of 5 minutes, it effectively prevents the generation of reactive oxygen species (ROS) triggered by the GPR84 agonist. In TNF-α primed neutrophils, GLPG1205 exhibits strong antagonistic activity against ZQ16-induced ROS, with an IC50 value of 15 nM. Additionally, at a concentration of 0.5 μM, GLPG1205 completely suppresses the ZQ16-induced increase in intracellular calcium levels ([Ca2+]i) in neutrophils[1].

GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model. GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model. Oral administration of GLPG1250 (30mg/kg; twice daily for 2 weeks, starts from 7 days post-challenge) greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model. Oral administration of GLPG1250 (30mg/kg; once daily starts from 18 weeks post irradition) significantly reduces college deposition in the mouse lung[1].