In vitro activity: GLPG1690 is a potent and the first selective autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nM. GLPG1690 has the potential applications in the treatment of idiopathic pulmonary disease (IPF). GLPG1690 showed improved pharmacokinetic properties with a low plasma clearance and high bioavailability in mouse and rat. The good pharmacokinetic profile is further confirmed in dog, with GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%). In a Phase 1 study, GLPG1690 demonstrated favorable safety and tolerability profile, as well as a strong pharmacodynamic signal implying target engagement.

Kinase Assay: GLPG1690 is a potent and the first selective autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nM. GLPG1690 shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay

Cell Assay: Ziritaxestat (formerly GLPG1690) is a potent and a first-in-class selective autotaxin (ATX) inhibitor (IC50 = 131 nM and Ki of 15 nM) with the potential to be used in the treatment of idiopathic pulmonary disease (IPF). As of Feb 2021, the phase 3 trial has failed. GLPG1690 showed improved pharmacokinetic properties with a low plasma clearance and high bioavailability in mouse and rat. The good pharmacokinetic profile is further confirmed in dog, with GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%). In a Phase 1 study, GLPG1690 demonstrated favorable safety and tolerability profile, as well as a strong pharmacodynamic signal implying target engagement.