GLPG1690 (Ziritaxestat, GLPG 1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.
GLPG1690 (Ziritaxestat) inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma with IC50 of 418 nM, 542 nM, and 242 nM, respectively.
GLPG1690 (Ziritaxestat shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.
GLPG1690 also is an inhibitor of the ectonucleotide pyrophosphatase/ phosphodiesterase family (ENPP2).
