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Beschreibung

An orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-beta isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively, 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC, 101 nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30 mg/kg, p.o.).