Drug intelligence / Profile preview

ziritaxestat

Development stage
Discontinued
Lead developer
Galapagos
Modality
Small Molecules
Administration
Oral
01

Overview

Ziritaxestat is an investigational small molecule drug that acts as a selective inhibitor of autotaxin (ENPP2 protein), the main enzyme responsible for lysophosphatidic acid (LPA) production. LPA is a pro-fibrotic and pro-inflammatory lipid mediator implicated in diseases such as idiopathic pulmonary fibrosis (IPF) and systemic sclerosis (SSc). By inhibiting autotaxin, ziritaxestat reduces LPA levels, aiming to mitigate fibrotic processes. The drug was co-developed by Galapagos and Gilead Sciences. It reached phase 3 clinical trials for IPF but failed to demonstrate efficacy in these studies; development has been discontinued for all indications[4][5][6][7].

Other names
ziritaxestat2-((2-ethyl-6-(4-(2-(3-hydroxyazetidin-1-yl)-2-oxoethyl)-piperazin-1-yl)-8-methylimidazo[1,2-a]pyridin-3-yl)-(methyl)amino)-4-(4-fluorophenyl)-thiazole-5-carbonitrileziritaxestatum
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)ENPP2 (Ectonucleotide pyrophosphatase/phosphodiesterase family member 2)ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)ABCG2 (Breast cancer resistance protein)CYP2C8 (Cytochrome P450 2C8)

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