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GLPG1690 + voriconazole
- Development stage
- Discontinued
- Lead developer
- Galapagos
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**GLPG1690 + voriconazole** is a combination of ziritaxestat (coded as GLPG1690), a small molecule, selective autotaxin inhibitor, and voriconazole, a triazole antifungal. Ziritaxestat was developed for fibrotic diseases (notably idiopathic pulmonary fibrosis and systemic sclerosis) but its development has been discontinued. Autotaxin inhibition by ziritaxestat reduces lysophosphatidic acid, a lipid mediator implicated in fibrosis and inflammation. Voriconazole is an antifungal that acts primarily via inhibition of 14\u03b1-demethylase (CYP51A1) in fungi. The combination has been studied in healthy volunteers primarily to evaluate pharmacokinetic drug-drug interactions, as voriconazole is a strong CYP3A4 inhibitor and affects the metabolism of GLPG1690, leading to markedly increased GLPG1690 exposure.
- Brand names
- Vfend
- Other names
- ziritaxestat + voriconazole
02
Targets
ENPP2 (Ectonucleotide pyrophosphatase/phosphodiesterase family member 2)CYP51A1 (Sterol 14α-demethylase)
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