Biochem/physiol Actions
Orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (HIF-PH) PHD inhibitor with erythropoiesis-stimulatory efficacy in vivo.
Roxadustat (FG-4592) is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (HIF-PH) PHD inhibitor that enhances the expression of hypoxia early response genes in cultures and in vivo by stabilizing HIF. Roxadustat protects PC12 from TBHP-induced apoptosis by upregulating cellular HIF-1α (62% without vs 21% with 6h 20 µM roxadustat pretreatment prior to 4h 150 µM TBHP induction). Roxadustat stimulates circulating EPO production in mice in vivo (40 or 80 mg/kg p.o.).