FG-2216

FG‑2216 is a potent, orally active small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (PHD2). By inhibiting PHD2, it stabilizes hypoxia-inducible transcription factors (HIFs), particularly HIF‑1α, independent of oxygen availability. This leads to increased expression of HIF target genes such as erythropoietin (EPO), glucose transporters, glycolytic enzymes, and vascular endothelial growth factor. The primary pharmacological effect observed in clinical studies is robust induction of erythropoietin and modest increases in fetal hemoglobin. FG‑2216 has been investigated for the treatment of anemia associated with chronic kidney disease and end-stage renal disease[1][2][5].

Other names

N-[(1-chloro-4-hydroxyisoquinolin-3-yl)carbonyl]glycine(1-chloro-4-hydroxyisoquinoline-3-carbonyl)glycine2-(1-chloro-4-hydroxyisoquinoline–3-carboxamido)acetic acidCHEMBL426560CHEMBL-426560CHEMBL 426560