FG-2216 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 3.9 micromolar). It has been shown to reversibly stimulate erythropoietin secretion at 100 μM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.
FG 2216 is an erythropoietic agent which is orally active prolyl-hydroxylase inhibitor which increases erythropoietin production in end-stage kidney disease.
BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD). BIQ induces significant and reversible plasma erythropoietin (EPO) levels in vitro and in hemodialysis patients.
1. hsieh mm, linde ns, wynter a et al. hif prolyl hydroxylase inhibitionresults in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. blood. 2007 sep 15;110(6):2140-7.
