Chemical Name: N-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]-glycine
Synonyms: FG-4592, ASP1517, Roxadustat
The hypoxia-inducible factor (HIF) pathway alters gene expression in response to low oxygen tension. Under normoxic conditions, HIF-specific prolyl hydroxylases (HIF-PHs) initiate the degradation of oxygen-sensitive HIF isoforms. As 2-oxoglutarate (2-OG) is a required co-factor for HIF-PH activity, analogs of 2-OG may inhibit HIF-PH and prevent HIF turnover.
FG-4592 is an analog of 2-OG that has been developed as an inhibitor of HIF-PHs. It induces EPO expression, promoting red blood cell production in vivo.
This substance has passed through Phase III clinical trials with successful outcomes.