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 and is likely to be approved for pharmaceutical use in the near future.