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Synonyms: ASP-1517 | ASP1517 | Evrenzo® | FG-4592 | FG4592
roxadustat is an approved drug (EMA (2021))
Compound class: Synthetic organic
Comment: Roxadustat is a compound which inhibits hypoxia inducible factor prolyl hydroxylase (HIF-PH) activity. HIF-PH inhibitors are being investigated as novel therapies for anemia, especially anemia caused by chronic kindney disease (CKD) . It is hoped that HIF-PH inhibitors will provide a more effective alternative to the use of erythropoetin replacement therapy plus iron supplementation in CKD patients.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|Roxadustat was the first HIF-PH inhibitor to reach Phase 3 clinical trial. Click here to link to ClinicalTrials.gov's listing of registered Phase 3 roxadustat trials.
The EMA approved roxadustat for the treatment of anemia due to chronic kidney failure in August 2021.
|Mechanism Of Action and Pharmacodynamic Effects|
|Under normoxic conditions HIF-PH effects the degradation of HIF1-α subunits (using O2 as a substrate to hydroxylate proline residues in HIF-1α), resulting in minimal HIF-induced transcriptional activity. When oxygen levels are limited, HIF-1α is not directed for degradation, permittinh induction of transcription. HIF-PH inhibitors mimic this natural response to hypoxia, which stablises HIFα transcription factors thereby switching on transcription of genes associated with processes such as erythropoiesis and vasculogenesis . In anemic patients HIF-PH inhibitors increase erythropoietin levels and subsequently increase red blood cell counts . There are three human HIF-PHs, with gene symbols EGLN1, -2 and -3.|