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) [2]. 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 ChartsThese 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. ✖ |
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Bioactivity Comments |
We have been unable to find an ihibitory constant for roxadustat's inhibition of HIF-PHs (EGLN1-3). Associated patents examine stabilisation of HIF-1α or increased erythropoietin levels as markers of HIF-PH inhibition. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
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Targets where the ligand is described in the comment field | |
Target | Comment |
Zinc transporter 10 | SLC30A10 mediates manganese excretion, and its expression is enhanced by manganese via an hypoxia-inducible factor (HIF)-regulated pathway [4]. The HIF-stabilising prolyl hydroxylase inhibitor roxadustat reduces manganese-induced neurotoxicity in vivo, which suggests that this mechanism may be a viable treatment option for neurological disease such as manganese-induced parkinsonism in humans. |