Synonyms: AKB-6548 | AKB6548 | Vafseo®
vadadustat is an approved drug (Japan (2020), EMA (2023), FDA (2024))
Compound class:
Synthetic organic
Comment: Vadadustat is an orally bioavailable HIF prolyl-hydroxylase inhibitor. It targets the enzymes PHD1, PHD2 and PHD3 to mediate an increase in endogenous erythropoietin production which delivers anti-anemia action. See also enarodustat.
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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References |
1. Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR. (2018)
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. J Med Chem, 61 (16): 6964-6982. [PMID:29712435] |
2. Langley GW, Abboud MI, Lohans CT, Schofield CJ. (2019)
Inhibition of a viral prolyl hydroxylase. Bioorg Med Chem, 27 (12): 2405-2412. [PMID:30737136] |
3. Markham A. (2020)
Vadadustat: First Approval. Drugs, 80 (13): 1365-1371. [PMID:32852744] |
4. Yeh TL, Leissing TM, Abboud MI, Thinnes CC, Atasoylu O, Holt-Martyn JP, Zhang D, Tumber A, Lippl K, Lohans CT et al.. (2017)
Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. Chem Sci, 8 (11): 7651-7668. [PMID:29435217] |