Synonyms: compound 14 [PMID: 29259755] | Enaroy® | JTZ-951 | JTZ951
enarodustat is an approved drug
Compound class:
Synthetic organic
Comment: Enarodustat (JTZ-951) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) enzyme activity [3]. Inhibition of prolyl hydroxylation of HIF transcription factors is used as an alternative to erythropoiesis-stimulating agents (epoetin, darbepoetin) for the treatment of anaemia resulting from chronic kidnery disease [1,4].
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. Fukui K, Shinozaki Y, Kobayashi H, Deai K, Yoshiuchi H, Matsui T, Matsuo A, Matsushita M, Tanaka T, Nangaku M. (2019)
JTZ-951 (enarodustat), a hypoxia-inducibe factor prolyl hydroxylase inhibitor, stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor. Eur J Pharmacol, 859: 172532. [PMID:31301309] |
2. Markham A. (2021)
Enarodustat: First Approval. Drugs, 81 (1): 169-174. [PMID:33320297] |
3. Ogoshi Y, Matsui T, Mitani I, Yokota M, Terashita M, Motoda D, Ueyama K, Hotta T, Ito T, Hase Y et al.. (2017)
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. ACS Med Chem Lett, 8 (12): 1320-1325. [PMID:29259755] |
4. (2017)
Erratum Regarding "Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD" (Am J Kidney Dis. 2017;69[6]:815-826). Am J Kidney Dis, 69 (6): 869. [PMID:28532635] |