Synonyms: EXAMPLE 2 [WO2014102818A1] | Oxemia® | ZYAN-1 | ZYAN1
Compound class:
Synthetic organic
Comment: Desidustat (ZYAN1) is an orally bioavailable inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) enzymes (PHD1, PHD2, and PHD3; genes EGLN2, EGLN1 and EGLN3 respectively) [5]. It was developed as a strategy to promote erythropoietin (EPO) synthesis and erythropoiesis by stabilising HIF-α transcription factors, as a mechanism to treat anemia associated with chronic diseases. Orally active HIF-PH inhibitors are being exploited as alternatives to injectable erythropoietin stimulating drugs, such as epoetin and darbepoetin, to treat anemia.
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Bioactivity Comments |
We have been unable to find an inhibitory constant for desidustat 's inhibition of its intended prolyl hydroxylase enzyme targets (EGLN1-3). Stabilisation of HIF-1α, increased erythropoietin levels, decreased hepcidin levels, and elevated erythropoesis are used as surrogate markers of HIF-PH inhibition. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
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