Molidustat

Molidustat
Clinical data
Other names	Bay 85-3934
ATC code	None;
Identifiers
	IUPAC name 2-(6-Morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one;
CAS Number	1154028-82-6;
PubChem CID	59603622;
UNII	9JH486CZ13;
KEGG	D12122;
CompTox Dashboard (EPA)	DTXSID80151089 ;
ECHA InfoCard	100.248.923
Chemical and physical data
Formula	C13H14N8O2
Molar mass	314.309 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4;
	InChI InChI=1S/C13H14N8O2/c22-13-10(20-2-1-16-18-20)8-17-21(13)12-7-11(14-9-15-12)19-3-5-23-6-4-19/h1-2,7-9,17H,3-6H2; Key:IJMBOKOTALXLKS-UHFFFAOYSA-N;

Molidustat (INNTooltip International Nonproprietary Name; Bay 85-3934) is a drug which acts as an HIF prolyl-hydroxylase inhibitor and thereby increases endogenous production of erythropoietin, which stimulates production of hemoglobin and red blood cells. It is in Phase III clinical trials for the treatment of anemia caused by chronic kidney disease.^[1]^[2] Due to its potential applications in athletic doping, it has also been incorporated into screens for performance-enhancing drugs.^[3]

References

^ Flamme I, Oehme F, Ellinghaus P, Jeske M, Keldenich J, Thuss U (2014). "Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects". PLOS ONE. 9 (11): e111838. Bibcode:2014PLoSO...9k1838F. doi:10.1371/journal.pone.0111838. PMC 4230943. PMID 25392999.
^ Gupta N, Wish JB (June 2017). "Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD". American Journal of Kidney Diseases. 69 (6): 815–826. doi:10.1053/j.ajkd.2016.12.011. PMID 28242135.
^ Dib J, Mongongu C, Buisson C, Molina A, Schänzer W, Thuss U, Thevis M (January 2017). "Mass spectrometric characterization of the hypoxia-inducible factor (HIF) stabilizer drug candidate BAY 85-3934 (molidustat) and its glucuronidated metabolite BAY-348, and their implementation into routine doping controls". Drug Testing and Analysis. 9 (1): 61–67. doi:10.1002/dta.2011. PMID 27346747.

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