Molidustat

Molidustat
Clinical data
Trade names	Varenzin-CA1
Other names	Bay 85-3934
Routes of; administration	By mouth
ATC code	None;
Legal status
Legal status	US: ℞-only;
Identifiers
	IUPAC name 2-(6-Morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one;
CAS Number	1154028-82-6; 1375799-59-9;
PubChem CID	59603622;
DrugBank	DB15642; DBSALT002944;
ChemSpider	30922476; 32699298;
UNII	9JH486CZ13; CI0NE7C96T;
KEGG	D12122;
ChEMBL	ChEMBL3646118;
PDB ligand	A1H (PDBe, RCSB PDB);
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 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.^[2]^[3] Due to its potential applications in athletic doping, it has also been incorporated into screens for performance-enhancing drugs.^[4]

Veterinary use

Molidustat is indicated for the control of nonregenerative anemia associated with chronic kidney disease in cats.^[1]^[5] The US Food and Drug Administration (FDA) conditionally approved it in May 2023.^[5]

The reasonable expectation of effectiveness of Molidustat was evaluated in a study conducted in two phases.^[5] The first phase involved a multi-center, double-masked, randomized, placebo-controlled field effectiveness and safety study.^[5] The second phase was an unmasked, optional continuation of the field study.^[5] The study enrolled 23 cats from 4 to 17 years of age from various breeds or breed mixes diagnosed with nonregenerative anemia associated with CKD.^[5] The FDA granted conditional approval of Varenzin-CA1 to Elanco US Inc.^[5]

References

^ ^a ^b "Archived copy". Archived from the original on 2023-05-02. Retrieved 2023-05-02.{{cite web}}: CS1 maint: archived copy as title (link)
^ 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, et al. (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.
^ ^a ^b ^c ^d ^e ^f ^g "FDA Conditionally Approves First Drug for Anemia in Cats with Chronic Kidney Disease". U.S. Food and Drug Administration (Press release). 1 May 2023. Archived from the original on 1 May 2023. Retrieved 1 May 2023. This article incorporates text from this source, which is in the public domain.

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[Varenzin-CA1_FOI_Summary-1] "Archived copy". Archived from the original on 2023-05-02. Retrieved 2023-05-02.{{cite web}}: CS1 maint: archived copy as title (link)

[2] 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.

[3] 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.

[4] Dib J, Mongongu C, Buisson C, Molina A, Schänzer W, Thuss U, et al. (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.

[FDA_PR_20230501-5] ^ ^a ^b ^c ^d ^e ^f ^g "FDA Conditionally Approves First Drug for Anemia in Cats with Chronic Kidney Disease". U.S. Food and Drug Administration (Press release). 1 May 2023. Archived from the original on 1 May 2023. Retrieved 1 May 2023. This article incorporates text from this source, which is in the public domain.

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