Daprodustat

Daprodustat
Clinical data
Other names	GSK1278863
ATC code	B03XA07 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinane-5-carbonyl)amino]acetic acid;
CAS Number	960539-70-2;
PubChem CID	91617630;
DrugBank	DB11682;
ChemSpider	33427356;
UNII	JVR38ZM64B;
KEGG	D10874;
ChEMBL	ChEMBL3544988;
Chemical and physical data
Formula	C19H27N3O6
Molar mass	393.440 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C3CCCCC3n(c(=O)c1C(=O)NCC(=O)O)c(=O)n(c1O)C2CCCCC2;
	InChI InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,26H,1-11H2,(H,20,25)(H,23,24); Key:NVTKJBXOBFRPLQ-UHFFFAOYSA-N;

Daprodustat (INN, trade name Duvroq in Japan, development code GSK1278863) is a drug which acts as a 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] Daprodustat was approved in Japan in June 2020 for the treatment of patients with anemia due to chronic kidney disease.^[3] Due to its potential applications in athletic doping, it has also been incorporated into screens for performance-enhancing drugs.^[4]

References[]

^ Schmid H, Jelkmann W (August 2016). "Investigational therapies for renal disease-induced anemia". Expert Opinion on Investigational Drugs. 25 (8): 901–16. doi:10.1080/13543784.2016.1182981. PMID 27122198. S2CID 32493057.
^ Ariazi JL, Duffy KJ, Adams DF, Fitch DM, Luo L, Pappalardi M, et al. (December 2017). "Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor-Prolyl Hydroxylase Inhibitor for Anemia". The Journal of Pharmacology and Experimental Therapeutics. 363 (3): 336–347. doi:10.1124/jpet.117.242503. PMID 28928122.
^ "GSK receives first regulatory approval for Duvroq (daprodustat) in Japan for patients with anaemia due to chronic kidney disease" (Press release). GSK. 29 June 2020.
^ Thevis M, Milosovich S, Licea-Perez H, Knecht D, Cavalier T, Schänzer W (August 2016). "Mass spectrometric characterization of a prolyl hydroxylase inhibitor GSK1278863, its bishydroxylated metabolite, and its implementation into routine doping controls". Drug Testing and Analysis. 8 (8): 858–63. doi:10.1002/dta.1870. PMID 26361079.

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[1] Schmid H, Jelkmann W (August 2016). "Investigational therapies for renal disease-induced anemia". Expert Opinion on Investigational Drugs. 25 (8): 901–16. doi:10.1080/13543784.2016.1182981. PMID 27122198. S2CID 32493057.

[2] Ariazi JL, Duffy KJ, Adams DF, Fitch DM, Luo L, Pappalardi M, et al. (December 2017). "Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor-Prolyl Hydroxylase Inhibitor for Anemia". The Journal of Pharmacology and Experimental Therapeutics. 363 (3): 336–347. doi:10.1124/jpet.117.242503. PMID 28928122.

[3] "GSK receives first regulatory approval for Duvroq (daprodustat) in Japan for patients with anaemia due to chronic kidney disease" (Press release). GSK. 29 June 2020.

[4] Thevis M, Milosovich S, Licea-Perez H, Knecht D, Cavalier T, Schänzer W (August 2016). "Mass spectrometric characterization of a prolyl hydroxylase inhibitor GSK1278863, its bishydroxylated metabolite, and its implementation into routine doping controls". Drug Testing and Analysis. 8 (8): 858–63. doi:10.1002/dta.1870. PMID 26361079.

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Daprodustat

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