Daprodustat

Daprodustat (INN) (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 secondary to 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]

Daprodustat

Clinical data
Other names	GSK1278863
ATC code	None
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
UNII	JVR38ZM64B
KEGG	D10874
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

See also

• Desidustat
• Molidustat
• Roxadustat
• Vadadustat

References

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.
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. 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.