Daprodustat

Summary

Daprodustat
Daprodustat structure.png
Clinical data
Other namesGSK1278863
ATC code
  • None
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 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
FormulaC19H27N3O6
Molar mass393.440 g·mol−1
3D model (JSmol)
  • Interactive image
  • C3CCCCC3n(c(=O)c1C(=O)NCC(=O)O)c(=O)n(c1O)C2CCCCC2
  • 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]

See also

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. 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.