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Roxadustat

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Roxadustat
Clinical data
Other namesFG-4592
ATC code
  • None
Identifiers
  • 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.245.356 Edit this at Wikidata
Chemical and physical data
FormulaC19H16N2O5
Molar mass352.340 g/mol g·mol−1
3D model (JSmol)
  • CC1=NC(=C(C2=C1C=C(C=C2)OC3=CC=CC=C3)O)C(=O)NCC(=O)O

Roxadustat (INNTooltip International Nonproprietary Name) (FG-4592) 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, as it has already been detected being used illicitly by athletes despite not having yet been approved for medical use.[3][4][5]

See also

References

  1. ^ Provenzano R, Besarab A, Sun CH, Diamond SA, Durham JH, Cangiano JL, Aiello JR, Novak JE, Lee T, Leong R, Roberts BK, Saikali KG, Hemmerich S, Szczech LA, Yu KH, Neff TB. Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for the Treatment of Anemia in Patients with CKD. Clin J Am Soc Nephrol. 2016 Jun 6;11(6):982-91. . doi:10.2215/CJN.06890615. PMID 27094610. {{cite journal}}: Cite journal requires |journal= (help); Missing or empty |title= (help)
  2. ^ Becker K, Saad M. A New Approach to the Management of Anemia in CKD Patients: A Review on Roxadustat. Adv Ther. 2017 Apr;34(4):848-853. . doi:10.1007/s12325-017-0508-9. PMID 28290095. {{cite journal}}: Cite journal requires |journal= (help); Missing or empty |title= (help)
  3. ^ Beuck S, Schänzer W, Thevis M. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. Drug Test Anal. 2012 Nov;4(11):830-45. . doi:10.1002/dta.390. PMID 22362605. {{cite journal}}: Cite journal requires |journal= (help); Missing or empty |title= (help)
  4. ^ Buisson C, Marchand A, Bailloux I, Lahaussois A, Martin L, Molina A. Detection by LC-MS/MS of HIF stabilizer FG-4592 used as a new doping agent: Investigation on a positive case. J Pharm Biomed Anal. 2016 Mar 20;121:181-187. . doi:10.1016/j.jpba.2016.01.029. PMID 26808067. {{cite journal}}: Cite journal requires |journal= (help); Missing or empty |title= (help)
  5. ^ Eichner D, Van Wagoner RM, Brenner M, Chou J, Leigh S, Wright LR, Flippin LA, Martinelli M, Krug O, Schänzer W, Thevis M. Implementation of the prolyl hydroxylase inhibitor Roxadustat (FG-4592) and its main metabolites into routine doping controls. Drug Test Anal. 2017 Apr 4. . doi:10.1002/dta.2202. PMID 28378453. {{cite journal}}: Cite journal requires |journal= (help); Missing or empty |title= (help)
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