Daprodustat

Daprodustat
Names
Trade namesDuvroq, Jesduvroq
Other namesGSK1278863
IUPAC name
  • 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinane-5-carbonyl)amino]acetic acid
Clinical data
Drug classHypoxia-inducible factor prolyl hydroxylase inhibitor[1]
Main usesLow red blood cells due to chronic kidney disease[1]
Side effectsHigh blood pressure, blood clots, abdominal pain[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use
By mouth[1]
Typical dose1 to 24 mg OD[1]
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Chemical and physical data
FormulaC19H27N3O6
Molar mass393.440 g·mol−1
3D model (JSmol)
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, sold under the brand name Duvroq among others, is a medication used to treat low red blood cells due to chronic kidney disease.[1] It is used in those who have been on dialysis for more than four months.[1] It is taken by mouth.[1] It is used to reduce the need for blood transfusions.[1]

Common side effects include high blood pressure, blood clots, and abdominal pain.[1] Other side effects may include worsening heart failure and upper gastrointestinal bleeding.[1] Use may increase the risk of death.[1] It is not recommended in those with active cancer.[1] It interacts with medications that affect CYP2C8.[1] Use in pregnancy may harm the baby.[1] It is a hypoxia-inducible factor prolyl hydroxylase inhibitor which works by increasing erythropoietin.[1][2]

Daprodustat was approved for medical use in Japan in 2020,[2] and the United States in 2023.[1] It is the first by mouth treatment for low red blood cells caused by kidney disease.[3][4] Previously injectable erythropoiesis-stimulating agents were used for this purpose.[5]

Medical uses

Daprodustat is indicated for the treatment of anemia due to chronic kidney disease.[1]

Dosage

It is taken once per day at a dose of 1 mg to 24 mg.[1]

History

Daprodustat increases erythropoietin levels.[3] The effectiveness of daprodustat was established in a randomized study of 2,964 adult participants receiving dialysis.[3] In this study, participants received either oral daprodustat or injected recombinant human erythropoietin (a standard of care treatment for people with anemia due to chronic kidney disease).[3] Daprodustat raised and maintained the hemoglobin (the protein in red blood cells that carries oxygen and is a common measure of anemia) within the target range of 10-11 grams/deciliter, similar to that of the recombinant human erythropoietin.[3] The US Food and Drug Administration (FDA) granted the approval of Jesduvroq to GlaxoSmithKline LLC.[3]

Society and culture

Due to its potential applications in athletic doping, it has also been incorporated into screens for performance-enhancing drugs.[6]

References

  1. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 "Jesduvroq- daprodustat tablet, film coated". DailyMed. 1 February 2023. Archived from the original on 11 February 2023. Retrieved 11 February 2023.
  2. 1 2 Dhillon S (September 2020). "Daprodustat: First Approval". Drugs. 80 (14): 1491–1497. doi:10.1007/s40265-020-01384-y. PMC 7471535. PMID 32880805.
  3. 1 2 3 4 5 6 "FDA Approves First Oral Treatment for Anemia Caused by Chronic Kidney Disease for Adults on Dialysis". U.S. Food and Drug Administration (FDA) (Press release). 1 February 2023. Archived from the original on 4 February 2023. Retrieved 3 February 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  4. Harris, Emily (15 February 2023). "FDA Approves First Oral Treatment for Kidney Disease–Induced Anemia". Medical News in Brief. JAMA. 329 (9): 704. doi:10.1001/jama.2023.1556. PMID 36790833. Archived from the original on 19 March 2023. Retrieved 3 May 2023.
  5. "Issue 4 - March 1, 2023". www.pbdrx.com. Archived from the original on 30 June 2023. Retrieved 14 May 2023.
  6. 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.
Identifiers:
  • Clinical trial number NCT02879305 for "Anemia Studies in Chronic Kidney Disease: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor Daprodustat-Dialysis (ASCEND-D)" at ClinicalTrials.gov
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