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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