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Lesinurad information


Lesinurad
Clinical data
Pronunciation/lɛˈsɪnjuːræd/
le-SIN-ew-rad
Trade namesZurampic
AHFS/Drugs.comMonograph
MedlinePlusa616015
License data
  • EU EMA: by INN
  • US DailyMed: Lesinurad
Routes of
administration
Oral (tablets)
ATC code
  • M04AB05 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • US: ℞-only
Pharmacokinetic data
Bioavailability~100%[2]
Protein binding>98%
MetabolismHepatic (CYP2C9)
Elimination half-life~5 hours
ExcretionUrine (63%), feces (32%)
Identifiers
IUPAC name
  • 2-{[5-Bromo-4-(4-cyclopropyl-1-naphthyl)-4H-1,2,4-triazol-3-yl]sulfanyl}acetic acid
CAS Number
  • 878672-00-5
PubChem CID
  • 56928182
DrugBank
  • DB11560
ChemSpider
  • 28527877
UNII
  • 09ERP08I3W
KEGG
  • D09921
ChEBI
  • CHEBI:90929 checkY
CompTox Dashboard (EPA)
  • DTXSID201026091 Edit this at Wikidata
ECHA InfoCard100.216.089 Edit this at Wikidata
Chemical and physical data
FormulaC17H14BrN3O2S
Molar mass404.28 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • c1ccc2c(c1)c(ccc2n3c(nnc3Br)SCC(=O)O)C4CC4
InChI
  • InChI=1S/C17H14BrN3O2S/c18-16-19-20-17(24-9-15(22)23)21(16)14-8-7-11(10-5-6-10)12-3-1-2-4-13(12)14/h1-4,7-8,10H,5-6,9H2,(H,22,23)
  • Key:FGQFOYHRJSUHMR-UHFFFAOYSA-N

Lesinurad (brand name Zurampic) is a urate transporter inhibitor for treating high blood uric acid levels associated with gout.[2] It is recommended only as an adjuvant with either allopurinol or febuxostat when these medications are not sufficient.[3]

It received FDA approval on 22 December 2015.[3] The European Commission granted a marketing authorisation valid throughout the European Union on 18 February 2016.[4] In February 2019, lesinurad was discontinued in the United States by its manufacturer for business reasons, and was subsequently withdrawn in Europe in July 2020.[5][6]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  2. ^ a b "Zurampic (lesinurad) Tablets, for Oral Use. Full Prescribing Information" (PDF). AstraZeneca AB, S-151 85 Sodertalje, Sweden. Archived from the original (PDF) on 24 December 2015. Retrieved 23 December 2015.
  3. ^ a b "Drug Trial Snapshot: Zurampic". US Food and Drug Administration. 22 December 2015. Retrieved 14 October 2018.
  4. ^ "EPAR summary for the public" (PDF). EMA. 13 March 2016.
  5. ^ "Duzallo and Zurampic". Ironwood Pharmaceuticals. Archived from the original on 10 August 2020. Retrieved 31 July 2020.
  6. ^ "Duzallo". European Medicines Agency. The European Union. 17 September 2018. Retrieved 2 October 2020.

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Lesinurad

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Lesinurad (brand name Zurampic) is a urate transporter inhibitor for treating high blood uric acid levels associated with gout. It is recommended only...

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ATC code M04

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M04AB02 Sulfinpyrazone M04AB03 Benzbromarone M04AB04 Isobromindione M04AB05 Lesinurad M04AC01 Colchicine M04AC02 Cinchophen M04AC51 Colchicine and probenecid...

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Gout

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rate of side effects and many people develop resistance to it. Using lesinurad 400 mg plus febuxostat is more beneficial for tophi resolution than lesinural...

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Allopurinol

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Milurit, Alloril, Progout, Ürikoliz, Zyloprim, Zyloric, Zyrik, and Aluron. Lesinurad/allopurinol, a fixed-dose combination drug "Allopurinol Use During Pregnancy"...

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Hyperuricemia

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[citation needed] Uricosuric agents (benzbromarone, benziodarone, probenecid, lesinurad, sulfinpyrazone, ethebencid, zoxazolamine, and ticrynafen) increase the...

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SLC22A12

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interaction with PDZK1. Lesinurad,Ruzinurad and dotinurad are urate transporter inhibitors that have been approved to treat gout. Lesinurad enhances urate excretion...

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