Febuxostat

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Febuxostat
File:Febuxostat Structural Formulae V.1.svg
Systematic (IUPAC) name
2-(3-cyano-4-isobutoxyphenyl)-4-methyl-
1,3-thiazole-5-carboxylic acid
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
Pregnancy
category
  • C
Routes of
administration		 oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability ~49% absorbed
Protein binding ~99% to albumin
Metabolism via CYP1A2, 2C8, 2C9, UGT1A1, 1A3, 1A9, 2B7
Biological half-life ~5-8 hours
Excretion urine (~49% mostly as metabolites, 3% as unchanged drug); feces (~45% mostly as metabolites, 12% as unchanged drug)
Identifiers
CAS Number 144060-53-7
ATC code M04AA03 (WHO)
PubChem CID 134018
Chemical data
Formula C16H16N2O3S
Molar mass 316.374 g/mol[[Script error: No such module "String".]]
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Febuxostat (INN; brand names Adenuric (EU) and Uloric (US)) is an inhibitor of xanthine oxidase that is indicated for use in the treatment of hyperuricemia and gout.[1]. The drug is marketed by Menarini.

Febuxostat received marketing approval by the European Medicines Agency on April 21, 2008[2] and was approved by the U.S. Food and Drug Administration on February 16, 2009.[3]

A study comparing febuxostat to allopurinol found that more individuals treated with febuxostat had decreased levels of uric acid, but there was no difference in the amount of initial gout flares or the surface area of gout tophi.[4]

A committee of the British National Institute for Health and Clinical Excellence concluded that although febuxostat had been shown to be more effective than fixed-dose (300mg) allopurinol in lowering serum uric acid concentration, it had not been shown to be clinically or cost effective compared with the more appropriate comparator of allopurinol increased as required to control uric acid levels (up to 900mg). However, it recommended febuxostat for people who are intolerant of allopurinol.[5]

Mechanism of action

Febuxostat is a non-purine selective inhibitor of xanthine oxidase. It works by non-competitively blocking the channel leading to the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Hence, febuxostat inhibits xanthine oxidase, therefore reducing production of uric acid.

Side-effects

The adverse effects associated with febuxostat therapy include nausea, diarrhea, arthralgia, headache, increased hepatic serum enzyme levels and rash.[6][7]

References

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Antigout preparations (M04)
Uricosurics
Xanthine oxidase inhibitors
Mitotic inhibitors
Other

M: JNT

anat(h/c, u, t, l)/phys

proc, drug(M4)


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fr:Febuxostat ja:フェブキソスタット

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  1. ↑ Stamp LK, O'Donnell JL, Chapman PT (2007). "Emerging therapies in the long-term management of hyperuricaemia and gout". Internal medicine journal. 37 (4): 258–66. doi:10.1111/j.1445-5994.2007.01315.x. PMID 17388867. 
  2. ↑ "Adenuric (febuxostat) receives marketing authorisation in the European Union" (PDF). Retrieved 2008-05-28. 
  3. ↑ "Uloric Approved for Gout". U.S. News and World Report. Retrieved 2009-02-16. 
  4. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. ↑ Febuxostat for the management of hyperuricaemia in people with gout (TA164) Chapter 4. Consideration of the evidence
  6. ↑ ULORIC package insert, Takeda Pharmaceuticals America, Deerfield, IL, February, 2009.
  7. ↑ Love BL, Barrons R, Veverka A, Snider KM. Urate-lowering therapy for gout: focus on febuxostat. Pharmacotherapy 30: 594-608, 2010.
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