Description

Simple

A medication used for the treatment of high levels of a chemical called uric acid in people who suffer from gout, a painful condition affecting body tissues and joints because of uric acid buildup.

Clinical

A xanthine oxidase inhibitor used for the management of chronic hyperuricemia in patients with gout.

Overview

Febuxostat is a xanathine oxidase (XO) inhibitor indicated in patients with gout suffering from hyperuricemia and is used in its chronic management. Febuxostat is not recommended for the treatment of asymptomatic hyperuricemia. Febuxostat is marketed under the trade name Uloric by Takeda Pharmaceuticals America, Inc., and was approved by the FDA in February 2009.

Pharmacology

Indication

For the treatment of hyperuricemia in patients with gout.

Pharmacodynamic

Febuxostat (ULORIC) is a novel, xanthine oxidase/dehydrogenase (XO/XDH) inhibitor being developed by Teijin, TAP Pharmaceuticals, and Ipsen for the treatment of gout. The currently available XO inhibitor, allopurinol, has been associated with serious instances of severe hypersensitivity, in some cas... Read more

Mechanism of action

Febuxostat, a xanthine oxidase inhibitor, achieves its therapeutic effect by decreasing serum uric acid. Febuxostat is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations.

Absorption

>49%

Protein binding

99.2%

Volume of distribution

The mean apparent steady state volume of distribution (Vss/F) of febuxostat was approximately 50 L (CV ~40%)

Clearance

Information currently not available.

Half life

~5-8 hours.

Route of elimination

Febuxostat is eliminated primarily through both hepatic and renal pathways.

Toxicity

The FDA adverse event reporting system database, AERS, indicated potential signals of febuxostat-associated cardiovascular thromboembolic events. AERS is not capable of establishing the causal link and detecting the true frequency of an adverse event associated with a drug. The positive IC value fou... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Liver function abnormalities US
  • Kind: experimental
    • Percent: 4.6-6.6%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 4.2%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 0.5-1.6%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 1.6%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1.1-1.3%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 0.8%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 0.7-1.1%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 0.7%
  • Clinical Trial
    Hot flush US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Skin odor abnormal US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Flushing US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Skin altered pigmentation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Skin Discoloration US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Skin Lesion US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Purpura US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Triglycerides increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Amylase increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Potassium increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Glucose increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Cholesterol increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Bicarbonate decreased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Sodium increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    EEG abnormal US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Activated partial thromboplastin time prolonged US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Creatine increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Alopecia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Upper Respiratory Tract Infection US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Throat irritation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Sneezing US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Respiratory tract congestion US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pharyngeal edema US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Paranasal sinus hypersecretion US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Nasal dryness US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Petechiae US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Photosensitivity US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Peeling skin US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hair color changes US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hair growth abnormal US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Eczema US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Ecchymosis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dermatitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dermographism US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Angio edema US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urine positive for protein US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urine positive for white blood cells US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Blood urea increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • With Drugs Coadmin:
        • Name: Azathioprine
        • Drugbank Id: DB00993
    • Regions: US
    • With Drugs Coadmin:
        • Name: Mercaptopurine
        • Drugbank Id: DB01033

    Food Interactions

    Take with or without food.