pharmacopeia
GET
/api/v1/drug/febuxostat

Boxed warning

CARDIOVASCULAR DEATH Gout patients with established cardiovascular (CV) disease treated with febuxostat tablets had a higher rate of CV death compared to those treated with allopurinol in a CV outcomes study [see Warnings and Precautions (5.1) ] . Consider the risks and benefits of febuxostat tablets when deciding to prescribe or continue patients on febuxostat tablets. Febuxostat tablets should only be used in patients who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable [see Indications and Usage (1) ] . WARNING: CARDIOVASCULAR DEATH See full prescribing information for complete boxed warning. Gout patients with established cardiovascular (CV) disease treated with febuxostat had a higher rate of CV death compared to those treated with allopurinol in a CV outcomes study. ( 5.1 ) Consider the risks and benefits of febuxostat when deciding to prescribe or continue patients on febuxostat . Febuxostat should only be used in patients who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable. ( 1 )

2D structure
2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
SMILES CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O
InChIKey BQSJTQLCZDPROO-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

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.

Xanthine Oxidase

Indications

Sourced from openFDA
  • Febuxostat is a xanthine oxidase (XO) inhibitor indicated for the chronic management of hyperuricemia in adult patients with gout who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable. Limitations of Use : Febuxostat tablets are not recommended for the treatment of asymptomatic hyperuricemia.ICD-10: M10.9

Contraindications

Sourced from openFDA
  • Febuxostat tablets are contraindicated in patients being treated with azathioprine or mercaptopurine [see Drug Interactions (7) ] . Febuxostat tablets are contraindicated in patients being treated with azathioprine or mercaptopurine.contraindicated

Dosage & administration

Sourced from openFDA

Recommended dosage is 40 mg or 80 mg once daily. The recommended starting dosage is 40 mg once daily. For patients who do not achieve a serum uric acid (sUA) less than 6 mg/dL after 2 weeks, the recommended dosage is 80 mg once daily. ( 2.1 ) Patients with severe renal impairment: Limit the dosage to 40 mg once daily. ( 2.2 , 8.6 ) Flare prophylaxis is recommended upon initiation of febuxostat tablets. ( 2.4 ) Can be administered without regard to food or antacid use. ( 2.1 ) 2.1 Recommended Dosage The recommended febuxostat tablets dosage is 40 mg or 80 mg once daily. The recommended starting dosage of febuxostat tablets is 40 mg once daily. For patients who do not achieve a serum uric acid (sUA) less than 6 mg/dL after two weeks, the recommended febuxostat tablets dosage is 80 mg once daily. Febuxostat tablets can be taken without regard to food or antacid use [see Clinical Pharmacology (12.3) ]. Concurrent prophylactic treatment with a non-steroidal anti-inflammatory drug (NSAID) or colchicine is recommended [see Dosage and Administration (2.4) and Warnings and Precautions (5.2) ]. 2.2 Dosage Recommendations in Patients with Renal Impairment and Hepatic Impairment The recommended dosage of febuxostat tablets is limited to 40 mg once daily in patients with severe renal impairment. No dose modification is necessary when administering febuxostat tablets in patients with mild or moderate renal impairment [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3) ] .

Warnings & precautions

Sourced from openFDA

Gout Flares : An increase in gout flares is frequently observed after initiation of febuxostat. If a gout flare occurs during treatment, febuxostat need not be discontinued. Prophylactic therapy (i.e., non-steroidal anti-inflammatory drug or colchicine) upon initiation of treatment may be beneficial for up to six months. ( 2.4 , 5.2 ) Hepatic Effects : Cases of hepatic failure, some fatal, have been reported. If liver injury is detected, promptly interrupt febuxostat and treat cause, if possible, to resolution or stabilization. Permanently discontinue febuxostat if liver injury is confirmed, and no alternate etiology can be found. ( 5.3 ) Serious Skin Reactions : Serious skin and hypersensitivity reactions, including Stevens-Johnson syndrome, drug reaction with eosinophilia and systemic symptoms and toxic epidermal necrolysis have been reported in patients taking febuxostat. Discontinue febuxostat if serious skin reactions are suspected. ( 5.4 ) 5.1 Cardiovascular Death In a cardiovascular (CV) outcome study, gout patients with established CV disease treated with febuxostat had a higher rate of CV death compared to those treated with allopurinol. Sudden cardiac death was the most common cause of adjudicated CV deaths, 2.7% in the febuxostat group (83 of 3,098) as compared to 1.8% in the allopurinol group (56 of 3,092). Febuxostat was similar to allopurinol for nonfatal myocardial infarction (MI), nonfatal stroke and unstable angina with urgent coronary revascularization [see Clinical Studies (14.2) ] .

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described elsewhere in the prescribing information: Cardiovascular Death [see Warnings and Precautions (5.1) ] Hepatic Effects [see Warnings and Precautions (5.3) ] Serious Skin Reactions [see Warnings and Precautions (5.4) ] Adverse reactions in ≥ 1% of patients treated with febuxostat are liver function abnormalities, nausea, arthralgia, and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In Phase 2 and 3 clinical studies, a total of 2757 patients with hyperuricemia and gout were treated with febuxostat 40 mg or 80 mg daily. For febuxostat 40 mg, 559 patients were treated for ≥6 months. For febuxostat 80 mg, 1377 patients were treated for ≥6 months, 674 patients were treated for ≥1 year and 515 patients were treated for ≥2 years. In the CARES study, a total of 3098 patients were treated with febuxostat 40 mg or 80 mg daily; of these, 2155 patients were treated for ≥1 year and 1539 were treated for ≥2 years [see Clinical Studies (14.2) ] .

Use in specific populations

Sourced from openFDA

Patients with severe hepatic impairment: No studies have been conducted in this patient population. Caution should be exercised in these patients. ( 8.7 ) Patients with secondary hyperuricemia (including patients being treated for Lesch-Nyhan syndrome or malignant disease, or in organ transplant recipients): Febuxostat is not recommended for use as no studies have been conducted in this patient population. ( 8.8 ) 8.1 Pregnancy Risk Summary Limited available data with febuxostat use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes. No adverse developmental effects were observed in embryo-fetal development studies with oral administration of febuxostat to pregnant rats and rabbits during organogenesis at doses that produced maternal exposures up to 40 and 51 times, respectively, the exposure at the maximum recommended human dose (MRHD). No adverse developmental effects were observed in a pre- and postnatal development study with administration of febuxostat to pregnant rats from organogenesis through lactation at an exposure approximately 11 times the MRHD (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

Pharmacokinetics

Sourced from openFDA
Metabolism
In healthy patients, maximum plasma concentrations (C max ) and AUC of febuxostat increased in a dose proportional manner following single and multiple doses of 10 mg (0.25 times the lowest recommended dosage) to 120 mg (1.5 times the maximum recommended dosage). There is no accumulation when therapeutic doses are administered every 24 hours.

Overdosage

Sourced from openFDA

Febuxostat was studied in healthy patients in doses up to 300 mg daily for seven days without evidence of dose-limiting toxicities. No overdose of febuxostat was reported in clinical studies. Patients should be managed by symptomatic and supportive care should there be an overdose.

Approval history

Sourced from openFDA
  • Feb 13, 2009NDANDA021856Takeda Pharms Usa
  • Jul 1, 2019ANDAANDA205421Alembic
  • Jul 1, 2019ANDAANDA205467Sun Pharm
  • Oct 15, 2019ANDAANDA205414Hikma
  • Dec 30, 2019ANDAANDA210292Regcon Holdings
  • Dec 30, 2019ANDAANDA210461Msn
  • Jun 2, 2020ANDAANDA213069Sunshine
  • Oct 22, 2020ANDAANDA205374Dr Reddys

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
16,339 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Diarrhoea8635.3%
  2. 2Nausea8475.2%
  3. 3Acute Kidney Injury8455.2%
  4. 4Rash7944.9%
  5. 5Off Label Use7384.5%
  6. 6Gout6924.2%
  7. 7Drug Ineffective6834.2%
  8. 8Dyspnoea6343.9%
  9. 9Fatigue6133.8%
  10. 10Anaemia5843.6%
  11. 11Headache5823.6%
  12. 12Pneumonia5453.3%
  13. 13Pyrexia5383.3%
  14. 14Death5223.2%
  15. 15Renal Impairment5063.1%

Literature

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Recent PubMed references pinned to Febuxostat as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 113 ClinicalTrials.gov registrations naming Febuxostat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Febuxostat work?
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.
What is Febuxostat used for?
According to FDA labeling, Febuxostat carries indications including: Febuxostat is a xanthine oxidase (XO) inhibitor indicated for the chronic management of hyperuricemia in adult patients with gout who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable. Limitations of Use : Febuxostat tablets are not recommended for the treatment of asymptomatic hyperuricemia.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Febuxostat?
Febuxostat is classified as Preparations inhibiting uric acid production, Xanthine Oxidase Inhibitor, Xanthine Oxidase Inhibitors, Decreased Uric Acid Synthesis.
What are the brand names for Febuxostat?
Febuxostat is marketed under brand names including Uloric.
What are the contraindications for Febuxostat?
Febuxostat labeling lists contraindications including: Febuxostat tablets are contraindicated in patients being treated with azathioprine or mercaptopurine [see Drug Interactions (7) ] . Febuxostat tablets are contraindicated in patients being treated with azathioprine or mercaptopurine.. Always consult the full prescribing information and a clinician.
Note. Data for febuxostat is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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