2-(3-Cyano-4-(2-methylpropoxy)phenyl)-4-methylthiazole-5-carboxylic acid/Febuxostat/2-(3-Cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic Acid,This product is unavailable/2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid/5-Thiazolecarboxylic acid, 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-/Uloric/5-Thiazolecarboxylic acid, 2-(3-cyano-4-(2-methylpropoxy)phenyl)-4-methyl-/Tei-6720/Adenuric/Febuxostat,This product is unavailable/2-(3-Cyano-4-isobutoxyphenyl)-4-methyl-1,3-thiazole-5-carboxylic acid/TMX 67/2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid
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Cardiovascular risk is increased in patients with gout. We compared cardiovascular outcomes associated with febuxostat, a nonpurine xanthine oxidase inhibitor, with those associated with allopurinol, a purine base analogue xanthine oxidase inhibitor, in patients with gout and cardiovascular disease.
We conducted a multicenter, double-blind, noninferiority trial involving patients with gout and cardiovascular disease; patients were randomly assigned to receive febuxostat or allopurinol and were stratified according to kidney function. The trial had a prespecified noninferiority margin of 1.3 for the hazard ratio for the primary end point (a composite of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or unstable angina with urgent revascularization).
In total, 6190 patients underwent randomization, received febuxostat or allopurinol, and were followed for a median of 32 months (maximum, 85 months). The trial regimen was discontinued in 56.6% of patients, and 45.0% discontinued follow-up. In the modified intention-to-treat analysis, a primary end-point event occurred in 335 patients (10.8%) in the febuxostat group and in 321 patients (10.4%) in the allopurinol group (hazard ratio, 1.03; upper limit of the one-sided 98.5% confidence interval [CI], 1.23; P=0.002 for noninferiority). All-cause and cardiovascular mortality were higher in the febuxostat group than in the allopurinol group (hazard ratio for death from any cause, 1.22 [95% CI, 1.01 to 1.47]; hazard ratio for cardiovascular death, 1.34 [95% CI, 1.03 to 1.73]). The results with regard to the primary end point and all-cause and cardiovascular mortality in the analysis of events that occurred while patients were being treated were similar to the results in the modified intention-to-treat analysis.
In patients with gout and major cardiovascular coexisting conditions, febuxostat was noninferior to allopurinol with respect to rates of adverse cardiovascular events. All-cause mortality and cardiovascular mortality were higher with febuxostat than with allopurinol. (Funded by Takeda Development Center Americas; CARES ClinicalTrials.gov number, NCT01101035 .).
Cardiovascular Safety of Febuxostat or Allopurinol in Patients with Gout.
White WB, Saag KG, Becker MA, Borer JS, Gorelick PB, Whelton A, Hunt B, Castillo M, Gunawardhana L; CARES Investigators.
2018 Mar 29
Febuxostat is a potent non-purine selective xanthine oxidase inhibitor approved by the FDA in 2009 for management of hyperuricemia in people with gout. Areas covered: The authors summarize the pre-clinical studies and pivotal randomized controlled trials of febuxostat when used as a treatment for hyperuricaemia in gout Expert opinion: Febuxostat has clinical efficacy in serum urate lowering, and long-term use leads to improved outcomes such as gout flare frequency and tophus burden. Recently published post-approval placebo-controlled trials have demonstrated urate-lowering efficacy and safety of febuxostat in patients with chronic kidney disease, and reduced frequency of gout flares in people with early onset of gout. In November 2017, the FDA issued a drug safety communication based on the preliminary results of the CARES trial. This cardiovascular safety study of 6190 patients with gout and established cardiovascular disease comparing febuxostat and allopurinol showed no difference in the primary endpoint (a composite of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or unstable angina with urgent revascularization), but did report higher all-cause mortality (hazard ratio 1.22) and cardiovascular mortality (hazard ratio 1.34) with febuxostat. Based on currently available data, it seems likely that allopurinol, rather than febuxostat, will remain first line urate-lowering therapy for people with gout.
Febuxostat; cardiovascular; gout; urate
Febuxostat for the treatment of hyperuricaemia in gout.
Robinson PC1,2, Dalbeth N3,4.
PURPOSE OF REVIEW:
Concerns about the cardiovascular safety of febuxostat lead to reconsideration of the place of febuxostat in the management of gout.
The CARES trial is a randomized controlled trial mandated by the FDA to compare the cardiovascular safety of febuxostat and allopurinol in the management of gout. About 6190 patients with gout and major cardiovascular disease, randomly assigned to allopurinol or febuxostat, were prospectively followed up for a median of 32 months. No difference was noted in the occurrence of the primary end-point event, a composite of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or unstable angina with urgent revascularization, but cardiovascular death was significantly more common in the febuxostat group (4.3%) as compared with the allopurinol group (3.2%) (P = 0.03).
Present guidelines on the management of gout should be revised in view of recent findings. Allopurinol could be recommended as the sole first-line urate-lowering drug (ULD) in patients with no contraindication. In patients contraindicated to allopurinol, uricosurics could be preferred to febuxostat as first-line ULDs in patients with cardiovascular disease/risk factors and no history of uric acid stones.
The role of febuxostat in gout.
Bardin T1,2,3, Richette P1,2,3.