Febuxostat: A selective xanthine oxidase inhibitor for the treatment of hyperuricemia and gout

Annals of Pharmacotherapy

Volumn 40, Issue 12, 2006, Pages 2187-2194

  Bruce, Susan P ^a  

^a Center for Rheumatology LLP   (United States)

Author keywords

Febuxostat; Gout; Hyperuricemia; Xanthine oxidase inhibitor

Indexed keywords

ALLOPURINOL; ANTACID AGENT; COLCHICINE; CYTOCHROME P450; CYTOCHROME P450 2D6; FEBUXOSTAT; GUANINE DEAMINASE; HYDROCHLOROTHIAZIDE; HYPOXANTHINE; HYPOXANTHINE PHOSPHORIBOSYLTRANSFERASE; INDOMETACIN; NAPROXEN; NONSTEROID ANTIINFLAMMATORY AGENT; OROTATE PHOSPHORIBOSYLTRANSFERASE; OROTIDINE 5' PHOSPHATE DECARBOXYLASE; PLACEBO; PURINE; PURINE NUCLEOSIDE PHOSPHORYLASE; PYRIMIDINE; URATE; URATE OXIDASE; URIC ACID; XANTHINE; XANTHINE OXIDASE; XANTHINE OXIDASE INHIBITOR;

ABDOMINAL PAIN; ARTHRALGIA; CAPILLARY RESISTANCE; CLINICAL TRIAL; COCHRANE LIBRARY; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIARRHEA; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; DRUG WITHDRAWAL; GASTROINTESTINAL SYMPTOM; GOUT; HEADACHE; HUMAN; HYPERURICEMIA; JOINT SWELLING; KIDNEY FAILURE; LIVER FUNCTION TEST; MACULOPAPULAR RASH; MEDICAL LITERATURE; MEDLINE; MUSCULOSKELETAL DISEASE; MYALGIA; NAUSEA; NONHUMAN; PRIORITY JOURNAL; RASH; REVIEW; SCISEARCH; SIDE EFFECT; TREATMENT DURATION; TREATMENT OUTCOME; URIC ACID BLOOD LEVEL; URTICARIA; VOMITING;

GOUT; HUMANS; HYPERURICEMIA; THIAZOLES; XANTHINE OXIDASE;

EID: 33845654435     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1345/aph.1H121     Document Type: Review

References (36)

1. Choi HK, Mount DB, Reginato AM. Pathogenesis of gout. Ann Intern Med 2005;143:499-516.
2. Terkeltaub RA. Clinical practice. Gout. N Engl J Med 2003;349:1647-55.
3. Gutierrez-Macias A, Lizarralde-Palacios E, Martinez-Odriozola P, Miguel-De la Villa F. Fatal allopurinol hypersensitivity syndrome after treatment of asymptomatic hyperuricaemia. BMJ 2005;331:623-4.
4. Arellano F, Sacristan JA. Allopurinol hypersensitivity syndrome: a review. Ann Pharmacother 1993;27:337-43.
5. Vazquez-Mellado J, Morales EM, Pacheco-Tena C, Burgos-Vargas R. Relation between adverse events associated with allopurinol and renal function in patients with gout. Ann Rheum Dis 2001;60:981-3.
6. Raebel MA, McClure DL, Simon SR, et al. Frequency of serum creatinine monitoring during allopurinol therapy in ambulatory patients. Ann Pharmacother 2006;40:386-91. Epub 14 Feb 2006. DOI 10.1345/aph.1G589
7. Takano Y, Hase-Aoki K, Horiuchi H, et al. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci 2005;76:1835-47.
8. Zhao L, Takano Y, Horiuchi H. Effect of febuxostat, a novel non-purine, selective inhibitor of xanthine oxidase (NP-SIXO), on enzymes in purine and pyrimidine metabolism pathway (abstract). Arthritis Rheum 2003; 48(suppl):S531.
9. Mayer MD, Khosravan R, Vernillet L, Wu JT, Joseph-Ridge N, Mulford DJ. Pharmacokinetics and pharmacodynamics of febuxostat, a new non-purine selective inhibitor of xanthine oxidase in subjects with renal impairment. Am J Ther 2005;12:22-34
10. Becker MA, Kisicki J, Khosravan R, et al. Febuxostat (TMX-67), a novel, non-purine, selective inhibitor of xanthine oxidase, is safe and decreases serum urate in healthy volunteers. Nucleosides Nucleotides Nucleic Acids 2004;23:1111-6.
11. Murrell GA, Rapeport WG. Clinical pharmacokinetics of allopurinol. Clin Pharmacokinet 1986;11:343-53.
12. Schumacher HR Jr. Febuxostat: a non-purine, selective inhibitor of xanthine oxidase for the management of hyperuricaemia in patients with gout. Expert Opin Investig Drugs 2005;14:893-903.
13. Hoshide S, Takahashi Y, Ishikawa T, et al. PK/PD and safety of a single dose of TMX-67 (febuxostat) in subjects with mild and moderate renal impairment. Nucleosides Nucleotides Nucleic Acids 2004;23:1117-8.
14. Swan S, Khosravan R, Mayer MD, et al. Effect of renal impairment on pharmacokinetics, pharmacodynamics, and safety of febuxostat (TMX-67), a novel non-purine selective inhibitor of xanthine oxidase (abstract). Arthritis Rheum 2003;48(suppl):S529.
15. Khosravan R, Grabowski BA, Mayer MD, Wu JT, Joseph-Ridge N, Vernillet L. The effect of mild and moderate hepatic impairment on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel non-purine selective inhibitor of xanthine oxidase. J Clin Pharmacol 2006; 46:88-102.
16. Komoriya K, Osada Y, Hasegawa M, et al. Hypouricemic effect of allopurinol and the novel xanthine oxidase inhibitor TEI-6720 in chimpanzees. Eur J Pharmacol 1993;250:455-60.
17. Horiuchi H, Ota M, Kobayashi M, et al. A comparative study on the hypouricemic activity and potency in renal xanthine calculus formation of two xanthine oxidase/xanthine dehydrogenase inhibitors: TEI-6720 and allopurinol in rats. Res Commun Mol Pathol Pharmacol 1999;104:307-19.
18. Osada Y, Tsuchimoto M, Fukushima H, et al. Hypouricemic effect of the novel xanthine oxidase inhibitor, TEI-6720, in rodents. Eur J Pharmacol 1993;241:183-8.
19. Horiuchi H, Ota M, Kaneko H, Kasahara Y, Ohta T, Komoriya K. Nephrotoxic effects of allopurinol in dinitrofluorobenzene-sensitized mice: comparative studies on TEI-6720. Res Commun Mol Pathol Pharmacol 1999;104:293-305.
20. Yamamoto T, Moriwaki Y, Fujimura Y, et al. Effect of TEI-6720, a xanthine oxidase inhibitor, on the nucleoside transport in the lung cancer cell line A549. Pharmacology 2000;60:34-40.
21. Okamoto K, Eger BT, Nishino T, Kondo S, Pai EF. An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition. J Biol Chem 2003;278: 1848-55.
22. Kamatani N, Fujimori S, Hada T, et al. Phase II dose-response clinical trial using febuxostat (TMX-67), a novel-type xanthine oxidase/xanthine dehydrogenase inhibitor, for gout and hyperuricemia (abstract). Arthritis Rheum 2003;48(suppl):S530.
23. Schumacher HR Jr, Wortmann RL, Becker MA, et al. A phase 2, long term open-label safety and efficacy study of febuxostat, a novel non-purine, selective inhibitor of xanthine oxidase (abstract). Arthritis Rheum 2004;50(suppl):S335-6.
24. Wortmann RL, Becker MA, Schumacher HR Jr, MacDonald P, Palo WA, Joseph-Ridge N. Gout flare prophylaxis during management of chronic gout with febuxostat, a non-purine selective inhibitor of xanthine oxidase (abstract). Arthritis Rheum 2004;50(suppl):S335.
25. Joseph-Ridge N. Phase II, dose-response, safety and efficacy clinical trial of a new xanthine oxidase inhibitor TMX-67 (febuxostat) in subjects with gout (abstract). Arthritis Rheum 2003;46(suppl):S142.
26. Becker MA, Schumacher HR Jr, Wortmann RL, et al. Febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase: a twenty-eight-day, multicenter, phase II, randomized, double-blind, placebo-controlled, dose-response clinical trial examining safety and efficacy in patients with gout. Arthritis Rheum 2005;52:916-23.
27. Schumacher HR Jr, Becker MA, Wortmann RL, et al. Febuxostat vs allopurinol and placebo in subjects with hyperuricemia and gout: the 28-week APEX study (abstract). Arthritis Rheum 2005;52(suppl):S680.
28. Becker MA, Schumacher HR Jr, Wortmann RL, et al. Febuxostat compared with allopurinol in patients with hyperuricemia and gout. N Engl J Med 2005;353:2450-61.
29. Becker MA, Schumacher HR Jr, Wortmann RL, MacDonald P, Palo WA, Joseph-Ridge N. Febuxostat, a novel non-purine selective inhibitor of xanthine oxidase, therapy in allopurinol intolerant patients (abstract). Arthritis Rheum 2004;50(suppl):S336.
30. Khosravan R, Erdman K, Vernillet L, et al. Effect of febuxostat on pharmacokinetics of desipramine, a CYP2D6 substrate in healthy subjects (abstract). Clin Pharmacol Ther 2005;77(suppl):P43.
31. Khosravan R, Grabowski BA, Wu J, Joseph-Ridge N, Vernillet L. Effect of food or antacid on febuxostat pharmacokinetics and pharmacodynamics in healthy subjects (abstract). Clin Pharmacol Ther 2005;77(suppl):P50.
32. Grabowski BA, Khosravan R, Wu J, Lademacher C, Vernillet L. Effect of hydrochlorothiazide on pharmacokinetics and pharmacodynamics of febuxostat (abstract). Arthritis Rheum 2005;52(suppl):S103-4.
33. Khosravan R, Mayer MD, Wu J, Joseph-Ridge N, Vernillet L. Effect of concomitant administration of febuxostat and colchicine on pharmacokinetics of febuxostat and colchicine at steady state (abstract). Arthritis Rheum 2005;52(suppl):S102-3.
34. Khosravan R, Wu JT, Joseph-Ridge N, Vernillet L. Pharmacokinetic interactions of concomitant administration of febuxostat and NSAIDs. J Clin Pharmacol 2006;46:855-66.
35. Schumacher HR Jr, Becker M, Wortmann RL, et al. Magnetic resonance imaging of gouty tophi during treatment with febuxostat, a non-purine selective inhibitor of xanthine oxidase (abstract). Arthritis Rheum 2004; 50(suppl):S336.
36. Khosravan R, Kukulka M, Wu J, Joseph-Ridge N, Vernillet L. Effects of age and gender on febuxostat pharmacokinetics, pharmacodynamics, and safety in healthy subjects (abstract). Clin Pharmacol Ther 2005;77(suppl): P50.