Febuxostat, a novel drug for the treatment of hyperuricemia of gout

Future Rheumatology

Volumn 3, Issue 5, 2008, Pages 421-427

  Perez Ruiz, Fernando ^a   Dalbeth, Nicola ^b   Schlesinger, Naomi ^c  

^a HOSPITAL DE CRUCES   (Spain)

^b UNIVERSITY OF AUCKLAND   (New Zealand)

^c ROBERT WOOD JOHNSON MEDICAL SCHOOL   (United States)

Author keywords

Febuxostat; Gout; Urate lowering agents

Indexed keywords

ACETYLSALICYLIC ACID; ALLOPURINOL; ANTACID AGENT; AZATHIOPRINE; BENZBROMARONE; FEBUXOSTAT; FENOFIBRATE; HYDROCHLOROTHIAZIDE; IBUPROFEN; INDOMETACIN; MERCAPTOPURINE; NAPROXEN; PLACEBO; PROBENECID; URATE; WARFARIN; XANTHINE OXIDASE;

ARTICLE; CLINICAL TRIAL; DESENSITIZATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG EXCRETION; DRUG GLUCURONIDATION; DRUG INHIBITION; DRUG MECHANISM; DRUG MEGADOSE; DRUG METABOLISM; DRUG SAFETY; DRUG SUBSTITUTION; DRUG WITHDRAWAL; FOOD; FOOD DRUG INTERACTION; GOUT; HEART DISEASE; HUMAN; HYPERURICEMIA; KIDNEY FUNCTION; LIVER FUNCTION; LIVER FUNCTION TEST; LOW DRUG DOSE; NONHUMAN; OXIDATION; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; SIDE EFFECT; SKIN MANIFESTATION; TIME TO MAXIMUM PLASMA CONCENTRATION; URIC ACID BLOOD LEVEL;

EID: 67649721893     PISSN: 17460816     EISSN: None     Source Type: Journal    
DOI: 10.2217/17460816.3.5.421     Document Type: Article

References (61)

1. Mikuls TR, Saag KG: New insights into gout epidemiology. Curr. Opin. Rheumatol. 18, 199-203 (2006).
2. Yü TF, Gutman AB: Principles of current management of primary gout. Am. J. Med. Sci. 254, 893-907 (1967)
3. McCarthy G, Barthelemy CR, Veum JA, Wortmann RL: Influence of antihyperuricemic therapy on the clinical and radiographic progression of gout. Arthritis Rheum. 34(12), 1489-1494 (1991).
4. Yü TF: Milestones in the treatment of gout. Am. J. Med. 56, 676-685 (1974).
5. Zhang W, Doherty M, Bardin T et al.: EULAR evidence based recommendations for gout Part II. Management. Report of a Task Force of the EULAR Standing Committee for international clinical studies including therapeutics (ESCISIT). Ann. Rheum. Dis. 65, 1312-1324 (2006).
6. Perez-Ruiz F, Lioté F: Lowering serum uric acid levels: what is the optimal target for improving clinical outcomes in gout? Arthritis Rheum. 57(7), 1324-1328 (2007).
7. Sarawate AC, Patel PA, Schumacher HR, Yang W, Brewer KK, Baskt AW: Serum urate levels and gout flares. Analysis from managed care data. J. Clin. Rheumatol. 12, 61-65 (2006).
8. Riedel AA, Nelson M, Joseph-Ridge N, Wallace K, MacDonald PA, Becker M: Compliance with allopurinol therapy among managed care enrollees with gout: a retrospective analysis of administrative claims. J. Rheumatol. 31, 1575-1581 (2006).
9. Rundles RW, Metz EN, Silberman HR: Allopurinol in the treatment of gout. Ann. Intern. Med. 64(2), 229-258 (1966).
10. Gutman AB: Uricosuric drugs, with special reference to probenecid and sulfinpyazone. Adv. Pharmacol. 4, 91-142 (1966).
11. Sorensen LB, Levinson DJ: Clinical evaluation of benzbromarone. Arthritis Rheum. 19, 183-190 (1976).
12. Sherman MR, Saifer MGP, Perez-Ruiz F: PEG-uricase in the management of treatment-resistant gout and hyperuricemia. Adv. Drug Deliv. Rev. 60(1), 59-68 (2008).
13. Fukunari A, Okamoto K, Nishino T et al.: Y-700 [1-[3-Cyano-4-(2,2-dimethylpropoxy) phenyl]-1H-pyrazole-4-carboxylic acid]: a potent xanthine oxidoreductase inhibitor with hepatic excretion. J. Pharmacol. Exp. Ther. 311(2), 519-528 (2004).
14. Yeh L, Hingorani V, Manhard K et al.: Safety and uric acid lowering effect in humenas following multiple doses of RDEA806, a novel prodrug for the potential treatment of hyperuricemia. Ann. Rheum. Dis. 67(Suppl. II), 248-248 (2008).
15. Yeh L, Tamai I, Hamatake R et al.: Mode of action of RDEA594 as uric acid lowering agent in humans following multiple doses of its prodrug, RDEA806. Ann. Rheum. Dis. 67(Suppl. II), 247-247 (2008).
16. Takano Y, Hase-Aoki K, Horiuchi H et al.: Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci. 76(16), 1835-1847 (2005).
17. Okamoto K, Eger BT, Nishino T, Kondo S, Pai EF, Nishino T: An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition. J. Biol. Chem. 278(3), 1848-1855 (2003).
18. Osada Y, Tsuchimoto M, Fukushima H et al.: Hypouricemic effect of the novel xanthine oxidase inhibitor, TEI-6720, in rodents. Eur. J. Pharmacol. 241(2-3), 183-188 (1993).
19. 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. 250(3), 455-460 (1993).
20. Khosravan R, Grabowski B, Wu JT, Joseph-Ridge N, Vernillet L: Effect of food or antacid on pharmacokinetics and pharmacodynamics of febuxostat in healthy subjects. Br. J. Clin. Pharmacol. 65(3), 355-363 (2008).
21. Khosravan R, Grabowski BA, Wu JT, Joseph-Ridge N, Vernillet L: Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects. Clin. Pharmacokinet. 45(8), 821-841 (2006).
22. Khosravan R, Grabowski BA, Wu JT, Joseph-Ridge N, Vernillet L: Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects. Clin. Pharmacokinet. 45(8), 821-841 (2006).
23. Khosravan R, Grabowski B, Wu JT, Joseph-Ridge N, Vernillet L: Effect of food or antacid on pharmacokinetics and pharmacodynamics of febuxostat in healthy subjects. Br. J. Clin. Pharmacol. 65(3), 355-363 (2008).
24. Komoriya K, Hoshide S, Takeda K et al.: Pharmacokinetics and pharmacodynamics of febuxostat (TMX-67), a non-purine selective inhibitor of xanthine oxidase/xanthine dehydrogenase (NPSIXO) in patients with gout and/or hyperuricemia. Nucleosides Nucleotides Nucleic Acids 23(8-9), 1119-1122 (2004).
25. Khosravan R, Wu JT, Joseph-Ridge N, Vernillet L: Pharmacokinetic Interactions of Concomitant Administration of Febuxostat and NSAIDs. J. Clin. Pharmacol. 46(8), 855-866 (2006).
26. Mukoyoshi M, Nishimura S, Hoshide S et al.: In vitro drug-drug interaction studies with febuxostat, a novel non-purine selective inhibitor of xanthine oxidase: plasma protein binding, identification of metabolic enzymes and cytochrome P450 inhibition. Xenobiotica 38(5), 496-510 (2008).
27. Grabowski BA, Khosravan R, Wu JT, Lademacher C, Vernillet L: Effect of hydroclorthiazide on pharmacokinetics and pharmacodynamics of febuxostat. Arthritis Rheum. 52(Suppl.), S103-S104 (2005).
28. 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 23(8-9), 1117-1118 (2004).
29. 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. 12(1), 22-34 (2005).
30. 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 nonpurine selective inhibitor of xanthine oxidase. J. Clin. Pharmacol. 46(1), 88-102 (2006).
31. Cummins D, Sekar M, Halil O, Banner N: Myelosuppression associated with azathioprineallopurinol interaction after heart and lung transplantation. Transplantation 61(11), 1161-1162 (1996).
32. Becker MA, Schumacher HR Jr, Wortmann RL et al.: 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. 52(3), 916-923 (2005).
33. 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 23(8-9), 1111-1116 (2004).
34. Becker MA, Schumacher HR Jr, Wortmann RL et al.: Febuxostat compared with allopurinol in patients with hyperuricemia and gout. N. Engl. J. Med. 353(23), 2450-2461 (2005).
35. Schumacher HR, Becker MA, Wortmann RL et al.: Febuxostat vs. allopurinol and placebo in subjects with hyperuricemia and gout: the 28-week APEX study. Arthritis Rheum. 52(Suppl.), S680-S680 (2005).
36. Schumacher HR, Becker MA, Wortmann RL, Lloyd EJ, MacDonald PA, Joseph-Ridge N: The FOCUS trial 48-month interim analysis: long-term clinical outcomes of treatment with febuxostat in subjects with gout in an ongoing phase 2, open-label extension study. Ann. Rheum. Dis. 65(Suppl. II), 93-93 (2007).
37. Becker MA, Schumacher HR, MacDonald PA, Lloyd EJ, Lademacher C, Joseph-Ridge N: Urate-lowering therapy in subjects with gout: interim results from the febuxostat/allopurinol comparative extension long-term study (EXCEL). Ann. Rheum. Dis. 66 (Suppl. II), 230-230 (2007).
38. Perez-Ruiz F, Calabozo M, Fernandez-Lopez MJ et al.: Treatment of chronic gout in patients with renal function impairment. An open, randomized, actively controlled. J. Clin. Rheumatol. 5, 49-55 (1999).
39. Perez-Ruiz F, Alonso-Ruiz A, Calabozo M, Herrero-Beites A, Garcia-Erauskin G, Ruiz-Lucea E: Efficacy of allopurinol and benzbromarone for the control of hyperuricaemia. A pathogenic approach to the treatment of primary chronic gout. Ann. Rheum. Dis. 57(9), 545-549 (1998).
40. Reinders MK, Haggsma C, Jansen TL et al.: An randomized-controlled trial on the efficacy and tolerability with dose escalation of allopurinol 300-600 mg/day versus benzbromarone 100-200 mg/day in patients with gout. Ann. Rheum. Dis. doi:10.1136/ard.2008.091462 (2008).
41. Reinders MK, van Roon EN, Jansen TL et al.: Efficacy and tolerability of urate lowering drugs in gout: a randomised controlled trial of benzbromarone versus probenecid after failure of allopurinol. Ann. Rheum. Dis. DOI: 10.1136/ard.2007.083071, ard- (2008).
42. Fam AG, Dunne SM, Iazzetta J, Paton TW: Efficacy and safety of desensitization to allopurinol following cutaneous reactions. Arthritis Rheum. 44(1), 231-238 (2001).
43. Grahame R, Simmonds HA, McBride MB, Marsh FP: How should we treat tophaceous gout in patients with allopurinol hypersensitivity? Adv. Exp. Med. Biol. 431, 19-23 (1998).
44. Hepburn AL, Kaye SA, Feher MD: Long-term remission from gout associated with fenofibrate therapy. Clin. Rheumatol. 22, 73-76 (2003).
45. Singer JZ, Wallace SL: The allopurinol hypersensitivity syndrome. Unnecesary morbility and mortality. Arthritis Rheum. 29(1), 82-87 (1986).
46. Zhang W, Doherty M, Bardin T et al.: EULAR evidence based recommendations for gout Part II. Management. Report of a Task Force of the EULAR Standing Committee for international clinical studies including therapeutics (ESCISIT). Ann. Rheum. Dis. 65, 1312-1324 (2006).
47. Vazquez-Mellado J, Meoño Morales E, Pacheco-Tena C, Burgos-Vargas R: Relation between adverse events associated with allopurinol and renal function in patients with gout. Ann. Rheum. Dis. 60, 981-983 (2001).
48. Panomvana D, Sriprdit S, Angthararak S: Higher therapeutic plasma oxypurinol concentrations might be required for gouty patients with chronic kidney disease. J. Clin. Rheumatol. 14, 6-11 (2008).
49. Perez-Ruiz F, Hernando I, Villar I, Nolla JM: Correction of allopurinol dosing should be based on clearance of creatinine, but not plasma creatinine levels. Another insight to allopurinol-related toxicity. J. Clin. Rheumatol. 11, 129-133 (2005).
50. Dalbeth N, Stamp L: Allopurinol dosing in renal impairment: walking the tightrope between adequate urate lowering and adverse events. Semin. Dial. 20(5), 391-395 (2007).
51. Muñiz Caldas CA, Fuller R: Excellent response to the clinical treatment of tophaceous gout. Clin. Rheumatol. 26, 1553-1555 (2007).
52. Goldfarb E, Smythe CJ: Effects of allopurinol, a xanthine-oxidase inhibitor, and sulfinpyrazone upon the urinary and serum urate concentrations in eight patients with tophaceous gout. Arthritis Rheum. 9(3), 414-423 (2007).
53. Perez-Ruiz F, Calabozo M, Pijoan JI, Herrero-Beites AM, Ruibal A: Effect of urate-lowering therapy on the velocity of size reduction of tophi in chronic gout. Arthritis Rheum. 47(4), 356-360 (2002).
54. Perez-Ruiz F, Martin I, Canteli B: Ultrasonographic measurement of tophi as an outcome measure for chronic gout. J. Rheumatol. 34(9), 1888-1893 (2007).
55. Taylor WJ, Schumacher HR Jr, Singh JA, Grainger R, Dalbeth N: Assessment of outcome in clinical trials of gout a review of current measures. Rheumatology 46(12), 1751-1756 (2007).
56. Kanbay M, Ozkara A, Selcoki Y et al.: Effect of treatment of hyperuricemia with allopurinol on blood pressure, creatinine clearence, and proteinuria in patients with normal renal functions. Int. Urol. Nephrol. 39(4), 1227-1233 (2007).
57. George J, Carr E, Davies J, Belch JJF, Struthers A: High-dose allopurinol improves endothelial function by profoundly reducing vascular oxidative stress and not by lowering uric acid. Circulation 114(23), 2508-2516 (2006).
58. Zhao L, Roche BM, Wessale JL et al.: Chronic xanthine oxidase inhibition following myocardial infarction in rabbits: effects of early versus delayed treatment. Life Sci. 82(9-10), 495-502 (2008).
59. Sanchez-Lozada LG, Tapia E, Bautista-Garcia P et al.: Effects of febuxostat on metabolic and renal alterations in rats with fructose-induced metabolic syndrome. Am. J. Physiol. Renal Physiol. 294(4), F710-F718 (2008).
60. Sanchez-Lozada LG, Tapia E, Soto V et al.: Treatment with the xanthine oxidase inhibitor febuxostat lowers uric acid and alleviates systemic and glomerular hypertension in experimental hyperuricaemia. Nephrol. Dial. Transplant. 23(4), 1179-1185 (2008).
61. Strozzullo P, Puig JG: Uric acid and cardiovascular risk: Is the devil always so bad? Nutr. Metab. Cardiovasc. Dis. 17(6), 409-414 (2007).