Febuxostat (Uloric) is a non-purine selective xanthine oxidase inhibitor with IC50 of 114 -210 nM. It works by non-competitively blocking the molybdenum pterin center which is the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Hence, febuxostat inhibits xanthine oxidase, therefore reducing production of uric acid. Febuxostat inhibits both, oxidized as well as reduced form of xanthine oxidase because of which febuxostat cannot be easily displaced from the molybdenum pterin site.
|Source||J Transl Med (2015). Figure 2. Febuxostat|
|Cell Lines||H/R and H/R + Veh cells|
|Concentrations||1 and 10 μM|
|Incubation Time||24 h|
|Results||24 h In comparison with Sham group, I/R treatment increased the apoptotic index (34.9 ± 2.6 vs. 4.5 ± 0.9%, P < 0.01). Pretreatment with either febuxostat or allopurinol effectively attenuated the increase in apoptotic index (Febuxostat: 26.9 ± 3.7 vs. 34.9 ± 2.6%; Allopurinol: 29.4 ± 1.9 vs. 34.9 ± 2.6%, P < 0.01, respectively).|
|Source||J Transl Med (2015). Figure 1. Febuxostat|
|Method||Experimental in vivo|
|Cell Lines||Male C57BL/6 mice|
|Incubation Time||24 h|
|Results||Febuxostat treatment effectively blocked the increase of CK and LDH activities compared with I/R mice (CK: 121.9 ± 16.6 vs. 196.3 ± 15.3 mU/ml; LDH 765.5 ± 166.1 vs. 1549.8 ± 365.8 mU/ml; P < 0.01, respectively), similar to allopurinol (CK: 138.2 ± 7.18 vs. 196.3 ± 15.3 mU/ml; LDH: 1005.9 ± 53.1 vs. 1549.8 ± 365.8 mU/ml; P < 0.01, respectively).|
|Animal models||Adult male albino Wistar rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Efficacy and safety of febuxostat in patients with hyperuricemia and gout.
Garcia-Valladares et al. Ther Adv Musculoskelet Dis. 2011 Oct;3(5):245-53. PMID: 22870483.
Cardiovascular safety of febuxostat and allopurinol in patients with gout and cardiovascular comorbidities.
White et al. Am Heart J. 2012 Jul;164(1):14-20.. PMID: 22795277.
Development and validation of a liquid chromatography-tandem mass spectrometry method for the determination of febuxostat in human plasma.
Wang et al. Biomed Chromatogr. 2012 May 24. PMID: 22623034.
Use of newly available febuxostat in a case of chronic tophaceous gout contraindicated to allopurinol and probenecid.
Hilmi et al. Med J Malaysia. 2012 Feb;67(1):125-6. PMID: 22582566.
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