Febuxostat

• CAT Number: A000541
• CAS Number: 144060-53-7
• Molecular Formula: C16H16N2O3S
• Molecular Weight: 316.40
• Purity: ≥95%
• Synonyms: 144060-53-7; Adenuric; Uloric; Tei 6720; Tei-6720
• Target: XAO
• Solubility: >15.55mg/mL in DMSO
• Storage: -20°C
• IUPAC Name: 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
• InChI: InChI=1S/C16H16N2O3S/c1-9(2)8-21-13-5-4-11(6-12(13)7-17)15-18-10(3)14(22-15)16(19)20/h4-6,9H,8H2,1-3H3,(H,19,20)
• InChIKey: BQSJTQLCZDPROO-UHFFFAOYSA-N
• SMILES: CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O

Febuxostat（Cat No.:A000541）is a non-purine selective inhibitor of xanthine oxidase, used to treat hyperuricemia in patients with gout. By blocking xanthine oxidase, febuxostat reduces the production of uric acid, thereby lowering serum urate levels and preventing crystal deposition in joints and tissues. Unlike allopurinol, febuxostat is more selective and can be effective in patients with mild to moderate kidney impairment. Its targeted approach helps manage gout symptoms and prevents flare-ups, making it a valuable option for long-term uric acid control with a reduced risk of severe hypersensitivity reactions.

Reference

1: Nigovic B, Milanovic I. Green Electroanalytical Method for Fast Measurement of
Xanthine Oxidase Inhibitor Febuxostat. Anal Sci. 2017;33(11):1219-1223. doi:
10.2116/analsci.33.1219. PubMed PMID: 29129858.

2: Honorat JA, Nakatsuji Y, Shimizu M, Kinoshita M, Sumi-Akamaru H, Sasaki T,
Takata K, Koda T, Namba A, Yamashita K, Sanda E, Sakaguchi M, Kumanogoh A,
Shirakura T, Tamura M, Sakoda S, Mochizuki H, Okuno T. Febuxostat ameliorates
secondary progressive experimental autoimmune encephalomyelitis by restoring
mitochondrial energy production in a GOT2-dependent manner. PLoS One. 2017 Nov
6;12(11):e0187215. doi: 10.1371/journal.pone.0187215. eCollection 2017. PubMed
PMID: 29107957.

3: Gunawardhana L, McLean L, Punzi HA, Hunt B, Palmer RN, Whelton A, Feig DI.
Effect of Febuxostat on Ambulatory Blood Pressure in Subjects With Hyperuricemia
and Hypertension: A Phase 2 Randomized Placebo-Controlled Study. J Am Heart
Assoc. 2017 Nov 4;6(11). pii: e006683. doi: 10.1161/JAHA.117.006683. PubMed PMID:
29102979.

4: Yamanaka H, Tamaki S, Ide Y, Kim H, Inoue K, Sugimoto M, Hidaka Y, Taniguchi
A, Fujimori S, Yamamoto T. Stepwise dose increase of febuxostat is comparable
with colchicine prophylaxis for the prevention of gout flares during the initial
phase of urate-lowering therapy: results from FORTUNE-1, a prospective,
multicentre randomised study. Ann Rheum Dis. 2017 Nov 4. pii:
annrheumdis-2017-211574. doi: 10.1136/annrheumdis-2017-211574. [Epub ahead of
print] PubMed PMID: 29102957.

5: Yin YF, Guo Y, Song WD, Duan XC, Zheng XC, Zhong T, Zhang S, Yao X, Xu MQ,
Zhang Q, Zhang X. Improving Solubility and Oral Bioavailability of Febuxostat by
Polymer-Coated Nanomatrix. AAPS PharmSciTech. 2017 Oct 27. doi:
10.1208/s12249-017-0905-z. [Epub ahead of print] PubMed PMID: 29079988.

6: Sheer R, Null KD, Szymanski KA, Sudharshan L, Banovic J, Pasquale MK.
Predictors of reaching a serum uric acid goal in patients with gout and treated
with febuxostat. Clinicoecon Outcomes Res. 2017 Oct 10;9:629-639. doi:
10.2147/CEOR.S139939. eCollection 2017. PubMed PMID: 29066924; PubMed Central
PMCID: PMC5644566.

7: Collison J. Crystal arthritis: Febuxostat reduces synovitis in early gout. Nat
Rev Rheumatol. 2017 Oct 20. doi: 10.1038/nrrheum.2017.176. [Epub ahead of print]
PubMed PMID: 29051626.

8: Muraki S, Moriki K, Shigematsu S, Fukae M, Kakara M, Yamashita D, Hirota T,
Takane H, Shimada M, Hirakawa M, Ieiri I. Population Pharmacodynamic Analysis of
Uric Acid-Lowering Effects of Febuxostat Based on Electronic Medical Records in
Two Hospitals. J Clin Pharmacol. 2017 Oct 18. doi: 10.1002/jcph.1023. [Epub ahead
of print] PubMed PMID: 29045766.

9: Cutolo M, Cimmino MA, Perez-Ruiz F. Potency on lowering serum uric acid in
gout patients: a pooled analysis of registrative studies comparing febuxostat vs.
allopurinol. Eur Rev Med Pharmacol Sci. 2017 Sep;21(18):4186-4195. PubMed PMID:
29028079.

10: Kishimoto K, Kobayashi R, Hori D, Sano H, Suzuki D, Kobayashi K. Febuxostat
as a Prophylaxis for Tumor Lysis Syndrome in Children with Hematological
Malignancies. Anticancer Res. 2017 Oct;37(10):5845-5849. PubMed PMID: 28982910.