Febuxostat

Inquiry

Cat Number

API144060537

CAS Number

144060-53-7

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Customer Q&A

CAS Number

144060-53-7

EINECS

682-158-6

Storage

Store at room temperature

Synonyms

Adenuric; Uloric; Tei-6720; TMX 67; 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid

Molecular Formula

C16H16N2O3S

Molecular Weight

316.4

Smiles

CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O

Appearance

White to off-white crystalline powder

Melting Point

238-239℃

Boiling Point

536.6±60.0℃

General Description

Febuxostat is a non-purine selective inhibitor of xanthine oxidase, used for the chronic management of hyperuricemia in gout. It offers an alternative to allopurinol for patients with hypersensitivity or intolerance. The drug has a dual mechanism of action by inhibiting both the oxidized and reduced forms of xanthine oxidase.

Mechanism of Action

Febuxostat tightly binds to the molybdenum-pterin active site of xanthine oxidase, blocking the conversion of hypoxanthine to xanthine and xanthine to uric acid. This reduces serum urate levels by inhibiting the final two steps of purine degradation. Unlike allopurinol, febuxostat is not a purine base analogue and does not affect other enzymes involved in pyrimidine metabolism. The drug is metabolized primarily by the liver via CYP1A2, CYP2C8, and CYP2C9.

Application

Febuxostat is indicated for the long-term treatment of hyperuricemia in patients with gout who have failed or cannot tolerate allopurinol. Febuxostat is generally reserved for patients with contraindications or intolerance to allopurinol, and only after careful cardiovascular risk assessment.

In a prospective randomized open‑label trial (1070 elderly hyperuricemic patients with hypertension, diabetes, renal disease, or prior cardiovascular events), febuxostat lowered serum uric acid to 4.50 mg/dL versus 6.76 mg/dL in the non‑febuxostat group (P<0.001). The primary composite endpoint (cerebral, cardiovascular, renal events, and death) was significantly lower in the febuxostat group (HR 0.750, 95% CI 0.592–0.950; P=0.017). The most frequent event was renal impairment, which febuxostat delayed (HR 0.745, 95% CI 0.562–0.987; P=0.041). Febuxostat effectively lowers uric acid and slows the progression of renal dysfunction in high‑risk patients.

Fig. 1 Serial changes in serum uric acid level in the febuxostat and non-febuxostat groups. (Kojima S, et al., 2019)

References

Kojima S, et al. Febuxostat for Cerebral and CaRdiorenovascular Events PrEvEntion StuDy. Eur Heart J. 2019;40(22):1778-1786.

Does Febuxostat require protection from light during long-term storage?

Yes, it is photosensitive. UV light can cause photodegradation and discoloration. Store in light-resistant, tightly sealed containers, preferably original opaque packaging.

What is the recommended storage temperature for Febuxostat?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which can accelerate oxidative degradation of the thiazole ring.

Is Febuxostat susceptible to moisture-induced degradation?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and form a hydrate, affecting dissolution. Store with desiccant for long-term stability.

How is the impurity febuxostat N-oxide monitored during stability?

This oxidative degradation product is quantified using a stability-indicating HPLC method, ensuring it remains below ICH qualification thresholds.