Febuxostat for Gout and Hyperuricemia

English name：Febuxostat

CAS number：144060-53-7

Molecular formula: C16H16N2O3S

Molecular weight: 316.37

EINECS number: 682-158-6

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Mol file：144060-53-7.mol

Structural formula:

Melting point: 238-239°(dec.)

Boiling point: 536.6±60.0°C(Predicted)

Density: 1.31±0.1g/cm3(Predicted)

Chemicalbook storage conditions: 2-8°C

Solubility: Soluble in DMSO (a little), methanol (a little)

Acidity coefficient (pKa) : 2.48±0.10(Predicted)

Form: Powder

Color: White to almost white

Merck：14,3948

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：S1C(C(O)=O)=C(C)N=C1C1=CC=C(OCC(C)C)C(C#N)=C1

CAS database： 144060-53-7(CAS DataBase Reference)

Product description

febuxostat (febuxostat) is a new generation of xanthine oxidase inhibitor developed by Teijin Corporation of Japan, which is clinically used to treat hyperuricemia (gout). The structure of Febuxostat is completely different from the xanthine oxidase inhibitor drugs developed 40 years ago, and it is a new high-efficiency non-purine xanthine oxidase selective inhibitor. Xanthine oxidase is a Chemicalbook key enzyme that promotes the production of uric acid. Febuxotam can reduce the level of uric acid in the blood of patients with hyperuricemic gout. Clinical studies have shown that Febuxotam is safe and effective. It is metabolized by the liver and does not depend on renal excretion, so it is not necessary to reduce the dose in patients with moderate to severe hepatic and renal insufficiency. The dosage is 40 mg or 80 mg once daily and is not recommended for gout patients without hyperuricemia.

In February 2009, febuxotam was approved by the U.S. Food and Drug Administration (FDA) for the long-term treatment of patients with gout hyperuricemia.

Antigout drugs

Gout is a group of heterogeneous diseases that are inherited or acquired due to reduced excretion of uric acid and dysfunction of purine metabolism. Due to the excessive production of uric acid in the body and the decreased clearance capacity of the kidneys, the Chemicalbook of uric acid accumulates in the body, resulting in the deposit of urate crystals in the joints and organs. Therefore, gout is usually treated by promoting uric acid excretion and inhibiting uric acid production, and taking appropriate measures to improve related symptoms.

The production of uric acid in the body is related to the metabolism of purine. In the last step of purine metabolism, hypoxanthine produces xanthine under the action of xanthine oxidorereductase (XOR), and then produces uric acid further. Inhibiting the activity of this enzyme can effectively reduce the Chemicalbook production of uric acid. Febuxotam is a new generation of non-purine selective xanthine oxidase inhibitor recently developed in the world. By highly selective action on the oxidase, Febuxotam can reduce the synthesis of uric acid in the body and reduce the concentration of uric acid, thus effectively treating ventilation diseases.

In the past 30 years, allopurinol is the only drug used to inhibit uric acid production in clinical practice, and has been widely used in clinical practice as a gold treatment for gout, and has achieved good results in the treatment of anti-gout. Compared with allopurine, febuxostat has obvious advantages:

(1) Allopurinol can only inhibit the reduced XOR, while febuxotan can significantly inhibit both the oxidized and reduced XOR, so its uric acid lowering effect is more powerful and lasting;

(2) Since allopurinol is a purine analogue, it inevitably causes effects on the activity of other enzymes involved in purine and pyridine metabolism. Therefore, in allopurinol therapy, it is necessary to repeat large doses to maintain a higher drug level than Chemicalbook. This also leads to serious and even fatal adverse reactions due to drug accumulation. Febuxostat is a non-purine XOR inhibitor and therefore has a better safety profile.

Drugs that increase the risk of gout

Diuretics: furosemide, hydrochlorothiazide, metolazone

Salicylic acids: such as aspirin

Nicotinic acid

CyclosporineNeoral

Levodopa

Intermediate

4-hydroxythiobenzamide CAS No. : 25984-63-8 Appearance: Light green to white powder.

2- (4-hydroxyphenyl) -4-methylthiazole-5-ethyl formate CAS: 161797-99-5 Appearance: yellow powder.

2-(3-aldehyde - 4-hydroxyphenyl) -4-methylthiazole-5-ethyl formate CAS No. : 161798-01-2 Appearance: Light yellow to yellow powder.

2-[3-aldehyde-4-isobutoxy-phenyl] -4-methylthiazole-5-ethyl formate CAS No. : 161798-03-4 Appearance: Light yellow to white powder.

2-[3-cyano-4-isobutoxy-phenyl] -4-methylthiazole-5-ethyl formate CAS No. : 160844-75-7 Appearance: white to white powder.

Clinical application

Febuxostat, or febuxostat, clinically translated as febuxostat, is a drug that reduces uric acid production and should be taken as prescribed by a doctor. The drug reduces uric acid synthesis in the body, and Chemicalbook is commonly used to treat gout, which can improve the symptoms of gout in patients. When patients take febuxostat, they should follow the doctor's advice and not increase or decrease the dosage at will to avoid poor treatment effect.

Use

Treatment of hyperuricemia (Gout)

A xanthine oxidase and xanthine dehydrogenase inhibitor.

Safety information

RTECS number: XJ3675310

Customs Code: 2934.10.2000

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