FEBUXOSTAT API

FEBUXOSTAT API - Names and Identifiers

Name	Febuxostat
Synonyms	FBX Uloric Febuxostat FEBUXOSTAT API Febuxostat Tablets Febuxostat (Uloric) Febuxostat (TEI-6720) Febuxostat Tabletshehe Febuxostat (Polymorphs) Febuxostat (This product is unavailable in the U.S.) 2-[3-Cyano-4-isobutoxyphenyl]-4-methylthiazole-5-carboxylic acid 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid 2-[3-Cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
CAS	144060-53-7
EINECS	682-158-6
InChI	InChI=1/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)

FEBUXOSTAT API - Physico-chemical Properties

Molecular Formula	C16H16N2O3S
Molar Mass	316.37
Density	1.31±0.1 g/cm3(Predicted)
Melting Point	238-239°(dec.)
Boling Point	536.6±60.0 °C(Predicted)
Flash Point	278.3°C
Solubility	DMSO 63 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Vapor Presure	2.41E-12mmHg at 25°C
Appearance	Crystalline solid
Color	White to Off-White
Merck	14,3948
pKa	2.48±0.10(Predicted)
Storage Condition	2-8°C
Refractive Index	1.605
MDL	MFCD00871598
Physical and Chemical Properties	specification; White crystalline powder Melting Point: 201-202 ℃

FEBUXOSTAT API - Risk and Safety

RTECS

XJ3675310

FEBUXOSTAT API - Reference

Reference

1. Xu, Lieqiang, et al. "Anti-Hyperuricemic and Nephroprotective Effects of Dihydroberberine in Potassium Oxonate-and Hypoxanthine-Induced Hyperuricemic Mice." Frontiers in Pharmacology 12 (2021): 804.
2. [IF=6.529] Haiyang Yang et al."Accurate quantitative determination of affinity and binding kinetics for tight binding inhibition of xanthine oxidase."Biomed Pharmacother. 2021 Jul;139:111664
3. [IF=5.81] Xu Lieqiang et al."Anti-Hyperuricemic and Nephroprotective Effects of Dihydroberberine in Potassium Oxonate- and Hypoxanthine-Induced Hyperuricemic Mice."Front Pharmacol. 2021 Apr;0:804

FEBUXOSTAT API - Reference Information

Product description	Febuxostat (febuxostat) is a new generation of xanthine oxidase inhibitor developed by Japan Teijin Company. It is clinically used to treat hyperuricemia (gout). The structure is completely different from the xanthine oxidase inhibitor drug developed 40 years ago. It is a new and efficient non-purine xanthine oxidase selective inhibitor. Xanthine oxidase is a key enzyme that promotes the production of uric acid. Febuxostat can reduce the level of uric acid in the blood of patients with hyperuricemia and gout. Clinical studies have shown that this product is safe and effective. This product is metabolized by the liver and does not depend on the kidney. Therefore, it is effective for moderate-severe liver and kidney. Patients with renal insufficiency do not need to reduce the dose. The dosage is 40 mg or 80 mg once a day. It is not recommended for the treatment of gout patients without hyperuricemia. In February 2009, the U.S. Food and Drug Administration (FDA) approved febuxostat for the long-term treatment of gout hyperuricemia patients.
anti-gout drugs	gout is a group of heterogeneous diseases, which are hereditary or acquired uric acid excretion reduction and purine metabolism disorders. Due to excessive uric acid in the body and decreased renal clearance ability, uric acid accumulation in the body, resulting in the deposition of urate crystals in joints and various organs. Therefore, gout is usually treated by promoting uric acid excretion and inhibiting uric acid production, and adopting appropriate measures to improve related symptoms. The production of uric acid in the body is related to purine metabolism. In the final step of purine metabolism, hypoxanthine generates xanthine under the action of xanthine oxidoreductase (XOR), and then further generates uric acid, inhibiting the activity of the enzyme can effectively Reduce the production of uric acid. Febuxostat is a new generation of non-purine selective xanthine oxidase inhibitors newly developed in the world. It acts on the oxidase highly selectively to reduce the synthesis of uric acid in the body and reduce the concentration of uric acid, thereby effectively treating ventilation diseases. In the past 30 years, allopurinol is the only drug used to inhibit uric acid production in clinic, and is widely used as a golden treatment for gout, and has achieved good results in anti-gout treatment. Compared with allopurine, febuxostat has obvious advantages:(1) allopurinol only has an inhibitory effect on reduced XOR, while non-buxostat has a significant inhibitory effect on oxidized and reduced XOR. Therefore, its effect on reducing uric acid is more powerful and lasting;(2) Because allopurinol is a purine analog, it inevitably causes the effect of other enzyme activities involving purine and pyridine metabolism. Therefore, in allopurinol treatment, repeated high-dose administration is required to maintain high drug levels. This also brings serious and even fatal adverse reactions caused by drug accumulation. And non-buxotan is a non-purine XOR inhibitor, so it has better safety.
drugs to increase the risk of gout	diuretics: furosemide (furosemide), hydrochlorothiazide (hydrochlorothiazide), metorazon (metolazone) salicylic acid: such as aspirin (aspirin), nicotinic acid cyclosporin (CyclosporineNeoral), levodopa (Levodopa)
intermediate	4-hydroxythiobenzamide CAS No.:25984-63-8 Appearance: light green to white-like powder. 2-(4-hydroxyphenyl)-4-methylthiazol-5-ethyl formate CAS:161797-99-5 Appearance: yellow powder. 2-(3-aldo-4-hydroxyphenyl)-4-methylthiazol-5-ethyl formate CAS No.:161798-01-2 Appearance: light yellow to yellow powder. 2-[3-aldo-4-isobutoxyphenyl]-4-methylthiazol-5-ethyl formate CAS No.:161798-03-4 Appearance: light yellow to white-like powder. 2-[3-cyano-4-isobutoxyphenyl]-4-methylthiazol-5-ethyl formate CAS No.:160844-75-7 Appearance: white-like to white powder.
Use	Treatment of hyperuric acid (gout) A xanthine oxidase and xanthine dehydrogenase inhibitor.

Last Update：2024-04-10 22:29:15