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Febuxostat | CAS No: 144060-53-7 | GMP-certified suppliers
A medication that supports chronic management of hyperuricemia in adults with gout who cannot use allopurinol, helping maintain controlled urate levels for long‑term disease stability.
Therapeutic categories
Primary indications
- Febuxostat is indicated for the chronic management of hyperuricemia in adult patients with gout who have an inadequate response to a maximally titrated dose of [allopurinol], who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable
- It is not recommended for the treatment of asymptomatic hyperuricemia or secondary hyperuricemia
Product Snapshot
- Febuxostat is an oral small-molecule API supplied primarily for tablet and capsule formulations
- It is used for chronic management of hyperuricemia associated with gout in patients unsuitable for allopurinol
- The product holds approved status in major regulated markets including the US, EU, and Canada
Clinical Overview
Febuxostat selectively inhibits xanthine oxidoreductase, blocking both its oxidase and dehydrogenase forms. This suppresses the conversion of hypoxanthine to xanthine and xanthine to uric acid, reducing urate production independent of purine structural mimicry. Inhibition of the oxidase form can also reduce reactive oxygen species generation associated with inflammatory states.
Pharmacodynamically, daily dosing in the 40 to 80 mg range produces dose‑dependent decreases in serum uric acid of approximately 40 to 55 percent, with parallel reductions in serum xanthine and urinary uric acid excretion. Decreases in serum urate may transiently precipitate gout flares during initiation due to mobilization of tissue urate deposits.
Febuxostat undergoes extensive hepatic metabolism, with contributions from CYP1A2, CYP2C8, and CYP2C9 pathways, as well as UGT1A1, UGT1A3, UGT1A9, and UGT2B7. It is a substrate and inhibitor of certain transporters, including BCRP/ABCG2. Elimination occurs through both hepatic and renal routes. Clinically meaningful pharmacokinetic alterations may occur in moderate to severe hepatic impairment.
Safety considerations include a boxed warning regarding increased cardiovascular mortality observed in patients with gout and established cardiovascular disease in a post‑marketing trial. Use is generally reserved for patients unable to use allopurinol and is avoided in those with significant cardiovascular conditions. Photosensitivity reactions and gout flares have also been reported.
Notable marketed products include formulations for once‑daily oral administration across multiple regions. For API procurement, suppliers should provide evidence of control of polymorphic form, impurity profile, and residual solvent levels, along with compliance to ICH and regional pharmacopoeial specifications.
Identification & chemistry
| Generic name | Febuxostat |
|---|---|
| Molecule type | Small molecule |
| CAS | 144060-53-7 |
| UNII | 101V0R1N2E |
| DrugBank ID | DB04854 |
Pharmacology
| Summary | Febuxostat is a selective inhibitor of xanthine oxidoreductase, blocking both its oxidase and dehydrogenase activities to reduce uric acid production in purine metabolism. By limiting urate generation, it lowers serum uric acid levels and can influence urate crystal mobilization. Inhibiting both forms of the enzyme also reduces associated reactive oxygen species formation and related oxidative stress. |
|---|---|
| Mechanism of action | Gout is a form of acute arthritis that is characterized by the accumulation of crystals of monosodium urate and urate crystals in or around a joint, leading to inflammation and persistent urate crystal deposition in bones, joints, tissues, and other organs that may exacerbate over time. Hyperuricemia is closely related to gout, whereby it may exist for many years before the first clinical attack of gout; thus, aberrated serum uric acid levels and hyperuricemia are believed to be the biochemical aberration involved in the pathogenesis of gout.Xanthine oxidoreductase (XOR) can act as a xanthine oxidase or xanthine dehydrogenase. In humans, it is a critical enzyme for uric acid production as it catalyzes the oxidation reaction steps from hypoxanthine to xanthine and from xanthine to uric acid in the pathway of purine metabolism.Febuxostat potently inhibits XOR, blocking both its oxidase and dehydrogenase activities. With high affinity, febuxostat binds to XOR in a molecular channel leading to the molybdenum-pterin active site, where [allopurinol] demonstrates relatively weak competitive inhibition. XOR is mainly found in the dehydrogenase form under normal physiological conditions; however, in inflammatory conditions, XOR can be converted into the xanthine oxidase form, which catalyzes reactions that produce reactive oxygen species (ROS), such as peroxynitrite. ROS contribute to vascular inflammation and alterations in vascular function. As febuxostat can inhibit both forms of XOR, it can inhibit ROS formation, oxidative stress, and inflammation.In a rat model, febuxostat suppressed renal ischemia-reperfusion injury by attenuating oxidative stress. |
| Pharmacodynamics | Febuxostat is a novel, selective xanthine oxidase/dehydrogenase inhibitor that works by decreasing serum uric acid in a dose-dependent manner. In healthy subjects, febuxostat decreased the mean serum uric acid and serum xanthine concentrations, as well as the total urinary uric acid excretion. Febuxostat at daily doses of 40-80 mg reduced the 24-hour mean serum uric acid concentrations by 40 to 55%.Closely related to the drug-induced reduction of serum uric acid levels and mobilization of urate crystals in tissue deposits, febuxostat is associated with gout flares. Unlike [allopurinol] and [oxypurinol], febuxostat has no inhibitory actions against other enzymes involved in purine and pyrimidine synthesis and metabolism, because it does not structurally resemble purines or pyrimidines. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Xanthine dehydrogenase/oxidase | Humans | inhibitor |
ADME / PK
| Absorption | After oral administration, about 85% of febuxostat is absorbed rapidly.T<sub>max</sub> ranges from 1 to 1.5 hours. Following once-daily oral administration, C<sub>max</sub> was approximately 1.6 ± 0.6 mcg/mL at a dose of 40 mg febuxostat and 2.6 ± 1.7 mcg/mL at a dose of 80 mg febuxostat. A high-fat meal decreased C<sub>max</sub> by 49% and AUC by 18%, but there were no clinically significant changes in the ability of febuxostat to decrease serum uric acid concentrations. |
|---|---|
| Half-life | The apparent mean terminal elimination half-life of approximately 5 to 8 hours. |
| Protein binding | Febuxostat is approximately 99.2% bound to plasma proteins, primarily to albumin. Plasma protein binding is constant over the concentration range achieved with 40 mg and 80 mg doses. |
| Metabolism | Febuxostat is metabolized in the liver by UDP-glucuronosyltransferase (UGT) and Cytochrome P450 (CYP) enzymes, with the relative contribution of each enzyme isoform in the metabolism of febuxostat not fully elucidated. UGT1A1, UGT1A3, UGT1A9, and UGT2B7 mediate conjugation of febuxostat,which approximately accounts for 22–44% of the metabolism of the total dose administered, to produce the acyl-glucuronide metabolite.CYP1A2, CYP2C8, CYP2C9, and non-P450 enzymes are responsible for the oxidation reaction, which accounts for 2-8% of the metabolism of the dose.Oxidation reaction produces 67M-1, 67M-2, and 67M-4, which are pharmacologically active metabolites. 67M-1, 67M-2, and 67M-4 can further undergo glucuronidation and sulfation.Hydroxy metabolites are present in human plasma at much lower concentrations than the parent drug. |
| Route of elimination | Febuxostat is eliminated via both hepatic and renal pathways. Following oral administration of 80 mg radiolabeled febuxostat, approximately 49% of the dose was recovered in the urine. In urine, about 3% of the recovered dose accounted for unchanged febuxostat, 30% accounted for the acyl glucuronide metabolite, 13% accounted for oxidative metabolites and their conjugates, and 3% accounted for unidentified metabolites. Approximately 45% of the total dose was recovered in the feces, where 12% of the dose accounted for the unchanged parent drug. About 1% accounted for the acyl glucuronide metabolite, 25% accounted for oxidative metabolites and their conjugates, and 7% accounted for unidentified metabolites. |
| Volume of distribution | The apparent steady-state volume of distribution (V<sub>ss</sub>/F) of febuxostat ranges from 29 to 75 L, indicating a low to medium volume of distribution. |
| Clearance | Following oral administration of single doses of 10 to 240 mg, the mean apparent total clearance ranged from 10 to 12 L/h. |
Formulation & handling
- Oral small‑molecule API with low aqueous solubility, typically requiring solid‑dose technologies that enhance dissolution (e.g., particle size control or solubilizing excipients).
- Moderate lipophilicity (LogP ~3.5) and food‑insensitive absorption allow flexible oral formulations without strict fed/fasted constraints.
- Solid, thermally stable profile supports conventional tablet and capsule manufacturing with standard protection from moisture due to poor water solubility.
Regulatory status
| Lifecycle | The API shows a mixed lifecycle profile, with several U.S. patents expired (2019–2024) and remaining protections extending to 2031. In the EU, Canada, and the US, the market is partially mature with potential for increasing generic presence as later patents approach expiry. |
|---|
| Markets | EU, Canada, US |
|---|
Supply Chain
| Supply chain summary | Febuxostat is supplied primarily by a single originator manufacturer, with the branded product marketed across the EU, Canada, and the US. Core US patents expired in 2019 and 2024, while later‑expiring patents extend to 2031, creating mixed protection depending on jurisdiction and patent family. These expiries indicate that generic competition is already present in some markets, with additional entrants possible as remaining protections lapse. |
|---|
Safety
| Toxicity | Oral lowest published toxic dose (TDLO) in humans is 1.82 mg/kg/14D (intermittent).Oral LD<sub>50</sub> is 300 mg/kg in mice, 3200 mg/kg in rabbits, and 980 mg/kg in rats. No dose-limiting toxicities were observed with febuxostat administered at doses up to 300 mg daily for seven days in healthy subjects. There are no reports of overdose of febuxostat in clinical studies and there is no known antidote. Overdose should be managed by symptomatic and supportive care. |
|---|
- Human oral TDLO is reported at 1
- 82 mg/kg over 14 days (intermittent), with species‑specific oral LD50 values ranging from approximately 300 mg/kg (mouse) to 3200 mg/kg (rabbit), indicating moderate acute toxicity variability across models
- No dose‑limiting toxicities were identified in short‑term studies up to 300 mg/day in healthy subjects, and no antidote has been characterized for febuxostat exposure
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Febuxostat is a type of Uric acid lowering agents
Uric acid lowering agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) specifically designed to target and reduce elevated levels of uric acid in the body. Uric acid is a byproduct of purine metabolism and is typically excreted through the kidneys. However, when uric acid levels become excessively high, it can lead to a condition known as hyperuricemia, which is associated with gout and other related disorders.
Uric acid lowering agents work by inhibiting the production of uric acid or enhancing its excretion from the body. One commonly used class of drugs in this category is xanthine oxidase inhibitors (XOIs), which inhibit the enzyme xanthine oxidase responsible for converting purines to uric acid. By reducing the activity of xanthine oxidase, XOIs effectively lower uric acid levels.
Another class of drugs used as uric acid lowering agents are uricosurics. Uricosurics work by blocking the reabsorption of uric acid in the kidneys, thereby increasing its elimination through urine. This mechanism helps to lower the concentration of uric acid in the bloodstream.
Uric acid lowering agents play a crucial role in the management of hyperuricemia and related conditions such as gout. By effectively reducing uric acid levels, these pharmaceutical APIs alleviate symptoms associated with elevated uric acid, such as joint pain and inflammation.
It is important to note that the use of uric acid lowering agents should be done under the guidance and supervision of a healthcare professional. Individual patient factors and medical history should be considered when determining the appropriate medication and dosage.
Febuxostat (Uric acid lowering agents), classified under Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
Febuxostat API manufacturers & distributors
Compare qualified Febuxostat API suppliers worldwide. We currently have 28 companies offering Febuxostat API, with manufacturing taking place in 8 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 229 products |
| AXXO GmbH | Distributor | Germany | European Union | CoA, EDMF/ASMF, GMP, GDP, MSDS, USDMF | 243 products |
| Curia | Producer | United States | Spain | CoA, GMP, MSDS | 106 products |
| Dalian Wista Pharma Co Lt... | Producer | China | China | CoA | 16 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Duke Chem | Producer | Spain | Spain | CoA, GMP | 8 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Emeishan Hongsen Biopharm... | Producer | China | China | CoA, GMP, MSDS | 107 products |
| Excel Industries | Producer | India | India | CoA | 2 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF | 484 products |
| HEC Pharm | Producer | Germany | Unknown | CoA, USDMF | 31 products |
| Indoco Remedies | Producer | India | India | CoA, GMP, USDMF, WC | 19 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lupin | Producer | India | India | CoA, GMP, USDMF, WC | 155 products |
| MSN Organics | Producer | India | India | CoA, GMP, USDMF, WC | 21 products |
| Mylan | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 201 products |
| NGL Fine Chem | Producer | India | India | CoA | 4 products |
| PLIVA | Producer | Czech Republic | Croatia | CoA, GMP | 31 products |
| Quimica Sintetica | Producer | Spain | Spain | CoA, GMP | 51 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, GMP, JDMF, MSDS, USDMF, WC | 55 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 764 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
| Utopharm (Shanghai) Compa... | Producer | China | China | CoA | 12 products |
| Vasudha Pharma Chem Ltd. | Producer | India | India | CoA, GMP, MSDS, USDMF, WC | 37 products |
| WANBANG BIOPHARMA | Producer | China | China | CoA, USDMF | 2 products |
When sending a request, specify which Febuxostat API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Febuxostat API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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