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Lesinurad | CAS No: 878672-00-5 | GMP-certified suppliers
A medication that aids in managing hyperuricemia associated with gout by enhancing uric acid excretion when combined with a xanthine oxidase inhibitor in patients with insufficient response.
Therapeutic categories
Primary indications
- For use, in combination with a xanthine oxidase inhibitor, for the treatment of hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone
Product Snapshot
- Lesinurad is an oral small molecule formulated as film-coated tablets
- It is indicated for use in combination with xanthine oxidase inhibitors to manage hyperuricemia associated with gout
- Lesinurad holds regulatory approval in the US and EU markets
Clinical Overview
Pharmacologically, lesinurad belongs to the phenyl-1,2,4-triazole class of organic compounds. It exerts its effects by selectively inhibiting URAT1 and organic anion transporter 4 (OAT4). URAT1 is a major renal transporter responsible for the reabsorption of uric acid from the renal proximal tubules, while OAT4 contributes to uric acid retention, particularly in the context of diuretic therapy. Inhibition of these transporters increases urinary excretion of uric acid, resulting in dose-dependent reductions in serum urate concentrations.
Pharmacodynamic studies demonstrate that lesinurad produces significant increases in uric acid clearance with corresponding decreases in serum urate after single and multiple oral doses. Pharmacokinetic data indicate renal elimination as the primary excretion pathway. Lesinurad is also a substrate and inducer of cytochrome P450 enzymes, notably CYP2C9 and CYP3A4, which can have implications for drug-drug interactions and metabolism.
Safety considerations include monitoring for renal adverse effects, as the uricosuric mechanism increases uric acid excretion via the kidney, which may elevate the risk of nephrolithiasis and acute renal failure if not managed appropriately. Lesinurad is contraindicated as monotherapy due to increased rates of renal adverse events observed in clinical trials.
From a sourcing and quality perspective, the lesinurad API should comply with relevant pharmacopeial standards and undergo rigorous analytical characterization to ensure purity, consistency, and stability. Given its involvement with cytochrome P450 metabolism and renal elimination, batch-to-batch consistency in impurity profiles and physicochemical properties is critical for safe formulation and regulatory compliance.
Identification & chemistry
| Generic name | Lesinurad |
|---|---|
| Molecule type | Small molecule |
| CAS | 878672-00-5 |
| UNII | 09ERP08I3W |
| DrugBank ID | DB11560 |
Pharmacology
| Summary | Lesinurad is a uricosuric agent that targets uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4) to inhibit renal reabsorption of uric acid. By blocking these transporters, it promotes increased urinary excretion of uric acid, leading to dose-dependent reductions in serum uric acid levels. It is intended for use alongside xanthine oxidase inhibitors to manage hyperuricemia associated with gout. |
|---|---|
| Mechanism of action | Lesinurad inhibits the activity of uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4). URAT1 is a major transporter enzyme responsible for reuptake of uric acid from the renal tubules; inhibition of URAT1 function thereby increases excretion of uric acid. |
| Pharmacodynamics | Dose-dependent reductions in serum uric acid levels and increases in urinary uric acid excretion have been observed following single and multiple oral doses of lesinurad. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Solute carrier family 22 member 12 | Humans | inhibitor |
| Solute carrier family 22 member 11 | Humans | inhibitor |
ADME / PK
| Absorption | Oral lesinurad is rapidly absorbed, reaching maximum plasma concentrations (Cmax) within 1–4 h following the administration a single 200 mg dose (in either the fed or fasted state). |
|---|---|
| Protein binding | Lesinurad is extensively bound to proteins in plasma (greater than 98%), mainly to albumin. |
| Metabolism | Lesinurad undergoes oxidative metabolism mainly via the polymorphic cytochrome P450 CYP2C9 enzyme. |
| Route of elimination | Within 7 days following single dosing of radiolabeled lesinurad, 63% of administered radioactive dose was recovered in urine and 32% of administered radioactive dose was recovered in feces. Most of the radioactivity recovered in urine (> 60% of dose) occurred in the first 24 hours. Unchanged lesinurad in urine accounted for approximately 30% of the dose. |
| Volume of distribution | The mean steady state volume of distribution of lesinurad was approximately 20 L following intravenous dosing. |
Formulation & handling
- Lesinurad is a small molecule intended for oral administration as film-coated tablets.
- It exhibits low water solubility and has a moderate lipophilicity (LogP 4.09), which may affect formulation strategies.
- The API requires administration with food and adequate hydration to optimize absorption and reduce potential gastrointestinal effects.
Regulatory status
| Lifecycle | The API is currently under patent protection in the United States until dates ranging from late 2028 to mid-2030, indicating it remains in a protected lifecycle phase. It is marketed in both the US and EU, with potential for generic competition primarily after patent expirations in the US market. |
|---|
| Markets | US, EU |
|---|
Supply Chain
| Supply chain summary | Lesinurad is marketed under multiple branded products, primarily in the US and EU markets, with a limited global footprint beyond these regions. The originator companies maintain patent protection in the United States extending through 2028 to 2030, indicating that generic competition is not yet prevalent but may emerge once these patents expire. The supply landscape currently centers around originator firms managing both manufacturing and distribution. |
|---|
Lesinurad 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.
Lesinurad (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.
Lesinurad API manufacturers & distributors
Compare qualified Lesinurad API suppliers worldwide. We currently have 1 companies offering Lesinurad API, with manufacturing taking place in 1 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, CoA, GMP, MSDS, USDMF | 229 products |
When sending a request, specify which Lesinurad 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.).
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