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Probenecid | CAS No: 57-66-9 | GMP-certified suppliers
A medication that lowers serum uric acid to help manage chronic gouty arthritis, tophaceous gout, and diuretic‑related hyperuricemia for patients with recurrent debilitating attacks.
Therapeutic categories
Primary indications
- For the reduction of serum uric acid concentrations in chronic gouty arthritis and tophaceous gout in patients with frequent disabling gout attacks
- Has also been effectively used to promote uric acid excretion in hyperuricemia secondary to the administration of thiazide and related diuretics
Product Snapshot
- Oral small-molecule product supplied as tablets and capsules
- Used to lower serum uric acid in chronic gout and hyperuricemia associated with diuretic use
- Approved in the US and Canada, with additional investigational status in some contexts
Clinical Overview
Probenecid decreases tubular reabsorption of urate in the proximal convoluted tubule, promoting urinary excretion and reducing the miscible urate pool. Sustained uricosuria supports gradual mobilization of urate deposits in chronic gout. The compound competitively inhibits the renal secretion pathways of many weak organic acids, including penicillins and most cephalosporins. This effect can meaningfully increase systemic exposure to antibiotics predominantly cleared through tubular secretion.
Mechanistically, probenecid may interfere with transport enzymes requiring high‑energy phosphate bonds or disrupt substrate interaction at renal tubular receptor sites. It also interacts with several transporters, including OAT1, OAT3, and organic cation transporters, which contributes to its broad effects on renal drug handling.
Absorption is generally adequate after oral administration, with extensive plasma protein binding. The compound undergoes hepatic metabolism and is excreted primarily via the kidneys. Drug interactions are clinically important, particularly for agents with narrow therapeutic indices that rely on active tubular secretion. Safety considerations include the risk of uric acid nephrolithiasis, hypersensitivity reactions, and reduced efficacy in patients with significant renal impairment. Adequate hydration and cautious use with other renally cleared drugs are recommended.
Probenecid has been historically included in combination regimens for gonorrhea, neurosyphilis, and pelvic inflammatory disease to sustain antibiotic exposure.
For API procurement, sourcing should emphasize verified identity, control of sulfonamide-related impurities, and compliance with regional pharmacopeial specifications to ensure reliable performance in formulation and clinical use.
Identification & chemistry
| Generic name | Probenecid |
|---|---|
| Molecule type | Small molecule |
| CAS | 57-66-9 |
| UNII | PO572Z7917 |
| DrugBank ID | DB01032 |
Pharmacology
| Summary | Probenecid is a uricosuric agent that increases urinary uric acid excretion by inhibiting renal tubular reabsorption of urate, primarily through effects on organic anion transporters such as SLC22 family members. This activity lowers serum urate levels and reduces the miscible urate pool. Probenecid also competitively inhibits renal secretion of various weak organic acids, which can elevate systemic exposure to select β‑lactam antibiotics. |
|---|---|
| Mechanism of action | Probenecid inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Probenecid may also reduce plasma binding of urate and inhibit renal secretion of uric acid at subtherapeutic concentrations. The mechanism by which probenecid inhibits renal tubular transport is not known, but the drug may inhibit transport enzymes that require a source of high energy phosphate bonds and/or nonspecifically interfere with substrate access to protein receptor sites on the kidney tubules. |
| Pharmacodynamics | Probenecid is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the reabsorption of urate at the proximal convoluted tubule, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits. At the proximal and distal tubles, probenecid competitively inhibits the secretion of many weak organic acids including penicillins, most cephalosporins, and some other β-lactam antibiotics. This results in an increase in the plasma concentrations of acidic drugs eliminated principally by renal secretion, but only a slight increase if the drug is eliminated mainly by filtration. Thus, the drug can be used for therapeutic advantages to increase concentrations of certain β-lactam antibiotics in the treatment of gonorrhea, neurosyphilis, or pelvic inflammatory disease (PID). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Solute carrier family 22 member 6 | Humans | inhibitor |
| Solute carrier family 22 member 11 | Humans | inhibitor |
| Solute carrier family 22 member 8 | Humans | inhibitor |
ADME / PK
| Half-life | 6-12 hours |
|---|---|
| Protein binding | 75-95% |
| Route of elimination | Excreted principally in the urine as monoacyl glucuronide and unchanged drug. Alkalinization of urine increases renal probenecid excretion. |
Formulation & handling
- Oral small‑molecule API suitable for solid‑dose formulations; limited aqueous solubility may require solubility‑enhancing excipients.
- Benzenesulfonamide structure with moderate LogP supports conventional tablet processing without specialized containment.
- GI irritation potential suggests value in film‑coating or co‑formulation approaches to improve gastric tolerability.
Regulatory status
| Lifecycle | Patent expiry status in Canada and the US places the API in a mature phase of its lifecycle, with market conditions largely determined by the extent of generic entry in each jurisdiction. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Probenecid originated from a single innovator product but is now supplied primarily by numerous generic manufacturers and packagers. Branded references such as Benemid were historically marketed in North America, with current availability largely concentrated in the US and Canada. Patent expiry occurred long ago, and the extensive list of packagers reflects an established, mature generic market. |
|---|
Probenecid 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.
Probenecid (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.
Probenecid API manufacturers & distributors
Compare qualified Probenecid API suppliers worldwide. We currently have 2 companies offering Probenecid 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 |
|---|---|---|---|---|---|
| D. K. Pharmachem | Producer | India | India | CoA, JDMF | 2 products |
| Ipca Labs. | Producer | India | India | CoA, USDMF | 69 products |
When sending a request, specify which Probenecid 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 Probenecid 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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