- Raw materials
- Antifungals
- Antimycotics
- Sulconazole
Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Sulconazole API Manufacturers & Suppliers
1 verified results
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Commercial-scale Suppliers
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Sulconazole | CAS No: 61318-90-9 | GMP-certified suppliers
A medication that treats superficial dermatophytic infections and tinea versicolor by providing broad-spectrum antifungal activity against common fungal pathogens in topical applications.
Therapeutic categories
Primary indications
- Sulconazole solution 1
- 0% is indicated for the treatment of tinea cruris and tinea corporis caused by _Trichophyton rubrum_, _Trichophyton mentagrophytes_, _Epidermophyton floccosum_, and _Microsporum canis_
- And for the treatment of tinea versicolor
- Effectiveness has not been proven in tinea pedis (athlete’s foot)
Product Snapshot
- Sulconazole is available as topical cream and solution formulations
- It is primarily used for the treatment of various dermatophytic fungal infections including tinea cruris, tinea corporis, and tinea versicolor
- Sulconazole topical products are approved for use in the US market
Clinical Overview
Pharmacodynamically, sulconazole exhibits broad-spectrum antifungal activity against dermatophytes, yeasts, and certain filamentous and dimorphic fungi. Its relative inhibition factor (RIF) values are comparable to other imidazoles when tested against pathogenic yeasts and Aspergillus species. In vitro studies indicate that its fungicidal effect is concentration-dependent and varies with the fungal growth phase. Additionally, sulconazole demonstrates antibacterial activity against various Gram-positive bacteria, including Staphylococcus and Streptococcus faecalis, with minimum inhibitory concentrations below 12.5 mg/L.
The antifungal mechanism is consistent with that of imidazole class compounds. Sulconazole inhibits lanosterol 14-alpha demethylase, a cytochrome P450 enzyme essential for the conversion of lanosterol to ergosterol in fungal cell membranes. Disruption of ergosterol biosynthesis compromises membrane integrity, leading to increased fungal cell permeability and growth inhibition.
Key absorption, distribution, metabolism, and excretion (ADME) parameters are not well characterized due to the topical route of administration. Systemic absorption is minimal under recommended use conditions, limiting systemic exposure and related toxicity.
Safety and toxicity profiles indicate good tolerability when used topically. Adverse effects are typically localized and may include mild irritation or contact dermatitis. Sulconazole, like other azole antifungals, is known to inhibit cytochrome P450 enzymes CYP1A2, CYP2C9, and CYP2D6 to varying degrees, which could be relevant in systemic exposure contexts or in co-administered drug metabolism interactions.
From a regulatory perspective, sulconazole is approved for dermatological indications in various global markets. For API sourcing and quality assurance, pharmaceutical manufacturers should ensure compliance with pharmacopeial standards for identity, purity, and potency. Given its classification as a dichlorobenzene derivative and imidazole antifungal, careful control of synthetic impurities and residual solvents is critical to meet regulatory requirements and ensure patient safety.
Identification & chemistry
| Generic name | Sulconazole |
|---|---|
| Molecule type | Small molecule |
| CAS | 61318-90-9 |
| UNII | 5D9HAA5Q5S |
| DrugBank ID | DB06820 |
Pharmacology
| Summary | Sulconazole is a broad-spectrum antifungal agent that targets lanosterol 14-alpha demethylase, a cytochrome P450 enzyme critical for ergosterol synthesis in fungal cell membranes. Inhibition of this enzyme disrupts membrane integrity, leading to increased fungal permeability and growth inhibition. Sulconazole demonstrates activity against dermatophytes, yeasts, filamentous fungi, and certain Gram-positive bacteria. |
|---|---|
| Mechanism of action | The mechanism of action of sulconazole is not well established; however, it is thought to be similar to other imidazole derivatives. The function of imidazoles can be attributed to their structural resemblance to purines essential to metabolism. Imidazoles inhibit lanosterol 14-alpha demethylase, a cytochrome P-450-dependent enzyme in fungi responsible for converting lanosterol to ergosterol. Since ergosterol is required to maintain the integrity of the fungi membrane, the inhibition of lanosterol 14-alpha demethylase leads to increased fungal cellular permeability. Therefore, the use of an imidazole such as sulconazole inhibits fungal growth. |
| Pharmacodynamics | Sulconazole is a broad-spectrum antifungal that inhibits the growth of dermatophytes, yeasts and other filamentous and dimorphic fungi. The relative inhibition factor (RIF), a measurement that represents a fixed portion of the antigungal dose-response curve, can be determined to measure the inhibitory activity of antifungal drugs. Against pathogenic yeasts such as dermatophytes and Aspergilli, sulconazole had similar RIF values compared to other imidazoles. In _in vitro_ conditions, the fungicidal potency of sulconazole depends on its concentration and the growth phase of the inoculum cells. Sulconazole has also shown antibacterial properties _in vitro_, with inhibitory concentrations (MICs) under 12.5 mg/L against several _Staphylococcus_ species, as well as _Streptococcus faecalis_ and several Gram-positive anaerobes. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Lanosterol 14-alpha demethylase | inhibitor |
ADME / PK
| Absorption | A study done on healthy subjects given sulconazole 1% cream over a seven-day period, showed that the total percutaneous absorption of sulconazole after topical administration was 8.71-11.3% of the dose. Another study also done on healthy volunteers given 1 g of sulconazole 1% cream, estimated that about 12% of the dose was absorbed through the skin. In general, topical imidazoles are poorly absorbed (<15%); however, sulconazole may have higher levels of absorption compared to others. |
|---|---|
| Route of elimination | About 6.70% of the dose was recovered in urine, and 2.01% in feces over a 7 day collection period. Radioactivity could be detected in both urine and feces at 7 days potentially due to a reservoir effect. |
Formulation & handling
- Sulconazole is a small molecule intended exclusively for topical use, not suitable for oral or injectable formulations.
- Its high logP and low water solubility indicate significant lipophilicity, requiring formulation strategies to enhance skin penetration.
- Stable as a solid, sulconazole formulations should consider protection from moisture to maintain potency during storage.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently marketed in the US with patent protection having expired, resulting in a mature market characterized by the availability of generic alternatives. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Sulconazole is primarily supplied by originator companies with branded products available in the US market. The presence of multiple branded formulations suggests established originator involvement. Patent expiry details are not provided, limiting assessment of the generic competition landscape at this time. |
|---|
Safety
| Toxicity | Sulconazole has been shown to be embryotoxic in a study of rats given 125 times the human dose (in mg/kg) and also resulted in prolonged gestation and dystocia. There are no adequate or controlled studies in pregnant women, therefore sulconazole should only be used during pregnancy if potential benefit justifies potential risk to the fetus. |
|---|
- Sulconazole demonstrates embryotoxicity at high doses in animal studies, with potential risks including prolonged gestation and dystocia
- Safety data in pregnant women are insufficient
- Exposure should be minimized during pregnancy
Sulconazole is a type of Antimycotics
Antimycotics, a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs), are essential in the treatment of various fungal infections. These powerful medications target and eliminate harmful fungi that can cause infections in humans.
Antimycotics are classified into two main types: systemic and topical. Systemic antimycotics are administered orally or intravenously and work by circulating throughout the body, treating systemic fungal infections that affect internal organs or spread throughout the bloodstream. On the other hand, topical antimycotics are applied externally to treat localized fungal infections such as athlete's foot or yeast infections.
The efficacy of antimycotics lies in their ability to disrupt fungal cell membranes, inhibit the synthesis of fungal DNA or proteins, or interfere with essential metabolic processes specific to fungi. This targeted action minimizes damage to human cells, making these medications relatively safe for patients.
Commonly prescribed antimycotics include azoles, polyenes, allylamines, and echinocandins. Azoles inhibit the synthesis of ergosterol, a vital component of fungal cell membranes, while polyenes bind to ergosterol, resulting in the formation of pores that lead to cell death. Allylamines disrupt the synthesis of ergosterol and inhibit the activity of squalene epoxidase, an enzyme involved in ergosterol production. Echinocandins target the synthesis of β-(1,3)-D-glucan, an essential component of the fungal cell wall.
Antimycotics play a crucial role in the management of fungal infections, offering relief to patients and aiding in their recovery. As with any medication, it is important to follow healthcare professionals' guidance regarding dosage, duration of treatment, and potential side effects to ensure optimal therapeutic outcomes.
Sulconazole (Antimycotics), classified under Antifungals
Antifungals are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) designed to combat fungal infections. These medications are developed to target and eliminate fungi, including yeasts and molds, which can cause a range of diseases in humans and animals.
Antifungals work by interfering with specific components or processes essential for fungal growth and reproduction. They may inhibit the synthesis of fungal cell walls or disrupt the production of ergosterol, a crucial component of fungal cell membranes. By targeting these key mechanisms, antifungal APIs effectively hinder the growth and spread of fungal infections.
The diversity within the antifungal category is reflected in the various classes of antifungal APIs available. Azoles, polyenes, echinocandins, and allylamines are common classes of antifungals. Each class exhibits unique mechanisms of action and targets specific types of fungi. This diversity enables healthcare professionals to tailor treatment plans to the specific fungal infection, optimizing therapeutic outcomes.
Antifungal APIs find application in various pharmaceutical formulations, including oral medications, topical creams, ointments, and intravenous solutions. They are crucial for the treatment of common fungal infections like athlete's foot, ringworm, vaginal yeast infections, and oral thrush. Additionally, antifungals play a crucial role in managing serious systemic fungal infections that can pose significant health risks, especially in immunocompromised individuals.
Overall, antifungal APIs are indispensable tools in the fight against fungal infections, offering effective treatment options and improving the quality of life for patients suffering from these conditions. With ongoing research and development, the antifungal category continues to evolve, providing innovative solutions to combat the ever-changing landscape of fungal pathogens.
Sulconazole API manufacturers & distributors
Compare qualified Sulconazole API suppliers worldwide. We currently have 1 companies offering Sulconazole 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 |
|---|---|---|---|---|---|
| Erregierre | Producer | Italy | Italy | CoA, USDMF | 44 products |
When sending a request, specify which Sulconazole 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 Sulconazole 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.
