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Ketoconazole | CAS No: 65277-42-1 | GMP-certified suppliers
A medication that supports management of diverse systemic and superficial fungal infections and, in some regions, assists clinicians in treating endogenous Cushing's syndrome.
Therapeutic categories
Primary indications
- Ketoconazole is used in the treatment or prevention of fungal infections including blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis
- [FDA Label] In Europe, it is also used in the treatment of endogenous Cushing's syndrome
Product Snapshot
- Ketoconazole is an oral and topical small‑molecule antifungal available in multiple formats including tablets, capsules, creams, shampoos, gels, and solutions
- It is used for systemic and cutaneous fungal infections and is also applied in Europe for endogenous Cushing’s syndrome
- It holds approvals in the US, EU, and Canada, with certain uses remaining investigational
Clinical Overview
Its pharmacological activity is primarily fungistatic. Ketoconazole suppresses fungal growth by interfering with ergosterol biosynthesis, a process essential for maintaining fungal cell membrane integrity. The compound inhibits 14‑alpha‑sterol demethylase, a cytochrome P450–dependent enzyme responsible for converting lanosterol to ergosterol. This inhibition reduces ergosterol content, increases membrane permeability, and leads to accumulation of toxic sterol intermediates such as 14α‑methyl‑3,6‑diol, collectively contributing to impaired fungal viability.
Systemic absorption of oral ketoconazole is variable and influenced by gastric acidity. It undergoes extensive hepatic metabolism, largely via cytochrome P450 enzymes, and exhibits a high potential for drug–drug interactions due to potent inhibition of multiple CYP isoforms, including CYP3A4. Elimination occurs mainly through biliary excretion of metabolites.
Safety considerations are significant. Oral ketoconazole has been associated with hepatotoxicity, including cases of severe hepatic injury, as well as gastrointestinal intolerance. Due to these risks and the availability of safer triazole alternatives, its systemic use has declined. Ketoconazole also inhibits adrenal steroid synthesis, which can lead to reduced cortisol levels. Topical formulations remain in use for dermatological and mucosal fungal conditions, with generally lower systemic exposure.
Notable usage contexts include topical shampoos and creams, while historical systemic brands are now limited in availability due to safety restrictions.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of stereochemistry, impurity profiles, and residual solvent levels, along with evidence of compliance with current GMP and region-specific regulatory expectations.
Identification & chemistry
| Generic name | Ketoconazole |
|---|---|
| Molecule type | Small molecule |
| CAS | 65277-42-1 |
| UNII | R9400W927I |
| DrugBank ID | DB01026 |
Pharmacology
| Summary | Ketoconazole inhibits fungal lanosterol 14‑α‑demethylase, blocking ergosterol synthesis and disrupting membrane integrity, which leads to fungistatic growth arrest. Its activity also causes accumulation of toxic sterol intermediates that further impair membrane‑associated processes. The drug can additionally interact with several human cytochrome P450 enzymes and nuclear receptors, contributing to secondary endocrine effects. |
|---|---|
| Mechanism of action | Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol.This results in inhibition of ergosterol synthesis and increased fungal cellular permeability due to reduced amounts of ergosterol present in the fungal cell membrane. This metabolic inhibition also results in accumulation of 14α-methyl-3,6-diol, a toxic metabolite. The increase in membrane fluidity is also thought to produce impairment of membrane-bound enzyme systems as components become less closely packed. |
| Pharmacodynamics | Ketoconazole, similarly to other azole antifungals, is a fungistatic agent which causes growth arrest in fungal cells thereby preventing growth and spread of the fungus throughout the body. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Lanosterol 14-alpha demethylase | inhibitor | |
| Steroid 17-alpha-hydroxylase/17,20 lyase | Humans | inhibitor |
| Androgen receptor | Humans | binder |
ADME / PK
| Absorption | Ketoconazole requires an acidic environment to become soluble in water.At pH values above 3 it becomes increasingly insoluble with about 10% entering solution in 1 h. At pH less than 3 dissolution is 85% complete in 5 min and entirely complete within 30 min. A single 200 mg oral dose produces a Cmax of 2.5-3 mcg/mL with a Tmax of 1-4 h.Administering ketoconazole with food consistently increases Cmax and delays Tmax but literature is contradictory regarding the effect on AUC, which may experience a small decrease.A bioavailablity of 76% has been reported for ketoconazole. |
|---|---|
| Half-life | Ketoconazole experiences biphasic elimination with the first phase having a half-life of 2 hours and a terminal half life of 8 hours. |
| Protein binding | Ketoconazole is approximately 84% bound to plasma albumin with another 15% associated with blood cells for a total of 99% binding within the plasma. |
| Metabolism | The major metabolite of ketoconazole appears to be M2, an end product resulting from oxidation of the imidazole moiety.CYP3A4 is known to be the primary contributor to this reaction with some contribution from CYP2D6. Other metabolites resulting from CYP3A4 mediated oxidation of the imidazole moiety include M3, M4, and M5. Ketoconazole may also undergo N-deacetylation to M14, , alkyl oxidation to M7, N-oxidation to M13, or aromatic hydroxylation to M8, or hydroxylation to M9. M9 may further undergo oxidation of the hydroxyl to form M12, N-dealkylation to form M10 with a subsequent N-dealkylation to M15, or may form an iminium ion. No metabolites are known to be active however oxidation metabolites of M14 have been implicated in cytotoxicity. |
| Route of elimination | Only 2-4% of the ketoconazole dose is eliminated unchanged in the urine.Over 95% is eliminated through hepatic metabolism. |
| Volume of distribution | Ketoconazole has an estimated volume of distribution of 25.41 L or 0.36 L/kg.It distributes widely among the tissues, reaching effective concentrations in the skin, tendons, tears, and saliva.Distribution to vaginal tissue produces concentrations 2.4 times lower than plasma. Penetration into the CNS, bone, and seminal fluid are minimal. Ketoconazole has been found to enter the breast milk and cross the placenta in animal studies. |
| Clearance | Ketoconazole has an estimated clearance of 8.66 L/h. |
Formulation & handling
- Low aqueous solubility and high lipophilicity support topical, cutaneous, and vaginal formulations, often requiring solubilizers or emulsified systems for uniform delivery.
- Oral formulations benefit from food co‑administration to reduce GI irritation, and multivalent ions can reduce bioavailability, informing excipient selection.
- Solid-state stability is generally good, but light and moisture protection is recommended during handling and storage of bulk API.
Regulatory status
| Lifecycle | The API’s key U.S. patents expired between 2014 and 2020, indicating a well‑established and mature market position. With products marketed in Canada, the US, and the EU, the ingredient is likely in a late lifecycle phase with broad generic availability. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Ketoconazole has long-established originator involvement from Janssen-associated companies, with a broad secondary manufacturing and repackaging base comprising numerous North American and global generic suppliers. Branded and generic products are present in the US, Canada, and the EU, indicating mature international distribution. All listed US patents have expired, supporting the extensive generic competition already evident in the market. |
|---|
Safety
| Toxicity | Symptoms of overdose include acute liver injury, which may include both hepatocellular and cholestatic injury, accompanied by anorexia, fatigue, nausea, and jaundice.In case of overdose, gastric lavage with activated charcoal may be used if within one hour of ketoconazole ingestion otherwise provide supportive care.[FDA Label,L7736] If the patient shows signs of adrenal insufficiency, administer 100 mg hydrocortisone once together with saline and glucose infusion and monitor the patient closely. Blood pressure and fluid and electrolyte balance should be monitored over the next few days. |
|---|
- Overexposure is associated with hepatocellular and cholestatic injury, with reported manifestations such as jaundice, anorexia, fatigue, and nausea
- High systemic levels have been linked to adrenal suppression, necessitating monitoring of cortisol-related effects in controlled settings
- Handling should account for its potential to affect liver function and endocrine pathways, with appropriate controls to limit inhalation or accidental ingestion
Ketoconazole 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.
Ketoconazole (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.
Ketoconazole API manufacturers & distributors
Compare qualified Ketoconazole API suppliers worldwide. We currently have 20 companies offering Ketoconazole API, with manufacturing taking place in 6 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 |
|---|---|---|---|---|---|
| Caesar & Loretz GmbH (CAE... | Distributor | Germany | Unknown | BSE/TSE, CoA, GMP, ISO9001, MSDS | 211 products |
| Darshan Pharmachem (P) Li... | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 10 products |
| Derivados Quimicos | Producer | Spain | Spain | CoA, GMP, USDMF | 18 products |
| Duchefa Farma B.V. | Distributor | Netherlands | Mexico | CoA, GMP, ISO9001, MSDS | 170 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Gufic Biosciences | Producer | India | India | CoA, WC | 6 products |
| Janssen Pharma | Producer | Belgium | Unknown | CEP, CoA, GMP, KDMF, USDMF | 63 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Metapharmaceutical Indust... | Producer | Spain | India | BSE/TSE, CoA, GDP, GMP, MSDS, WC, WHO-GMP | 21 products |
| Nanjing Baijingyu | Producer | China | China | CoA, WC | 3 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | Unknown | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 44 products |
| Prachi Pharmaceuticals | Producer | India | India | CoA, FDA, GMP, ISO9001, USDMF, WHO-GMP | 12 products |
| Quimica Sintetica | Producer | Spain | Unknown | CoA, GMP, USDMF | 51 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sharon Bio-Medicine | Producer | India | India | CoA, GMP, USDMF, WC | 12 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 764 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
When sending a request, specify which Ketoconazole 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 Ketoconazole 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.
Frequently asked questions about Ketoconazole API
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Technical
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Regulatory
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