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Caspofungin | CAS No: 162808-62-0 | GMP-certified suppliers
A medication that treats esophageal candidiasis and invasive aspergillosis in patients unresponsive or intolerant to other antifungal therapies.
Therapeutic categories
Primary indications
- For the treatment of esophageal candidiasis and invasive aspergillosis in patients who are refractory to or intolerant of other therapies
Product Snapshot
- Caspofungin is available as an injectable, lyophilized powder formulation for intravenous administration
- It is indicated primarily for the treatment of esophageal candidiasis and invasive aspergillosis in patients who are refractory or intolerant to other therapies
- The product is approved for use in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Clinically, caspofungin is indicated for the treatment of esophageal candidiasis and invasive aspergillosis, particularly in patients who do not respond to or cannot tolerate alternative therapies. Its antifungal activity is directed against species of Aspergillus and Candida, fungi responsible for a range of systemic and mucosal infections.
Pharmacodynamically, caspofungin exerts its effect by inhibiting the synthesis of beta-(1,3)-D-glucan, a crucial polysaccharide component of the fungal cell wall. This inhibition occurs through targeting the enzyme beta-(1,3)-glucan synthase, impairing cell wall integrity and leading to fungal cell death. Importantly, beta-(1,3)-D-glucan is absent in mammalian cells, which contributes to the drug’s selectivity. Although antifungal resistance remains a theoretical concern, there are limited data on in vitro resistance to caspofungin by Aspergillus species.
Regarding pharmacokinetics, caspofungin is administered intravenously due to limited oral bioavailability. It undergoes slow metabolism with involvement of cytochrome P450 enzymes, including CYP3A4, and displays properties as both an inhibitor and substrate of transporters such as P-glycoprotein and organic anion transporting polypeptides (OATP1B1 and OATP1B3). These interactions may influence the disposition of concomitant drugs. The elimination of caspofungin is via hepatic metabolism, with a half-life supportive of once-daily dosing.
Safety considerations include monitoring for hepatic function due to potential liver enzyme elevations. Hypersensitivity reactions and infusion-related effects have been reported. Caspofungin’s safety profile necessitates attention in patients with preexisting hepatic impairment or receiving other hepatotoxic agents.
From a sourcing and quality perspective, caspofungin raw material must meet stringent pharmaceutical standards for purity, potency, and absence of microbial contamination. Reliable suppliers should provide detailed certificates of analysis and comply with relevant good manufacturing practices (GMP). Given its chemical complexity as a cyclic lipopeptide and peptide class antifungal, consistent manufacturing processes are critical to ensure batch-to-batch reproducibility and efficacy in clinical use.
Identification & chemistry
| Generic name | Caspofungin |
|---|---|
| Molecule type | Small molecule |
| CAS | 162808-62-0 |
| UNII | F0XDI6ZL63 |
| DrugBank ID | DB00520 |
Pharmacology
| Summary | Caspofungin is an antifungal agent that targets 1,3-beta-glucan synthase, inhibiting the synthesis of beta-(1,3)-D-glucan, a critical component of fungal cell walls in Aspergillus and Candida species. By disrupting cell wall integrity, it exerts fungicidal activity against invasive fungal infections. Caspofungin belongs to the echinocandin class, characterized by selective inhibition of fungal glucan synthesis absent in mammalian cells. |
|---|---|
| Mechanism of action | Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of <i>Aspergillus</i> species and <i>Candida</i> species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase. |
| Pharmacodynamics | Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat <i>Aspergillus</i> and <i>Candida</i> infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however <i>in vitro</i> resistance development to Caspofungin by Aspergillus species has not been studied. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 1,3-beta-glucan synthase component FKS1 | Aspergillus niger (strain CBS 513.88 / FGSC A1513) | inhibitor |
ADME / PK
| Absorption | 92% tissue distribution within 36-48 hours after intravenous infusion |
|---|---|
| Half-life | 9-11 hours |
| Protein binding | 97% |
| Metabolism | Metabolized slowly by hydrolysis and N-acetylation |
| Route of elimination | After single intravenous administration of [3H] caspofungin acetate, excretion of caspofungin and its metabolites in humans was 35% of dose in feces and 41% of dose in urine. |
| Clearance | * 12 mL/min [After single IV administration] |
Formulation & handling
- Caspofungin is formulated exclusively for intravenous administration as a lyophilized powder for solution or injection solution.
- It is a small molecule with low lipophilicity (LogP -4.8) and limited water solubility requiring careful reconstitution for parenteral use.
- Stability considerations include protection of the lyophilized powder from moisture and appropriate handling to maintain potency prior to solution preparation.
Regulatory status
| Lifecycle | The API is in a mature market phase in the US and Canada, with key patents expiring between 2013 and 2017, allowing for generic competition; its status in the EU may vary depending on regional patent protections and regulatory approvals. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Caspofungin is primarily manufactured by a single originator company with branded products marketed under the same name across the US, Canada, and EU. Multiple patents have been granted in North America, with the most recent expiring around 2017, indicating that generic competition may already be present or emerging in these markets. Packaging is managed by a limited number of companies supporting the supply chain. |
|---|
Safety
| Toxicity | Side effects include rash, swelling, and nausea (rare) |
|---|
- Potential for hypersensitivity reactions including rash and swelling
- Monitor for signs of allergic response during handling
- Rare incidence of nausea
Caspofungin 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.
Caspofungin (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.
Caspofungin API manufacturers & distributors
Compare qualified Caspofungin API suppliers worldwide. We currently have 8 companies offering Caspofungin API, with manufacturing taking place in 4 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, MSDS, USDMF | 229 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| BrightGene | Producer | China | China | CoA, KDMF | 11 products |
| Mahalaxmi Chemi Pharm | Producer | India | India | CoA | 13 products |
| Senova Technology Co., Lt... | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS, USDMF | 157 products |
| Shanghai Techwell Biophar... | Producer | China | China | CoA, USDMF, WC | 4 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001 | 762 products |
| Xellia | Producer | Denmark | Unknown | CoA, USDMF | 9 products |
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