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Micafungin | CAS No: 235114-32-6 | GMP-certified suppliers
A medication that treats invasive and esophageal Candida infections, prevents Candida in stem cell transplant patients, and offers alternative therapy for invasive aspergillosis.
Therapeutic categories
Primary indications
- Indicated for the treatment of candidemia, acute disseminated candidiasis, and certain other invasive <i>Candida</i> infections, as well as esophageal candidiasis, and prophylaxis of <i>Candida</i> infections in patients undergoing hematopoietic stem cell transplantation
- Micafungin is also used as an alternative for the treatment of oropharyngeal candidiases and has been used with some success as primary or salvage therapy, alone or in combination with other antifungals, for the treatment of invasive aspergillosis
- Indicated for the prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation
Product Snapshot
- Micafungin is a parenteral antifungal formulated as an injectable powder, lyophilized for solution
- It is primarily indicated for the treatment and prophylaxis of invasive Candida infections and esophageal candidiasis, including patients undergoing hematopoietic stem cell transplantation, and as alternative therapy for invasive aspergillosis
- Micafungin holds approval in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, micafungin is a lipopeptide derived from fermentation products of Coleophoma empetri. It functions as a selective inhibitor of beta-1,3-D-glucan synthase, an enzyme critical for the synthesis of 1,3-beta-D-glucan, a fundamental polysaccharide component of fungal cell walls. This mechanism results in disruption of fungal cell wall integrity, leading to fungicidal effects against certain Candida species, although typically it exhibits fungistatic activity against Aspergillus species. The absence of beta-1,3-D-glucan synthesis in mammalian cells confers a degree of selective toxicity.
Micafungin demonstrates a pharmacokinetic profile characterized by a high volume of distribution and extensive protein binding. It is primarily metabolized hepatically via arylsulfatase and catechol-O-methyltransferase pathways, with minimal involvement of the cytochrome P450 system. The elimination half-life supports once-daily intravenous dosing. Micafungin shows limited drug-drug interactions and can be administered concomitantly with immunosuppressants such as cyclosporine and tacrolimus, as well as HIV protease inhibitors like ritonavir, without significant alterations in pharmacokinetics.
Safety considerations include monitoring for hepatic function abnormalities and hypersensitivity reactions. It is generally well tolerated, though as with other echinocandins, infusion-related reactions and elevated liver enzymes have been reported. Appropriate renal and hepatic dosing adjustments should be considered based on clinical context.
Micafungin is marketed globally under various brand names but requires careful sourcing due to its complexity as a cyclic lipopeptide oligopeptide. Quality assurance in API procurement must ensure compliance with stringent purity specifications and control of stereochemical integrity to maintain antifungal potency and safety. Suppliers should provide detailed certificates of analysis confirming compliance with pharmacopeial standards.
Identification & chemistry
| Generic name | Micafungin |
|---|---|
| Molecule type | Small molecule |
| CAS | 235114-32-6 |
| UNII | R10H71BSWG |
| DrugBank ID | DB01141 |
Pharmacology
| Summary | Micafungin is a semisynthetic echinocandin antifungal that inhibits beta-1,3-D-glucan synthase, an enzyme critical for fungal cell wall synthesis and absent in mammalian cells. By disrupting beta-1,3-D-glucan production, micafungin exerts fungicidal activity against certain Candida species and fungistatic effects against Aspergillus. It is primarily targeted for invasive Candida infections and prophylaxis in immunocompromised patients. |
|---|---|
| Mechanism of action | Micafungin inhibits the synthesis of beta-1,3-D-glucan, an essential component of fungal cell walls which is not present in mammalian cells. It does this by inhibiting beta-1,3-D-glucan synthase. |
| Pharmacodynamics | Formerly known as FK463, micafungin is a semisynthetic lipopeptide synthesized from a fermentation product of <i>Coleophoma empetri</i> that works as an antifungal agent. It is a glucan synthesis inhibitor of the echinocandin structural class. The U.S. Food and Drug Administration approved micafungin in March 2005. Micafungin inhibits an enzyme essential for fungal cell-wall synthesis. Depending on its concentration, micafungin may be fungicidal against some <i>Candida</i>, but is usually fungistatic against <i>Apergillus</i>. Micafungin can be used concomitantly with a variety of other drugs, including the HIV protease inhibitor ritonavir and the transplant medications cyclosporine and tacrolimus. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 1,3-beta-glucan synthase component FKS1 | Aspergillus niger (strain CBS 513.88 / FGSC A1513) | inhibitor |
ADME / PK
| Absorption | Not absorbed orally |
|---|---|
| Half-life | 14-17 hours |
| Protein binding | Highly (>99%) protein bound in vitro, independent of plasma concentrations over the range of 10 to 100 µg/mL. The primary binding protein is albumin; however, micafungin, at therapeutically relevant concentrations, does not competitively displace bilirubin binding to albumin. Micafungin also binds to a lesser extent to a<sub>1</sub>-acid-glycoprotein. |
| Metabolism | Micafungin is metabolized to M-1 (catechol form) by arylsulfatase, with further metabolism to M-2 (methoxy form) by catechol-O-methyltransferase. M-5 is formed by hydroxylation at the side chain (w-1 position) of micafungin catalyzed by cytochrome P450 (CYP) isozymes. Even though micafungin is a substrate for and a weak inhibitor of CYP3A in vitro, hydroxylation by CYP3A is not a major pathway for micafungin metabolism in vivo. |
| Route of elimination | Fecal excretion is the major route of elimination (total radioactivity at 28 days was 71% of the administered dose). |
| Volume of distribution | * 0.39 ± 0.11 L/kg [adult patients with esophageal candidiasis] |
| Clearance | * 0.359 +/- 0.179 mL/min/kg [Adult Patients with IC with 100 mg] * 0.321 +/- 0.098 mL/min/kg [HIV- Positive Patients with EC with 50 mg] * 0.327 +/- 0.093 mL/min/kg [HIV- Positive Patients with EC with 100 mg] * 0.340 +/- 0.092 mL/min/kg [HIV- Positive Patients with EC with 150 mg] * 0.214 +/- 0.031 mL/min/kg [hematopoietic stem cell transplant recipients 3 mg/kg] * 0.204 +/- 0.036 mL/min/kg [hematopoietic stem cell transplant recipients 4 mg/kg] * 0.224 +/- 0.064 mL/min/kg [hematopoietic stem cell transplant recipients 6 mg/kg] * 0.223 +/- 0.081 mL/min/kg [hematopoietic stem cell transplant recipients 8 mg/kg] |
Formulation & handling
- Micafungin is a small molecule oligopeptide administered exclusively via intravenous injection in lyophilized powder or solution form.
- Due to its low LogP and moderate water solubility, micafungin requires careful formulation to ensure stability and solubility in aqueous parenteral preparations.
- Formulation and handling should consider its peptide structure, favoring sterile, controlled conditions to maintain potency and prevent degradation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has several key patents that expired between 2011 and 2019 in the United States and Canada, indicating a mature market with potential availability of generic formulations in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Micafungin is primarily manufactured and supplied by a limited number of originator companies, with Astellas Pharma Inc. serving as a key packager in the US and Canadian markets. The product has established branded presence mainly in North America, with multiple patent protections filed in the US and Canada. Given the most recent patent expiry dates extending into the mid-2010s, generic competition is likely already present or emerging in these regions. |
|---|
Safety
| Toxicity | Intravenous LD<sub>50</sub> in rats is 125mg/kg. In dogs it is >200mg/kg. No cases of overdosage have been reported. Repeated daily doses up to 8 mg/kg (maximum total dose of 896 mg) in adult patients have been administered in clinical trials with no reported dose-limiting toxicity. The minimum lethal dose is 125 mg/kg in rats, equivalent to 8.1 times the recommended human clinical dose for esophageal candidiasis based on body surface area comparisons. |
|---|
- Intravenous LD50 in rats is 125 mg/kg
- In dogs, it exceeds 200 mg/kg, indicating a moderate acute toxicity profile
- Repeated daily dosing up to 8 mg/kg in clinical settings has not demonstrated dose-limiting toxicity
Micafungin 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.
Micafungin (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.
Micafungin API manufacturers & distributors
Compare qualified Micafungin API suppliers worldwide. We currently have 10 companies offering Micafungin 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 |
| Biocon | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 36 products |
| BrightGene | Producer | China | China | CoA, USDMF | 11 products |
| Jiangsu Hansoh Pharma | Producer | China | China | CoA, USDMF | 10 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| Shanghai Techwell Biophar... | Producer | China | China | CoA, USDMF, WC | 4 products |
| Shanghai Tianwei Biology ... | Producer | China | China | CoA, JDMF | 6 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001 | 762 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
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