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Flucytosine | CAS No: 2022-85-7 | GMP-certified suppliers
A medication that treats serious systemic fungal infections caused by Candida and Cryptococcus species when used in combination with amphotericin B.
Therapeutic categories
Primary indications
- For the treatment (in combination with amphotericin B) of serious infections caused by susceptible strains of Candida (septicemia, endocarditis and urinary system infections) and/or Cryptococcus (meningitis and pulmonary infections)
Product Snapshot
- Flucytosine is available as both oral and parenteral formulations including tablets, capsules, and intravenous injection solutions
- It is primarily indicated for use in combination therapy targeting serious fungal infections caused by Candida and Cryptococcus species
- The product is approved and marketed in the US, with both approved and investigational status in various indications
Clinical Overview
Clinically, flucytosine is indicated for the management of serious infections caused by susceptible strains of Candida and Cryptococcus species. It is typically administered in combination with amphotericin B for conditions such as candidal septicemia, endocarditis, urinary tract infections, cryptococcal meningitis, and pulmonary cryptococcosis. Combination therapy is preferred to enhance antifungal efficacy and limit resistance development.
Pharmacodynamically, flucytosine acts as an antimetabolite by penetrating fungal cells through a cytosine-specific permease. Inside the fungal organism, it undergoes enzymatic conversion to 5-fluorouracil (5-FU). The generated 5-FU is extensively incorporated into fungal RNA, disrupting RNA function, and inhibits DNA synthesis by targeting enzymes such as thymidylate synthase. This mechanism leads to impaired nucleic acid synthesis, resulting in unbalanced fungal growth and cell death. The compound’s antifungal activity exhibits synergy with polyene antifungals, particularly amphotericin B.
Key pharmacokinetic features include selective uptake by fungal cells; systemic absorption occurs following oral administration, and the drug is primarily eliminated via renal excretion. Because of its renal clearance, dose adjustments are critical in patients with impaired kidney function to avoid toxicity.
Safety considerations include potential myelosuppression and hepatotoxicity. Flucytosine may cause inadvertent photosensitivity and has immunosuppressive properties. Monitoring of blood counts and liver function tests is advised during therapy. Resistance can arise through mutations affecting cytosine permease or enzymes involved in flucytosine metabolism, limiting its standalone use.
Notable drug formulations have been marketed under various brand names primarily for systemic antifungal therapy. The API should meet stringent purity criteria to ensure absence of impurities that could exacerbate toxicity or reduce efficacy. Reliable sourcing should focus on manufacturers complying with current Good Manufacturing Practices (cGMP) and providing validated certificates of analysis demonstrating appropriate assay, microbial limits, residual solvents, and endotoxin levels. Given the narrow therapeutic index and potential for severe adverse effects, rigorous quality control is essential for pharmaceutical development and regulatory submission.
Identification & chemistry
| Generic name | Flucytosine |
|---|---|
| Molecule type | Small molecule |
| CAS | 2022-85-7 |
| UNII | D83282DT06 |
| DrugBank ID | DB01099 |
Pharmacology
| Summary | Flucytosine is an antifungal antimetabolite that targets fungal nucleic acid synthesis by intracellular conversion to 5-fluorouracil, which inhibits DNA and RNA synthesis. It enters fungal cells via cytosine permease and disrupts nucleic acid metabolism, leading to impaired growth and cell death. Its primary targets include fungal DNA, thymidylate synthase, and related enzymes involved in nucleic acid biosynthesis. |
|---|---|
| Mechanism of action | Although the exact mode of action is unknown, it has been proposed that flucytosine acts directly on fungal organisms by competitive inhibition of purine and pyrimidine uptake and indirectly by intracellular metabolism to 5-fluorouracil. Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. It also appears to be an inhibitor of fungal thymidylate synthase. |
| Pharmacodynamics | Flucytosine is an antimetabolite that acts as an antifungal agent with <i>in vitro</i> and <i>in vivo</i> activity against Candida and Cryptococcus. Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. Antifungal synergism between Ancobon and polyene antibiotics, particularly amphotericin B, has been reported. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | cross-linking/alkylation |
| DNA (cytosine-5)-methyltransferase 1 | Humans | other |
| Thymidylate synthase | Yeast | inhibitor |
ADME / PK
| Absorption | Rapidly and virtually completely absorbed following oral administration. Bioavailability 78% to 89%. |
|---|---|
| Half-life | 2.4 to 4.8 hours. |
| Protein binding | 28-31% |
| Metabolism | Flucytosine is deaminated, possibly by gut bacteria or by the fungal targets, to 5-fluorouracil, the active metabolite. |
| Route of elimination | Flucytosine is excreted via the kidneys by means of glomerular filtration without significant tubular reabsorption. A small portion of the dose is excreted in the feces. |
Formulation & handling
- Flucytosine is a small molecule drug available for both oral and parenteral administration including intravenous injection.
- It exhibits good water solubility (2.14 g/L) and low lipophilicity (LogP -1), indicating favorable aqueous formulation characteristics.
- Handling should consider its halopyrimidine structure, but no specific sensitivity to food or unusual stability issues are reported.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently marketed in the US with patent protection expired, allowing for generic competition. Market dynamics reflect a mature product lifecycle. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Flucytosine involves multiple packagers serving primarily the US market. The branded products, such as Ancobon and flucytosine, have a presence predominantly in the US, with no noted activity in the EU or other regions. Patent expiration has allowed for existing generic competition within the marketplace. |
|---|
Safety
| Toxicity | Oral, rat: LD<sub>50</sub> = >15 gm/kg. |
|---|
- Exhibits low acute oral toxicity in rats (LD₅₀ › 15 g/kg)
- Handle with standard precautions to prevent inhalation or dermal exposure
- Use appropriate personal protective equipment to avoid contamination during manufacturing
Flucytosine 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.
Flucytosine (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.
Flucytosine API manufacturers & distributors
Compare qualified Flucytosine API suppliers worldwide. We currently have 2 companies offering Flucytosine API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Maithri Labs. | Producer | India | India | CoA, USDMF | 5 products |
| Nantong Jinghua | Producer | China | China | CEP, CoA, USDMF, WC | 12 products |
When sending a request, specify which Flucytosine 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.).
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