Micafungin

Micafungin Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Micafungin, the second member of the echinocandin class of antifungal agents was launched in Japan for the parenteral treatment of various fungal infections caused by Aspergillus and Candida spp. such as fungaemia and respiratory and gastrointestinal mycoses. This water-soluble semisynthetic cyclic lipopeptide is synthesized by acylation with (5-(4- pentyloxyphenyl)isoxazol-3-yl)benzoate of the cyclic peptide nucleus (FR-179642).obtained by enzymatic cleavage of the naturally occurring echinocandin FR-901379, derived from the fungus Coleophoma empedri Micafungin acts by inhibiting the synthesis of 1,3-beta-glucan, an essential polysaccharide of the cell wall of many pathogenic fungi. Micafungin has a marked fungicidal effect on almost all species of Candida, including fluconazole-resistant spp. C. albicans, C. glabrata, C. Krusei, C. parapsilosis and C. tropicalis and a fungistatic effect on a range of Aspergillus species including A. flaws, A. fumigates and A. terreus. Like caspofungin, micafungin is inactive against Cryptococcus neoformans, and the emerging pathogen Trichosporon cutaneum and Fusarium solani. Micafungin has proved highly effective in mouse models of Cancfidiasis and Aspergillus infections (including those using an amphotericin B- and itraconazole-resistant isolate of A. fumigatus). In phase I studies, micafungin had linear pharmacokinetics with an elimination half-life ranging from 11.7 to 15.2 h after injection and was well tolerated.

• Originator

  Fujisawa (Japan)

• Verwenden

  An echinocandin antifungal drug which inhibits the synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall, and represent a valuable treatment option for fungal infections.

• Verwenden

  Micafungin is an antifungal drug that inhibits the production of β-1,3-glucan, an essential component of fungal cell walls.

• Verwenden

  Micafungin is a semi-synthetic cyclic lipopeptide belonging to the echinocandin class that was reported in 1999 from Fujisawa in Japan. Unlike other marketed semi-synthetic derivatives in this class, micafungin is not derived from echinocandin but rather from FR901379 which contains a phenolic sulphate to enhance aqueous solubility, a serious limitation in the class. Micafungin inhibits the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi and is extensively referenced in the literature with over 700 citations.

• Definition

  ChEBI: A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invas ve candidiasis, and of aspergillosis in patients who are intolerant of other therapy.

• Trademarks

  Mycamine(Astellas);Funguard.

• Antimicrobial activity

  It is active against Aspergillus spp., Candida spp. and the cyst form of Pn. jirovecii. Resistance has rarely been reported.

• Pharmazeutische Anwendungen

  A semisynthetic lipopeptide derived from a fermentation product of Coleophoma empetri. Formulated as the monosodium salt for intravenous infusion.

• Pharmakokinetik

  C_max 50 mg 1-h infusion: c. 5 mg/L 1 h post infusion
  Plasma half-life: 11–15 h
  Volume of distribution: 0.4 L/kg
  Plasma protein binding: 99%
  Blood concentrations increase in proportion to dosage. Unlike anidulafungin and caspofungin, a loading dose is not required.
  Distribution
  The drug is widely distributed, the highest concentrations being found in the liver. Levels in the CSF and urine are negligible.
  Metabolism and excretion
  It is metabolized by the liver and the three inactive metabolites are excreted in the feces (70%). Less than 1% of a dose is eliminated as unchanged drug in the urine. No dosage adjustment is required in patients with severe renal impairment or mild to moderate hepatic impairment. The effect of severe hepatic impairment on micafungin pharmacokinetics has not been studied. Micafungin is not cleared by hemodialysis.

• Clinical Use

  Candidemia and certain invasive forms of candidosis
  Esophageal candidosis
  Prophylaxis of Candida infections in hematopoietic stem cell transplant (HSCT) recipients

• Nebenwirkungen

  Occasional histamine-mediated infusion-related reactions, injection site reactions and transient abnormalities of liver enzymes have been reported. Isolated cases of significant hepatic or renal dysfunction, hepatitis, or liver or renal failure have also been described.

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Ciclosporin: possibly increases ciclosporin concentration.
  Sirolimus: increases sirolimus concentration.

• Stoffwechsel

  Metabolised in the liver by arylsulfatase to its catechol form and further metabolised to the methoxy form by catechol-O-methyltransferase. Some hydroxylation to micafungin via cytochrome P450 isoenzymes also occurs. Exposure to these metabolites is low and metabolites do not contribute to the overall efficacy of micafungin. After 28 days about 71% of a dose is recovered in the faeces and 12% in the urine.

Micafungin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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