ミカファンギン

用途キャンデイン系抗真菌薬真菌特有の細胞壁構成成分β-1,3-グルカンの合成酵素を阻害する

説明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.

使用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.

定義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.