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Ascomycin (FK 520, FR900520) is a novel neutral macrolide immunosuppressant, isolated from the cultured broth of Streptomyces hygroscopicus subsp. yakushimaensis No. 7238.

In vitro: Ascomycin (FK 520, FR900520) suppressed lymphocyte reaction in a dose dependent fashion. Ascomycin was non-toxic at concentrations less than 3,200 nM, at which the percent inhibition was 18.9%. Ascomycin showed antifungal activity against Aspergillus fumigatus IFO 5840. Ascomycin had no inhibitory effect on bacteria or yeast at 100 μg/ml [1].

In vivo: Ascomycin was dose-dependently effective and clearly prolonged skin allograft survival at 3.2 mg/kg or more, though all skin allografts were rejected within 7 days in rats treated intramuscularly with olive oil. Ascomycin, dissolved in olive oil, showed no adverse effect when administered intraperitoneally to ddY mice (male, 8 weeks old) at 100 mg/kg [1].

Clinical trial: Ascomycin macrolactam derivative, Pimecrolimus, had been tested in both adults and pediatric patients with Atopic Dermatitis in two seperate clinical trials.

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