Ascomycin is a naturally occuring macrolide produced by the fermentation of Streptomyces hygroscopicus and an ethyl analog of tacrolimus (FK506), exhibiting strong immunosuppressant properties.
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Ascomycin (FK520) is a macrocyclic antibiotic that also exhibits antifungal and immunosuppressive activity[3]. Ascomycin (Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. IC50 values of FR-900520 for mouse mixed lymphocyte reaction was 0.55 nM. FR-900520, the major component, clearly prolonged skin allograft survival in rats[4]. Ascomycin also had a 3-fold lower immunosuppressive potency in a popliteal lymph node hyperplasia assay, resulting in an equivalent therapeutic index consistent with a common mechanistic dependence on calcineurin inhibition. In 14-day studies, nephrotoxicity was not induced by continuous i.p. infusion of ascomycin at 10 mg/kg/day or daily oral administration (up to 50 mg/kg/day) in rats on a normal diet, nor by continuous i.v. infusion (up to 6 mg/kg/day) in rats on a low salt diet to enhance susceptibility[5].
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