Antifungal Activity of LY303366, a Novel Echinocandin B, in Experimental Disseminated Candidiasis in Rabbits

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Antifungal activity of LY303366, a novel echinocandin B, in experimental disseminated candidiasis in rabbits.

The safety and antifungal activity of LY303366 (LY), a new broad-spectrum semisynthetic echinocandin, were studied against disseminated candidiasis in persistently neutropenic rabbits. In vitro time-kill assays demonstrated that LY has concentration-dependent fungicidal activity. The pharmacokinetics of LY in the plasma of nonneutropenic rabbits suggested a linear relationship between dose and ...

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Antifungal efficacy, safety, and single-dose pharmacokinetics of LY303366, a novel echinocandin B, in experimental pulmonary aspergillosis in persistently neutropenic rabbits.

LY303366 is a novel semisynthetic derivative of echinocandin B and a potent inhibitor of fungal (1,3)-beta-D-glucan synthase. The antifungal efficacy and safety of LY303366 were investigated in treatment and prophylaxis of primary pulmonary aspergillosis due to Aspergillus fumigatus in persistently neutropenic rabbits. Treatment study groups were either not treated (controls) or treated with am...

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Mycological and histopathological findings of experimental disseminated candidiasis in dogs

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LY303366 is a semisynthetic derivative of the echinocandin class. During preclinical studies, lethal toxicity was observed in DBA/2 mice pretreated with a cortisone acetate dose followed by treatment with LY303366 at doses ranging from 12.5 to 50 mg/kg of body weight/day given intraperitoneally (i.p.). In the cortisone-treated, uninfected controls, 90% given LY303366 at 50 mg/kg died. Deaths oc...

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The in vivo activity of the Merck antifungal echinocandin drug candidate MK-0991 (L-743,872) was evaluated in mouse models of disseminated candidiasis, aspergillosis, and cryptococcosis. The echinocandins are potent inhibitors of 1,3-beta-D-glucan synthase. Two models of disseminated candidiasis were used. In a Candida albicans mouse survival model with both DBA/2N and CD-1 mice, estimates of t...

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ژورنال

عنوان ژورنال: Antimicrobial Agents and Chemotherapy

سال: 1999

ISSN: 0066-4804,1098-6596

DOI: 10.1128/aac.43.9.2148