Abstract
The pneumocandins are semisynthetic analogs of echinocandin-like compounds that have shown efficacy in animal models of systemic candidiasis, disseminated aspergillosis, and pneumocystis pneumonia. However, the most common form of Aspergillus infection in susceptible patients is pulmonary aspergillosis, which was not directly tested in the mouse models used in the past. We have evaluated three pneumocandins, L-693,989, L-731,373, and L-733,560, in a rat model of pulmonary aspergillosis. Male Sprague-Dawley rats were treated for 2 weeks with cortisone and tetracycline and fed a low-protein diet before being inoculated via the trachea with 10(6) conidia of Aspergillus fumigatus H11-20. In the absence of drug treatment, the animals developed a progressive, rapidly fatal bronchopneumonia. All three pneumocandins at doses of 5 mg/kg (intraperitoneally [i.p.] every 12 h [q12h]) were effective in delaying mortality in this model. Survival at day 7 postinfection was 20% among controls (n = 10 for all groups), while it was 60, 80, and 90% in groups that were treated with L-693,989, L-731,373, and L-733,560, respectively. In another trial, survival at day 7 postinfection was 25% among controls (n = 8 for all groups); it was 87.5% in a group treated with amphotericin B (0.5 mg/kg i.p. q12h) and was 100% in a group treated with L-733,560 (0.625 mg/kg i.p. q12h). In a separate trial, aerosol L-693,989 administered 2 h before infection (5 mg/kg) delayed mortality. Eight of the 10 animals treated with aerosol L-693,989 survived for 7 days, whereas only 2 of 10 control animals survived. We conclude that the pneumocandins we tested were highly effective in an animal model of pulmonary aspergillosis.
MeSH Terms
Aerosols
Animals
Anti-Bacterial Agents/administration & dosage,pharmacology,therapeutic use
Antifungal Agents/administration & dosage,pharmacology,therapeutic use
Aspergillosis/drug therapy,microbiology,pathology
Aspergillus fumigatus/drug effects
Infusions, Parenteral
Lung/pathology
Lung Diseases, Fungal/drug therapy,microbiology,pathology
Male
Microbial Sensitivity Tests
Peptides
Peptides, Cyclic/administration & dosage,pharmacology,therapeutic use
Rats
Rats, Sprague-Dawley
Chemicals
Aerosols
Anti-Bacterial Agents
Antifungal Agents
L 731373
L 733560
Peptides
Peptides, Cyclic
L 693989
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Kurtz M B
Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Bernard E M
Edwards F F
Marrinan J A
Dropinski J
Douglas C M
Armstrong D
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