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In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts.
Open accessAbstract
The in vitro activity of the novel triazole antifungal agent posaconazole (Noxafil; SCH 56592) was assessed in 45 laboratories against approximately 19,000 clinically important strains of yeasts and molds. The activity of posaconazole was compared with those of itraconazole, fluconazole, voriconazole, and amphotericin B against subsets of the isolates. Strains were tested utilizing Clinical and Laboratory Standards Institute broth microdilution methods using RPMI 1640 medium (except for amphotericin B, which was frequently tested in antibiotic medium 3). MICs were determined at the recommended endpoints and time intervals. Against all fungi in the database (22,850 MICs), the MIC(50) and MIC(90) values for posaconazole were 0.063 microg/ml and 1 mug/ml, respectively. MIC(90) values against all yeasts (18,351 MICs) and molds (4,499 MICs) were both 1 mug/ml. In comparative studies against subsets of the isolates, posaconazole was more active than, or within 1 dilution of, the comparator drugs itraconazole, fluconazole, voriconazole, and amphotericin B against approximately 7,000 isolates of Candida and Cryptococcus spp. Against all molds (1,702 MICs, including 1,423 MICs for Aspergillus isolates), posaconazole was more active than or equal to the comparator drugs in almost every category. Posaconazole was active against isolates of Candida and Aspergillus spp. that exhibit resistance to fluconazole, voriconazole, and amphotericin B and was much more active than the other triazoles against zygomycetes. Posaconazole exhibited potent antifungal activity against a wide variety of clinically important fungal pathogens and was frequently more active than other azoles and amphotericin B.
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“Interestingly, loss of SrbA resulted in a strain of A. fumigatus highly susceptible to fluconazole, an azole that normally has minimal activity against A. fumigatus [58],[59].”
From A Sterol-Regulatory Element Binding Protein Is Required for Cell Polarity, Hypoxia Adaptation, Azole Drug Resistance, and Virulence in Aspergillus fumigatus (2008) · cites this paper as [58]
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Posaconazole vs. Fluconazole or Itraconazole Prophylaxis in Patients with Neutropenia
Cornely, O. A., Maertens, J. A., Winston, D. J., Perfect, J. R., Ullmann, A. J., Walsh, T. J., HELFGOTT, D. C., Hołowiecki, J., Stockelberg, D., Goh, Y. T., et al. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa061094 · Cited by 1,802
Posaconazole or Fluconazole for Prophylaxis in Severe Graft-versus-Host Disease
Ullmann, A. J., Lipton, J. H., Vesole, D. H., Chandrasekar, P. H., Langston, A. A., Tarantolo, S., Greinix, H., de Azevedo, W. M., Reddy, V. S., Boparai, N., et al. (2007) · New England Journal of Medicine · doi:10.1056/nejmoa061098 · Cited by 1,339
Epidemiology of Invasive Mycoses in North America
Pfaller, M. A., & Diekema, D. J. (2010) · Critical Reviews in Microbiology · doi:10.3109/10408410903241444 · Cited by 901
Ashbee, H. R., Barnes, R. A., Johnson, E. M., Richardson, M. D., Gorton, R., & Hope, W. W. (2013) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkt508 · Cited by 721
Isavuconazole treatment for mucormycosis: a single-arm open-label trial and case-control analysis
Marty, F. M., Ostrosky‐Zeichner, L., Cornely, O. A., Mullane, K. M., Perfect, J. R., Thompson, G. R., Alangaden, G. J., Brown, J. W., Fredricks, D. N., Heinz, W., et al. (2016) · The Lancet Infectious Diseases · doi:10.1016/s1473-3099(16)00071-2 · Cited by 714
Metadata
- Authors
- Sabatelli, F., Patel, R., Mann, P. A., Mendrick, C. A., Norris, C. C., Hare, R., Loebenberg, D., Black, T. A., & McNicholas, P. M.
- Affiliations
- Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
- ORCID
- Mann, P. A.
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2006-06
- Volume
- 50
- Issue
- 6
- Pages
- 2009-2015
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- OpenAlex
- W2139126851
- Cited by
- 491
- References
- 38
- Citations by year
- 2026: 8 · 2025: 13 · 2024: 8 · 2023: 8 · 2022: 13 · 2021: 16 · 2020: 17 · 2019: 16 · 2018: 37 · 2017: 20 · 2016: 21 · 2015: 26 · 2014: 33 · 2013: 23 · 2012: 27
- FWCI
- 28.15
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Health Sciences › Medicine › Infectious Diseases › Fungal Infections and Studies
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Fungal Plant Pathogen Control
- Keywords
- posaconazole, fluconazole, itraconazole, voriconazole, amphotericin B, antifungal susceptibility, minimum inhibitory concentration, molds, yeast, Candida, Cryptococcus, Aspergillus, Zygomycetes, triazole antifungals, antifungal resistance, in vitro antifungal activity
- MeSH terms
- Amphotericin B, Antifungal Agents, Aspergillosis, Aspergillus, Candida, Candidiasis, Cryptococcosis, Cryptococcus, Fungi, Humans, Microbial Sensitivity Tests, Mycoses, Pyrimidines, Triazoles, Fluconazole, Itraconazole, Drug Resistance, Fungal, Voriconazole, In Vitro Techniques
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