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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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Successful multimodal treatment of Paecilomyces lilacinus infection in a dog
Espadale, E., Buckley, L. M., Borio, S., McEwan, N. R., & Schmidt, V. M. (2018) · Veterinary Record Case Reports · doi:10.1136/vetreccr-2018-000627 · Cited by 2
Rath, S., Behera, I. C., & Sahu, M. C. (2018) · Apollo Medicine · doi:10.4103/am.am_43_18 · Cited by 2
Hyalohyphomycosis: Infection Due to Hyaline Moulds
Hospenthal, D. R. (2015) · Springer eBooks · doi:10.1007/978-3-319-13090-3_11 · Cited by 2
Veselov, A. V. (2020) · Clinical Microbiology and Antimicrobial Chemotherapy · doi:10.36488/cmac.2020.2.96-117 · Cited by 2
Posaconazole (Noxafil), an Extended-Spectrum Oral Triazole Antifungal Agent
Chang, M., & Chagan, L. (2008) · PubMed Central · Cited by 2
A rare case of subcutaneous zygomycosis on the neck of an immunocompetent patient
Avendaño, M. V., Contreras, S. A., Dhoble, C. Y., Camacho, A. R., Perez, M. M., & Amari, K. R. (2015) · Case Reports in Internal Medicine · doi:10.5430/crim.v2n3p57 · Cited by 2
Antifungal Agents in Current Pediatric Practice
Cecinati, V., Perillo, T., Brescia, L. P., & Russo, F. G. (2013) · Current Infectious Disease Reports · doi:10.1007/s11908-013-0337-1 · Cited by 2
Bow, E. J., & Bacteriol, D. (2009) · Current Fungal Infection Reports · doi:10.1007/s12281-009-0005-y · Cited by 2
“Posaconazole has, in vitro, been more active than either amphotericin B or voriconazole against Aspergillus species; however, the clinical relevance of this observation is not known [ 11 ,12].”
BackgroundDrug Interaction Profile of Posaconazole
Leung, S., & Poulakos, M. N. (2008) · Internet Journal of Allied Health Sciences and Practice · doi:10.46743/1540-580x/2008.1196 · Cited by 2
Case of a diabetic man cured from rhinocerebral zygomycosis
Lakatos, B., Nikolova, R., Ocskay, L., Csomor, J., & Prinz, G. (2010) · Orvosi Hetilap · doi:10.1556/oh.2010.28969 · Cited by 2
Polyenes for prevention and treatment of invasive fungal infections
Drew, R. H. (2019) · CRC Press eBooks · doi:10.1201/9780429402012-10 · Cited by 2
Wang, Y., Zhao, J., Hu, J., Zhao, X., & Yao, Y. (2020) · Pharmacology & Pharmacy · doi:10.4236/pp.2020.111003 · Cited by 2
“Posaconazole is categorized as a broad-spectrum triazole antifungal agent with potent in vitro and in vivo activities against a large number of clinically important yeasts and models [4] [5].”
BackgroundИлнуровна, В. Р., Lisovskaya, S. А., Mayanskaya, K. A., Samigullin, D. V., & Isaeva, G. S. (2021) · Russian Journal of Infection and Immunity · doi:10.15789/2220-7619-foa-1495 · Cited by 2
“solani обладает наибольшей устойчивостью [25, 29, 31, 32].”
Andes, D. R., & Dismukes, W. E. (2010) · Springer eBooks · doi:10.1007/978-1-4419-6640-7_5 · Cited by 3
Gharibi, S. (2018) · The Sydney eScholarship Repository (The University of Sydney) · Cited by 2
Intravenous posaconazole: key features of clinical pharmacology and practical applications
Veselov, A. V., & Климко, Н. Н. (2022) · Oncohematology · doi:10.17650/1818-8346-2022-17-2-121-133 · Cited by 1
Mucormycosis: Issues, Pathophysiology, Diagnosis and Treatment
Regmi, S., & Mahato, P. L. (2023) · Journal of Karnali Academy of Health Sciences · doi:10.61814/jkahs.v6i1.521 · Cited by 1
Ashok, A., Fernando, S. S., Lee, S. J., Coutsouvelis, J., Mangalore, R. P., & Morrissey, C. O. (2025) · Therapeutic Drug Monitoring · doi:10.1097/ftd.0000000000001425 · Cited by 1
Invasive periodic multivisceral aspergillosis in HIV-infected patient with normal CD4+ cell count
Hasseine, L., Roger, P., Novellas, S., Salvador, F. D., Dunyach‐Remy, C., Bertout, S., & Gari-Toussaint, M. (2011) · Journal de Mycologie Médicale · doi:10.1016/j.mycmed.2011.03.005 · Cited by 1
Prevention and Management of Infectious Complications in Kidney Transplant Recipients
Santos, R. D., & Brennan, D. C. (2014) · Springer eBooks · doi:10.1007/978-1-4939-0342-9_27 · Cited by 1
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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