Cited by 491Antifungal resistance and susceptibilityFungal Infections and StudiesFungal Plant Pathogen Control

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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.

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Sabatelli, F., Patel, R., Mann, P. A., Mendrick, C. A., Norris, C. C., Hare, R., Loebenberg, D., Black, T. A., McNicholas, P. M.·2006·Antimicrobial Agents and Chemotherapy

DOI 10.1128/aac.00163-06

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Abstract

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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Yasuda, J. M. 2001. An update on antifungal therapy: a focus on systemic agents for invasive fungal infections. Calif. J. Health-Syst. Pharm.13:4-12.

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Background
Crossover between the control of fungal pathogens in medicine and the wider environment, and the threat of antifungal resistance
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Background
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“Our results were in agreement with those of Sabatelli et al.(4), in which of the isolates inhibited by posaconazole only 1.”
ResultInfluential
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Background
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Background
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BackgroundInfluential
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Background
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Background
The antifungal susceptibilities of oral Candida spp isolates from HIV-infected patients
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Rivard, R. G., McCall, S., Griffith, M. E., Hawley, J. S., Ressner, R. A., Borra, H., Moon, J. E., Beckius, M. L., Murray, C. K., & Hospenthal, D. R. (2007) · Medical Mycology · doi:10.1080/13693780701390157 · Cited by 16
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“Compared with FLC or VRC, POS and ISA show extended spectrum activity and improved potency against Candida spp. and molds such as Aspergillus spp. [92–94].”
Background
Zigomicetos y zigomicosis en la era de las nuevas terapias antifúngicas
Torres-Narbona, M., Guinea, J., Muñóz, P., & Bouza, E. (2007) · Revista española de quimioterapia. Suplemento · Cited by 15
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Posaconazole Serum Level on Day 2 Predicts Steady State Posaconazole Serum Level
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“Currently only available as an oral suspension, posaconazole is an important member of the antifungal armamentarium, possessing broad spectrum of antifungal activity.(6,7) Despite data demonstrating improved clinical outcomes, including overall survival, versus”
Background
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Munzen, M. E., Garcia, A. D. G., & Martinez, L. R. (2023) · Future Microbiology · doi:10.2217/fmb-2022-0269 · Cited by 15
Design and synthesis of fluorine aromatic scaffolds containing drugs approved by the US FDA from 2002 to 2022
Xu, P., Zhu, L., Zhang, D., Li, Z., Ge, R., & Tian, Q. (2024) · Results in Chemistry · doi:10.1016/j.rechem.2024.101446 · Cited by 13
Efficacy of voriconazole in vitro and in invertebrate model of cryptococcosis
Spadari, C. D. C., de Bastiani, F. W. M. D. S., Pisani, P. B. B., Melo, A. S. D. A., & Ishida, K. (2019) · Archives of Microbiology · doi:10.1007/s00203-019-01789-8 · Cited by 16
Diffuse primary cutaneous infection by Alternaria alternata in a liver transplant recipient with pulmonary nocardiosis: Importance of prompt identification for clinical resolution
Campoli, C., Ferraro, S., Salfi, N. C. M., Coladonato, S., Morelli, M. C., Giannella, M., Ambretti, S., Viale, P., & Cricca, M. (2020) · Medical Mycology Case Reports · doi:10.1016/j.mmcr.2020.04.007 · Cited by 14
Posaconazole-amino acid cocrystals for improving solubility and oral bioavailability while maintaining antifungal activity and low In vivo toxicity
Vemuri, V. D., Lankalapalli, S., & Guntaka, P. R. (2022) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2022.103491 · Cited by 14
Voriconazole, Combined with Amphotericin B, in the Treatment for Pulmonary Cryptococcosis Caused by C. neoformans (Serotype A) in Mice with Severe Combined Immunodeficiency (SCID)
Silva, E. G., Paula, C. R., Baroni, F. D. A., & Gambale, W. (2011) · Mycopathologia · doi:10.1007/s11046-011-9499-2 · Cited by 14
In Vitro Susceptibility of Environmental Isolates of Exophiala dermatitidis to Five Antifungal Drugs
Duarte, A. P. M., Pagnocca, F. C., Baron, N. C., Melhem, M. D. S. C., Palmeira, G. A., de Angelis, D. D. F., & Attili‐Angelis, D. (2012) · Mycopathologia · doi:10.1007/s11046-012-9597-9 · Cited by 14
Treatment of cryptococcosis in the setting of HIV coinfection
Khawcharoenporn, T., Apisarnthanarak, A., & Mundy, L. M. (2007) · Expert Review of Anti-infective Therapy · doi:10.1586/14787210.5.6.1019 · Cited by 14
Exploration of Medicinal Plants as Sources of Novel Anticandidal Drugs
Kumar, A., Khan, F., & Saikia, D. (2019) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026619666191025155856 · Cited by 12
Activity of fluconazole and its Cu(II) complex towards Candida species
Ząbek, A., Nagaj, J., Grabowiecka, A., Dworniczek, E., Nawrot, U., Młynarz, P., & Jeżowska‐Bojczuk, M. (2014) · Medicinal Chemistry Research · doi:10.1007/s00044-014-1275-7 · Cited by 13
“…pharmacokinetics, spectrum of activity, bioavailability, low toxicity and lack of interaction with other drugs, fluconazole has so far been used to treat more than 100 million people in the world (Charlier et al., 2006; Dery and Hasbun, 2011; Sabatelli et al., 2006; Löffler et al., 1997).”
Correlation between antifungal consumption and the distribution of Candida species in different hospital departments of a Lebanese medical Centre
Awad, L. S., Tamim, H., Abdallah, D., Salameh, M. A., Mugharbil, A., Jisr, T., Zahran, K., Droubi, N., Ibrahim, A., & Moghnieh, R. (2018) · BMC Infectious Diseases · doi:10.1186/s12879-018-3512-z · Cited by 14
How I Treat Histoplasmosis
Hoz, R. M. L., Loyd, J. E., Wheat, L. J., & Baddley, J. W. (2012) · Current Fungal Infection Reports · doi:10.1007/s12281-012-0117-7 · Cited by 13
Posaconazole against Candida glabrata Isolates with Various Susceptibilities to Fluconazole
Spreghini, E., Maida, C. M., Tomassetti, S., Orlando, F., Giannini, D., Milici, M. E., Scalise, G., & Barchiesi, F. (2008) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00130-08 · Cited by 13
“5 g/ml), representing an unusual condition with respect to that reported by recent reports (14, 16).”
Result
Pharmacokinetics of posaconazole in koalas ( Phascolarctos cinereus ) after intravenous and oral administration
Gharibi, S., Kimble, B., Vogelnest, L., Barnes, J., Stadler, C. K., & Govendir, M. (2017) · Journal of Veterinary Pharmacology and Therapeutics · doi:10.1111/jvp.12407 · Cited by 13
Use of posaconazole in the treatment of invasive fungal infections
Mehta, A. K., & Langston, A. A. (2009) · Expert Review of Hematology · doi:10.1586/ehm.09.46 · Cited by 12
Role of New Antifungal Agents in the Treatment of Invasive Fungal Infections in Transplant Recipients: Isavuconazole and New Posaconazole Formulations
Li, J., Nguyen, C. T., & Garcia‐Diaz, J. (2015) · Journal of Fungi · doi:10.3390/jof1030345 · Cited by 12
Allogeneic hematopoietic cell transplantation in patients with acute myeloid leukemia and pulmonary mucormycosis
Schneidawind, D., Nann, D., Vogel, W., Faul, C., Fend, F., Horger, M., Kanz, L., & Bethge, W. A. (2012) · Transplant Infectious Disease · doi:10.1111/tid.12019 · Cited by 12
“In vitro minimum inhibitory concentration (MIC) of POS against mucorales at which 50% or 90% of the isolates were inhibited (MIC50 or MIC90) is comparable to those of LAB (19, 20).”
Result
Comparison of posaconazole and voriconazole in vitro killing against Candida krusei
Cantón, E., Pemán, J., Valentín, A., Bosch, M., Espinel‐Ingroff, A., & Gobernado, M. (2008) · Diagnostic Microbiology and Infectious Disease · doi:10.1016/j.diagmicrobio.2008.07.001 · Cited by 13
“krusei isolates as determined by MIC values (Cantón et al., 2008; Pemán et al., 2006; Sabatelli et al., 2006), but scarce information is available about their fungicidal activity and killing kinetics.”
Method
Associated factors with voriconazole plasma concentration: a systematic review and meta-analysis
Li, X., Hu, Q., & Xu, T. (2024) · Frontiers in Pharmacology · doi:10.3389/fphar.2024.1368274 · Cited by 11
Potency and Preclinical Evidence of Synergy of Oral Azole Drugs and Miltefosine in an Ex Vivo Model of Leishmania ( Viannia ) panamensis Infection
Fernández, O. L., Rosales-Chilama, M., Quintero, N., Travi, B. L., Wetzel, D. M., Gómez, M. A., & Saravia, N. G. (2021) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.01425-21 · Cited by 11
Antimicrobial activity of iodoquinol 1%-hydrocortisone acetate 2% gel against ciclopirox and clotrimazole.
Burnett, B. P., & Mitchell, C. M. (2008) · PubMed · Cited by 11
Susceptibilidad a azoles y anfotericina B de aislados de Candida spp: Experiencia de una red de salud universitaria,entre 2004 y 2010
Lorena Porte, T., León, P., Gárate, C., Guzmán, A. M., Labarca, J. A., & García, P. (2012) · Revista chilena de infectología · doi:10.4067/s0716-10182012000200005 · Cited by 11
Development, clinical utility, and place in therapy of posaconazole for prevention and treatment of invasive fungal infections
Klepser, M. E. (2010) · Drug Design Development and Therapy · doi:10.2147/dddt.s7773 · Cited by 11
Clinical pharmacology of antifungal agents to overcome drug resistance in pediatric patients
Stergiopoulou, T., & Walsh, T. J. (2015) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2015.1000302 · Cited by 11
“and dermatophytes [59,60].”
Pharmacogenomics of Antifungal Agents
Ashbee, H. R., & Gilleece, M. H. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-386882-4.00038-4 · Cited by 11
“including Candida, Aspergillus, dimorphic fungi, and some melanized fungi, but not Fusarium, Scedosporium, or the mucoraceous molds [16].”
BackgroundInfluential
A Rare Case of Fungal Burn Wound Infection Caused by Fusarium solani in Vietnam
Que, A. T., Minh, N. T., Ánh, Đ. N., Lam, N. N., Dung, T. N., Chau, N. T. M., & Le, T. (2020) · Journal of Investigative Medicine High Impact Case Reports · doi:10.1177/2324709620912122 · Cited by 11
Eumycetoma
Bustamante, B., & Campos, P. E. (2010) · Springer eBooks · doi:10.1007/978-1-4419-6640-7_24 · Cited by 11
Actividad antifúngica in vitro de voriconazol: Nuevos datos después de los primeros años de experiencia clínica
Quindós, G., Carrillo‐Muñoz, A. J., Eraso, E., Cantón, E., & Pemán, J. (2007) · Revista Iberoamericana de Micología · doi:10.1016/s1130-1406(07)70043-8 · Cited by 11
Discovery of highly potent antifungal triazoles by structure-based lead fusion
Wang, W., Wang, S., Dong, G., Liu, Y., Guo, Z., Miao, Z., Yao, J., Zhang, W., & Sheng, C. (2011) · MedChemComm · doi:10.1039/c1md00103e · Cited by 10
Candida infection in the intensive care unit: A study of antifungal susceptibility pattern of Candida species in Milad hospital, Tehran, Iran
Alimehr, S., Abad, H. S. E., Fallah, F., Rahbar, M., Mohammadzadeh, M., Vossoghian, S., Tabatabaee, S., Roudbary, M., & Zaini, F. (2015) · Journal de Mycologie Médicale · doi:10.1016/j.mycmed.2015.09.005 · Cited by 10
Fungal Prophylaxis with a Gastro-Resistant Posaconazole Tablet for Patients with Hematological Malignancies in the POSANANTES Study
Péterlin, P., Chauvin, C., Gouill, S. L., Péré, M., Dalichampt, M., Guillaume, T., Garnier, A., Paré, M., Bourgeois, A. L., Moreau, P., et al. (2017) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.01746-17 · Cited by 10
“KEYWORDS posaconazole, prophylaxis, gastro-resistant tablet Posaconazole is an extended-spectrum triazole antifungal agent active againstCandida, Aspergillus, Cryptococcus, and Mucorales (1), with a demonstrated efficacy in the prophylaxis and treatment of invasive fungal disease (IFD) (2–5).”
Background
In vitro antifungal susceptibility testing of fungi in patients with onychomycosis
El‐Hamd, M. A., Elhameed, M. I. A., Fattouh, M., & Saleh, R. A. (2020) · Dermatologic Therapy · doi:10.1111/dth.13429 · Cited by 10
Bacterial and fungal causes of infectious keratitis among patients attending Research Institute of Ophthalmology
Abouzeid, A. I., Eissa, S. A., Aboelnour, A. E., & Awad, A. M. R. (2020) · Bulletin of the National Research Centre/Bulletin of the National Research Center · doi:10.1186/s42269-020-00330-y · Cited by 10
The Role of New Posaconazole Formulations in the Treatment of Candida albicans Infections: Data from an In Vitro Pharmacokinetic-Pharmacodynamic Model
Beredaki, M.-I., Arendrup, M. C., Andes, D. R., Mouton, J. W., & Meletiadis, J. (2021) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.01292-20 · Cited by 10
“fluconazole and voriconazole against Candida albicans isolates (2, 3).”
Background
Cytotoxic Effect of Voriconazole on Human Corneal Epithelial Cells
Sobolewska, B., Guerel, G., Hofmann, J., Bayyoud, T., Bartz‐Schmidt, K. U., & Yoeruek, E. (2015) · Ophthalmic Research · doi:10.1159/000371712 · Cited by 10
Propofol lipidic infusion promotes resistance to antifungals by reducing drug input into the fungal cell
Costa‐de‐Oliveira, S., Araújo, R., Silva-Dias, A., Pina‐Vaz, C., & Rodrigues, A. G. (2008) · BMC Microbiology · doi:10.1186/1471-2180-8-9 · Cited by 10
Use of posaconazole in the treatment of infective rhinocerebral mucormycosis
Kulendra, K. N., Habibi, M., Butler, C. R., Clarke, P. A., & Howard, D. J. (2010) · The Journal of Laryngology & Otology · doi:10.1017/s0022215110000678 · Cited by 10
“12,16 However, in contrast to previous azole antifungals such as fluconazole and voriconazole, it also demonstrates enhanced in vitro activity against mucorales.”
Farmacodinamia y farmacocinética de la micafungina en adultos, niños y neonatos
Catalán-González, M., & Montejo, J. C. (2009) · Revista Iberoamericana de Micología · doi:10.1016/s1130-1406(09)70005-1 · Cited by 9
Blad-Containing Oligomer Fungicidal Activity on Human Pathogenic Yeasts. From the Outside to the Inside of the Target Cell
Pinheiro, A. M., Carreira, A., Rollo, F., Fernandes, R., Ferreira, R. B., & Monteiro, S. (2016) · Frontiers in Microbiology · doi:10.3389/fmicb.2016.01803 · Cited by 10
“…was compared to that of AMB, a commonly used human antifungal agent, and the results demonstrate that the concentrations needed to induce both cellular inhibition and cellular death are very similar to those referenced for AMB (Cantón et al., 2004; Sabatelli et al., 2006; Cordeiro et al., 2013).”
Result
Antifungals: Drug Class, Mechanisms of Action, Pharmacokinetics/Pharmacodynamics, Drug-Drug Interactions, Toxicity, and Clinical Use
Nett, J. E., & Andes, D. R. (2014) · ASM Press eBooks · doi:10.1128/9781555817176.ch22 · Cited by 10
Ciclopirox olamine: an antifungal alternative against cryptococcosis
Oliveira, P. C., MEDEIROS, C., Macêdo, D. P. C., de Andrade, S. L., Correia, M. T. A. L., Mesquita, S. D., de Lima-Neto, R. G., & Neves, R. P. (2010) · Letters in Applied Microbiology · doi:10.1111/j.1472-765x.2010.02914.x · Cited by 10
“Therefore, it is imperative to find alternative antifungal agents for cryptococcosis treatment with no toxicity to mammalian cells (Souza et al. 2005; Mattos et al. 2006; Sabatelli et al. 2006).”
Background
Posaconazole for the Management of Mucosal Candidiasis
Vázquez, J. A. (2007) · Future Microbiology · doi:10.2217/17460913.2.3.245 · Cited by 10
“krusei [51].”
Actualités sur le posaconazole
Paugam, A. (2007) · Médecine et Maladies Infectieuses · doi:10.1016/j.medmal.2006.11.002 · Cited by 10
Understanding antifungal prophylaxis with posaconazole in hematology patients: an evolving bedside to bench story
Sheppard, D. C., Campoli, P., & Duarte, R. F. (2014) · Haematologica · doi:10.3324/haematol.2013.100263 · Cited by 10

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
DOI: 10.1128/aac.00163-06
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
Licence: journals.asm.org/non-commercial-tdm-license (tdm)
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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In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts.

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