In Vitro Activities of the Novel Investigational Tetrazoles VT-1161 and VT-1598 Compared to the Triazole Antifungals against Azole-Resistant Strains and Clinical Isolates of Candida albicans
Open accessAbstract
The fungal Cyp51-specific inhibitors VT-1161 and VT-1598 have emerged as promising new therapies to combat fungal infections, including Candida spp. To evaluate their in vitro activities compared to other azoles, MICs were determined by Clinical and Laboratory Standards Institute (CLSI) method for VT-1161, VT-1598, fluconazole, voriconazole, itraconazole, and posaconazole against 68 C. albicans clinical isolates well characterized for azole resistance mechanisms and mutant strains representing individual azole resistance mechanisms.
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Oteseconazole exhibited potent in vitro activity against most fluconazole-resistant C. albicans and C. krusei isolates (mean MIC ≤ 0.15 μg/mL) and echinocandin-resistant C. glabrata.
“It exhibited potent in vitro activity against most fluconazole-resistant C. albicans and C. krusei isolates (mean MIC ≤ 0.15 μg/mL) as well as echinocandin-resistant C. glabrata [44, 49].”
From Investigational Agents for the Treatment of Resistant Yeasts and Molds (2021) · cites this paper as [49]
Recently, two new drugs, oteseconazole and ibrexafungerp, are characterized by higher efficacy in the treatment of VVC and less potential to cause side effects.
“Recently, two new drugs characterized by higher efficacy in the treatment of VVC and less potential to cause side effects have appeared—oteseconazole and ibrexafungerp [13,14].”
From Treatment of Vulvovaginal Candidiasis—An Overview of Guidelines and the Latest Treatment Methods (2023) · cites this paper as [13]
Tetrazole compounds VT-1129, VT-1161 and VT-1598 are currently awaiting or undergoing clinical trials to treat a wide variety of fungal infections.
“The tetrazole compounds, VT-1129, VT-1161 and VT-1598, so named because of an additional nitrogen on the five-membered azole ring that defines the class, are currently awaiting or undergoing clinical trials to treat a wide variety of fungal infections.53 , 54”
From Molecular and genetic basis of azole antifungal resistance in the opportunistic pathogenic fungus<i>Candida albicans</i> (2020) · cites this paper as [54]
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References 49 · Cited by 52
Research works printed but not linked: 2
- [47]Clinical and Laboratory Standards Institute. 2008. Reference method for broth microdilution antifungal susceptibility testing of yeasts; approved standard, 3rd ed. CLSI document M27-A3. CLSI, Wayne, PA. [Google Scholar]
- [48]Clinical and Laboratory Standards Institute. 2012. Reference method for broth microdilution antifungal susceptibility testing of yeasts; fourth informational supplement CLSI document M27-S4. CLSI, Wayne, PA. [Google Scholar]
- Authors
- Nishimoto, A. T., Wiederhold, N. P., Flowers, S. A., Zhang, Q., Kelly, S. L., Morschhäuser, J., Yates, C. M., Hoekstra, W. J., Schotzinger, R. J., Garvey, E. P., & Rogers, P. D.
- Affiliations
- University of Tennessee Health Science Center (US)
- The University of Texas at San Antonio Health Science Center (US)
- Swansea University (GB)
- University of Würzburg (DE)
- Viamet Pharmaceuticals (United States) (US)
- ORCID
- Venue
- Antimicrobial Agents and Chemotherapy
- Publisher
- American Society for Microbiology
- Published
- 2019-06
- Volume
- 63
- Issue
- 6
- ISSN
- 0066-4804 (ISSN-L)
- 1098-6596
- PMC
- PMC6535515
- OpenAlex
- W2924845564
- Cited by
- 52
- References
- 49
- Citations by year
- 2026: 5 · 2025: 7 · 2024: 7 · 2023: 11 · 2022: 8 · 2021: 8 · 2020: 1 · 2019: 4 · 2018: 1
- FWCI
- 4.03
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Antimicrobial Agents and Chemotherapy (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- HHS | NIH | National Institute of Allergy and Infectious Diseases (R01AI058145)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Life Sciences › Agricultural and Biological Sciences › Ecology, Evolution, Behavior and Systematics › Fungal Plant Pathogen Control
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Fungal and yeast genetics research
- Keywords
- tetrazoles, Candida albicans, azole resistance, triazole antifungals, ERG11, ERG3, MRR1, UPC2, TAC1, resistance mechanisms, minimum inhibitory concentration, clinical isolates
- MeSH terms
- Antifungal Agents, Azoles, Candida albicans, Fungal Proteins, Humans, Microbial Sensitivity Tests, Mutation, Pyridines, Tetrazoles, Transcription Factors, Fluconazole, Drug Resistance, Fungal
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